ライフサイエンスコーパス: carboxamide

1 (5-amino-1-beta-D-ribofuranosyl-imidazole-4-carboxamide).

2 thyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide).

3 es ejects the leader peptide as a C-terminal carboxamide.

4 corresponding beta-C-H arylated/acetoxylated carboxamides.

5 on a new class of trypanocides, the pyrazine carboxamides.

6 ely 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides.

7 eries of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides.

8 ydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamides.

9 nd testing a series of 2,4-dioxopyrimidine-1-carboxamides.

10 rom bisdiazaphospholanes containing tertiary carboxamides.

11 tiary benzoic acid amides and alpha-branched carboxamides.

12 ]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide].

13 lbutanoyl )-1,2,3,4-tetrahydroisoquinoline-3-carboxamide].

14 Previously, we identified phenylisoxazole carboxamide 1 as a hit compound, which inhibited the GAT

15 Quinolinone-3-carboxamide 1, a novel CFTR potentiator, was discovered

16 with the AMPK activator, 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside (AICAR), induced AMP

17 5-Aminoimidazole-4-carboxamide 1-beta-d-ribofuranoside (AICAR, or acadesine

18 5-Aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside (AICAR; 8 mg.kg(-1).

19 vators, e.g. phenformin and aminoimidazole-4-carboxamide 1-beta-d-ribofuranoside inhibited IL-4-evoke

20 Activation of AMPK with 5-aminoimidazole-4-carboxamide 1-beta-d-ribofuranoside, metformin, or overe

21 of the alpha-methyl-alpha-ethyl-beta-hydroxy carboxamide (1 or 2).

22 )-2-((S)-3-phenylpiperidin-1-yl)pyrimidine-4-carboxamide (1, LEI-401) as the first potent and selecti

23 -N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (1; ORG27569) is a prototypical allosteric m

24 r hair cells, we identified a urea-thiophene carboxamide, 1 (ORC-001), as protective against aminogly

25 o-5,6,7,8-tetrahydrothieno[2,3-b]quinoline-2-carboxamide, 1).

26 f 1,8-dihydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides, 1,4-dihydroxy-2-oxo-1,2-dihydro-1,8-naphth

27 sphate (AMP)-kinase using 5-aminoimidazole-4-carboxamide-1-b-D-ribofuranoside (AICAR) has been shown

28 5-Aminoimidazole-4-carboxamide-1-beta-d-ribofuranoside (AICAr) is the precu

29 MP-mimetic AMPK activator 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR) potently sup

30 t with the AMPK activator 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR).

31 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside monophosphate (AICAR

32 studies identified AICAR (5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside) as a pharmacologica

33 of purines and histidine, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranosyl 5'-monophosphate (ZMP

34 onophosphate (ZMP) and/or 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranosyl 5'-triphosphate (ZTP)

35 PK or AICAR conversion to 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranosyl monophosphate (ZMP) w

36 y slows the metabolism of 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranosyl-5'-monophosphate (ZMP

37 the potent AMPK activator 5-aminoimidazole-4-carboxamide-1-d-ribofuranoside (AICAR) attenuated LPS-in

38 that binding of succinyl-5-aminoimidazole-4-carboxamide-1-ribose-5'-phosphate (SAICAR), a metabolite

39 e novel SAR and identify N-butyl-1H-indole-2-carboxamide (11d), which displayed both increased negati

40 imethylamino)phenethyl)-3-pentyl-1H-indole-2-carboxamide (11j) was identified.

41 nd 2-oxo-5-phenyl-N-(4-phenylbutyl)oxazole-3-carboxamide 12a, which resulted in the identification of

42 imethylamino)phenethyl)-3-propyl-1H-indole-2-carboxamide (12d) was identified.

43 dimethylamino)phenethyl)-3-hexyl-1H-indole-2-carboxamide (12f) with a KB of 89.1 nM, which is among t

44 y of a trisubstituted thieno[3,2-b]pyrrole 5-carboxamide 15c that exhibits potent inhibitory activity

45 o-4 -(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide 16d (OICR-9429) is a potent and selective ch

46 l)-N-(trans-4-(18)F-fluoro methylcyclohexane)carboxamide ((18)F-mefway) exhibited promising in vivo p

47 Various 3-methylthiophene/furan-2-carboxamides (1a-e) were derived from their correspondin

48 oxyuridine (Bn-dU) or 5-[N-(1-naphthylmethyl)carboxamide]-2'-deoxyuridine (Nap-dU) replacing dT.

49 were N-(3'-chlorophenyl)-4-oxo-4H-chromene-3-carboxamide (20) (IC50 = 403 pM) and N-(3',4'-dimethylph

50 ethylbicyclo[3.1.1]heptan-3-yl)-1H-indole -2-carboxamide (26), that shows excellent activity against

51 N-(3',4'-dimethylphenyl)-4-oxo-4H-chromene-3-carboxamide (27) (IC50 = 669 pM), acting as competitive

52 N-Isopropyl-1H-indole-2-carboxamide (3) displayed allosteric pharmacology and se

53 ylamino)phenyl]-5-methyl-3-phenylisoxazole-4-carboxamide (3, IC50 = 3 muM), exhibited no activity on

54 In N-(3,4-difluorophenyl-1H-indazole-5-carboxamide (30, PSB-1434, IC50 human MAO-B 1.59 nM, sel

55 4-piperidyl)phenyl]-2-oxo-N-pentyl-oxazole-3-carboxamide 32b as a potent AC inhibitor with optimal ph

56 alternative core was designed, DHBF-3-one-7-carboxamide (36, IC50 = 16.2 muM).

57 -(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide (38a, PSB-1491, IC50 human MAO-B 0.386 nM, >

58 arious picolinamides/oxalylamides/pyrazine-2-carboxamides 4/7/9/11, which were derived from the corre

59 yclobutylmethyl-adenine and 1,2,4-triazole-3-carboxamide (40, MRS7451) nucleobases.

60 ty, and 2-amino- N-benzylbenzo[ d]thiazole-6-carboxamide (4c) was finally identified as a novel poten

61 AO-A) and N-(3,4-dichlorophenyl)-1H-indole-5-carboxamide (53, PSB-1410, IC50 human MAO-B 0.227 nM, >5

62 hydroquinazolin-3-yl)phenyl]- 9H-carbazole-1-carboxamide 6 (BMS-935177) was selected to advance into

63 hyl-1H-pyrazol-3-yl)e thyl]amino}quinoline-3-carboxamide (74) as potent and highly selective ATM inhi

64 -5-(2-(p-tolylamino)thiazol-4-yl)isoxazole-3-carboxamide 7a and N-(pyridin-2-yl)-5-(2-(p-tolylamino)t

65 -1,4-dioxino[2,3-g]thieno[2,3-b]quinoline-8 -carboxamide (8), inhibited this interaction with a measu

66 s, 2-oxo-4-phenyl-N-(4-phenylbutyl)oxazole-3-carboxamide 8a and 2-oxo-5-phenyl-N-(4-phenylbutyl)oxazo

67 -5-(2-(p-tolylamino)thiazol-4-yl)isoxazole-3-carboxamide 8a, were found to show high inhibitory activ

68 -1-yl)-2-oxoethox y] thieno[2,3-b]pyridine-2-carboxamide), a M(2)/M(4) receptor-selective positive al

69 tyl-4-(2-chlorophenyl)-N-methylquinazoline-2-carboxamide), a new analog of (11)C-(R)-PK11195, showed

70 utan-2-yl)-1, 2,3,4-tetrahydroisoquinoline-3-carboxamide, a pan antagonist with nanomolar affinity fo

71 matic SAR investigation of the benzoxazolone carboxamides, a recently described class of AC inhibitor

72 previously reported 4-hydroxy-2-quinolone-3-carboxamides, a structural optimization program led to t

73 razin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide], a positron-emitting, high-affinity ligand

74 l)-6,8-dimethyl-2-(pyridin-2- yl)quinoline-4-carboxamide], a selective GPR55 antagonist.

75 The carboxamide acceptor was shown to be the best candidate.

76 rrolidinones are available by epoxidation of carboxamide-activated bicyclic lactam substrates derived

77 arylation of an N-allyl-5-methylisoxazole-3-carboxamide afforded the E-cinnamylamines plausibly via

78 on/acetoxylation of aliphatic- and alicyclic carboxamides afforded the corresponding beta-C-H arylate

79 However, 5-aminoimidazole-4-carboxamide (AICA) protection was incomplete, suggesting

80 r 5-amino-1-beta-D-ribofuranosyl-imidazole-4-carboxamide (AICAR) or adenovirus expressing constitutiv

81 ilic and highly polar functionalities (e.g., carboxamide, alkylamine, piperazine, piperidine, but not

82 nyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3- carboxamide (AM251) was coapplied with oxo-m.

83 amino] carbonyl phenyl benzo (b)thiophene-2-carboxamide (ANA-12) into the dorsal medial NTS (dmNTS)

84 One of the hits, indole-2-carboxamide analog (1), had low micromolar potency again

85 ed the discovery of the 2-phenylpyrimidine-4-carboxamide analogs as P2Y12 antagonists with nanomolar

86 e report herein the discovery of an indole-2-carboxamide analogue, 3, as a highly potent antitubercul

87 4-(4-phenylpiperazin-1-yl)butyl)-1H-indole-2-carboxamide analogues as high affinity and selective D(3

88 to an exciting new series of (R)-azetidine-2-carboxamide analogues that have sub-micromolar potencies

89 Four novel triazole carboxamide analogues, 24d, 24e, 24f, and 39c, demonstra

90 CEST and NMR analyses reveal highly shifted carboxamide and hydroxyl peaks with intensities that inc

91 Secondary metabolites phenazine-1-carboxamide and pyochelin activate a G-protein-signaling

92 h uniquely has a fluorine atom replacing the carboxamide and stands apart from the current DBOs in re

93 vant 2-hydroxy-3-oxo-2,3-dihydrobenzofuran-2-carboxamides and 2-hydroxy-3-oxo-2,3-dihydrobenzofuran-2

94 cavitand intermediate into the corresponding carboxamides and 2-ketocarboxamides.

95 Here, we designed and synthesized six new carboxamides and 24 new sulfonamides for a detailed stru

96 A broad range of aliphatic carboxamides and alkyl chloroformates are compatible wit

97 arylation/benzylation of aliphatic/alicyclic carboxamides and benzamides were ascertained from the X-

98 s by reductive functionalization of tertiary carboxamides and lactams is described.

99 aced with various functionalities (hydrazine carboxamides and meta-substituted amides) resulting in i

100 2,3-dihydrobenzofuran-7-carboxamide (DHBF-7-carboxamide) and 2,3-dihydrobenzofuran-3(2H)-one-7-carbo

101 nels, ML213 (N-mesitybicyclo[2.2.1]heptane-2-carboxamide) and ICA-069673 N-(6-chloropyridin-3-yl)-3,4

102 s(2-pyridylmethyl)amine-N-ethyl-2-pyridine-2-carboxamide) and the S = 0 [Fe(PaPy3)CO](+) reference co

103 henyl]-1-[3-(2-furanyl)benzoyl]-3-piperidine carboxamide) and/or Fas-activating antibody in the prese

104 o(II)2 complexes featuring CEST-active tetra(carboxamide) and/or hydroxyl-substituted bisphosphonate

105 BC inhibitor, 2-amino-N,N-dibenzyloxazole-5-carboxamide, and the carboxyltransferase inhibitor, andr

106 ydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamides, and 1-hydroxy-2-oxo-1,2-dihydro-1,8-naphth

107 tive coupling of indoline with sulfonamides, carboxamides, and anilines is reported.

108 H-pyrrolo[2,3-d]pyrimidi n-4-yl)piperidine-4-carboxamide] and WEE1 inhibitor AZD1775 [2-allyl-1-(6-(2

109 onding multiple beta-C-H arylated open-chain carboxamides (anti beta-acyloxy amides).

110 nfirm that substituted 2,4-dioxopyrimidine-1-carboxamides are a novel class of potent inhibitors of A

111 ies, and efficacy of a series of quinoline-4-carboxamides are described.

112 he structure of 1-(pyridin-4-yl)piperidine-4-carboxamide, are described.

113 ntly identified 1,8-naphthyridin-2(1H)-one-3-carboxamide as a new scaffold very suitable for the deve

114 ation of 6-(pyrimidin-4-yloxy)-naphthalene-1-carboxamides as a new class of potent and selective huma

115 tly, we have identified the oxazinoquinoline carboxamides as a novel class of CB(2) receptor full ago

116 ydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamides as an INSTI scaffold, making a limited set

117 ationship (SAR) of a library of pyrimidine-4-carboxamides as inhibitors of NAPE-PLD that led to the i

118 b]pyridin-3-yl)amino-benzo[ d]isothiazole-3-carboxamides as mGlu(4) PAMs.

119 the identification of thieno[3,2-b]pyrrole-5-carboxamides as novel reversible inhibitors of KDM1A, wh

120 lino)ethyl)-2-morpholino-4-oxo-4H-chromene-6-carboxamides as PI3Kbeta/delta inhibitors, which led to

121 n-1-yl)-2-oxoethox y]thieno[2,3-b]pyridine-2-carboxamide) as a novel probe of the human M2 and M4 all

122 novel hit series of 5-amino-1,2,3-triazole-4-carboxamides (ATC).

123 Selective 5-aminopyrazole-4-carboxamide-based bumped-kinase inhibitors (BKIs) are ef

124 nt, selective, and brain-penetrant oxazole-4-carboxamide-based inhibitors of glycogen synthase kinase

125 sporidium growth inhibitors identifies the 6-carboxamide benzoxaborole AN7973.

126 m of the thiazine and the oxygen atom of the carboxamide bind to Arg-120 and Tyr-355 via another high

127 oxybenzyl)-4,6-dimethylthieno[2,3-b]pyridine carboxamide), bind to the human M4 mAChR allosteric pock

128 e SIRT3 active site revealed that the common carboxamide binds in the nicotinamide C-pocket and the a

129 enantiopure tetra-carboxylic acid and tetra-carboxamide bis(diazaphospholane) ligands that obviates

130 nyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3 -carboxamide] blocked these responses.

131 -bromo-N-(piperidin-3-yl)benzo[b]thiophene-2-carboxamide (Br-PBTC), which both increases activation a

132 -bromo-N-(piperidin-3-yl)benzo[b]thiophene-2-carboxamide (Br-PBTC), which selectively potentiates the

133 iazol-3-yl)-3,6-dichlorobenzo[ b]thiophene-2-carboxamide (BT3)) significantly increase residual BCKDC

134 es, arising from reorientation of the Gln-63 carboxamide by Arg85' to preclude direct hydrogen bondin

135 ; 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide) can suppress HD pathology caused by mutant

136 o[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide (CB-5083), was developed and demonstrated br

137 identified the 4-pyridinone-benzisothiazole carboxamide compound 1C8 as displaying strong anti-HIV-1

138 These studies demonstrate that indole-2-carboxamide compounds are viable candidates for continue

139 functionalized pyrazolo[1,5- a]pyrimidine-5-carboxamide core or a thieno[3,2- b]pyridine-5-carboxami

140 compounds, which embodies a benzothiophene-2-carboxamide core.

141 rboxamide core or a thieno[3,2- b]pyridine-5-carboxamide core.

142 of CXCR3 that contain tetrahydroisoquinoline carboxamide cores.

143 poration of modified nucleotides such as 5-N-carboxamide-deoxyuridines into random nucleic acid libra

144 notypic screening hit based on a quinoline-4-carboxamide derivative resulted in the highly promising

145 aluation of a series of 1,2-diarylimidazol-4-carboxamide derivatives developed as CB1 receptor antago

146 ruption by small molecules, with thiophene-3-carboxamide derivatives emerging as promising candidates

147 4-Quinolone-3-carboxamide derivatives have long been recognized as pot

148 eloped second- and third-generation indole-2-carboxamide derivatives with improved potency, solubilit

149 Six 6-iodoquinoxaline-2-carboxamide derivatives with various side chains bearing

150 se-resistant penicillins [dicloxacillin] and carboxamide derivatives) and 3 antithrombotic/anticoagul

151 ric 7-hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide derivatives.

152 ofuran-3(2H)-one-7-carboxamide (DHBF-3-one-7-carboxamide) derivatives were synthesized and evaluated

153 H2 ligands from 6 (BMS-986165), a pyridazine carboxamide-derived Tyk2 JH2 ligand as a clinical Tyk2 i

154 hydrazine enables access to dihydroindazole-carboxamides, devoid of a bridge-head nitrogen (C).

155 amide) and 2,3-dihydrobenzofuran-3(2H)-one-7-carboxamide (DHBF-3-one-7-carboxamide) derivatives were

156 Novel substituted 2,3-dihydrobenzofuran-7-carboxamide (DHBF-7-carboxamide) and 2,3-dihydrobenzofur

157 -2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide, dihydrochloride; Abbott Laboratories, Abbot

158 g studies reveal strong N-Li contacts in the carboxamide enolate moiety.

159 y 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide (Ex-527).

160 eries of N-phenyl-4H-thieno[3, 2-b]pyrrole-5-carboxamide for which we obtained X-ray structures of th

161 veal key structural requirements of indole-2-carboxamides for allosteric modulation of CB1: a critica

162 the synthesis of pyrrole-2-carboxylates and -carboxamides from chalcones and glycine esters or amides

163 ion of multiple beta-C-H arylated open-chain carboxamides from the Pd-catalyzed, bidentate ligand-dir

164 3-position of (R)- or (S)- tetrahydrofuran-2-carboxamides furnished the corresponding (2R,3R) and (2S

165 In the case of an activating Weinreb carboxamide, further chemoselective elaboration leads to

166 The introduction of a carboxamide group between the thiazole and pyrrolidine r

167 ng closure of the aldimine moieties with the carboxamide group elicited by N-bromosuccinimide in pyri

168 The parent LCo complex features CEST-active carboxamide groups and an uncoordinated crown ether moie

169 nists bearing substituted 1-methylcyclohexyl-carboxamide groups at position 2 of the benzothiazole sc

170 gh both the nitrogen and oxygen atoms of the carboxamide groups.

171 [(3-methoxyphenyl)amino]-8-methylquinoline-3-carboxamide (GSK 256066) after 1, 2, 6, or 18 hours of e

172 The secondary carboxamides had the best cellular activities, and the 3

173 A novel series of 3-quinoline carboxamides has been discovered and optimized as select

174 age to afford dihydro-oxepino[4,5-b]indole-4-carboxamides, has been discovered.

175 Indole-2-carboxamides have been identified as a promising class o

176 We report that a series of novel indoline-2-carboxamides have been identified as inhibitors of Trypa

177 Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systemat

178 )-4-methyl-N-(piperidin-1-yl)-1H-pyrazo le-3-carboxamide]; however, it had minimal effects on binding

179 N-(4-(benzyloxy)-3-methoxybenzyl)thiophene-2-carboxamide hydrochloride.

180 strategy resulted in lead compound 3 (DHBF-7-carboxamide; IC50 = 9.45 muM).

181 Retention of pyocyanin (PYO) and phenazine carboxamide in the biofilm matrix is facilitated by eDNA

182 ydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamides IN inhibitors to develop compounds that hav

183 oxoethyl]spiro[1H-indene-1,4'-piperidine]-1'-carboxamide) in DA amacrine cells and the selective sst4

184 Some 1,4,5-trisubstituted triazole carboxamides induced dramatic depletion of the examined

185 timization of a series of 4-aminocinnoline-3-carboxamide inhibitors of Bruton's tyrosine kinase are r

186 novel 4-hydroxy-2-(heterocyclic)pyrimidine-5-carboxamide inhibitors of hypoxia-inducible factor (HIF)

187 e exchange of both D-amino acids and D-amino carboxamides into nascent peptidoglycan, but the E. coli

188 y of the substrate alpha-COO(-) group to the carboxamide is absolutely required for catalysis.

189 ipiravir (T705; 6-fluoro-3-hydroxypyrazine-2-carboxamide) is a pyrazine analog that has demonstrated

190 -hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (Ivacaftor) reduces F508-CFTR cellular stabi

191 Metalation of the dinucleating, tetra(carboxamide) ligand HL with Cu(2+) in the presence of py

192 Carboxamide-ligated 8 is shown to be unreactive towards

193 d with aromatic substitutions appended via a carboxamide linker to the 5-position of their bases.

194 Replacement of the carboxamide linker with a methanimine spacer leading to

195 n N-aryl-sulfonamide, ML335, and a thiophene-carboxamide, ML402-define a cryptic binding pocket unlik

196 e show that compounds 5, 10, and 20 indole-2-carboxamides modulate cAMP signaling through CB2.

197 The 1H-indole-2-carboxamide moiety of 1 extends into a secondary pocket

198 that include and extend from the 1H-indole-2-carboxamide moiety of 1.

199 arba-cyclophellitol, with an N-(4-azidobutyl)carboxamide moiety, proved to be a potent inhibitor (Ki

200 ro-4H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide monohydrate]] (galunisertib) (IC(50) = 380 n

201 whereby subtle modifications to the indole-2-carboxamide motif confer dramatic changes in functional

202 hyl-5-oxo-1,4,5,6,7,8-hexahydro-quinoline -3-carboxamide; MQC) dose-dependently suppressed the respon

203 of the pyrimido[5,4-b]indole scaffold at the carboxamide, N-3, and N-5 positions revealed differentia

204 carrying a heterocyclic tail at the indole-2-carboxamide nitrogen as potential anti-HIV/AIDS agents.

205 ]-6-fluoro-3-oxo-2,3-dihydro-1H-isoind ole-4-carboxamide (NMS-P118, 20by).

206 zed a diverse set of methoxybenzothiophene-2-carboxamides, of which the N-benzylated derivative showe

207 -N-[3-(trifluoromethyl)phenyl]-1H-p yrrole-3-carboxamide) or Trpv4 ablation.

208 )-4-piperidyl]carbamoylamino]ethyl]purine-2 -carboxamide], or adenosine shows that the adenosine moie

209 ating H(2) ema(2-) with bridging sulfurs and carboxamide oxygens within Mn-mu-S-CH(2) -C-O, 5-membere

210 acrocycle 19, possessing the phenylimidazole carboxamide P1, exhibited excellent selectivity against

211 -2-benzylidene-3-oxo-2,3-dihydrobenzofuran-7-carboxamide; PARP-1 IC(50) = 434 nM) led to a tetrazolyl

212 enyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide (PHCCC), a small molecule glutamate receptor

213 Here we report a class of piperidine carboxamides (PIPCs) as potent, noncovalent agonists of

214 observations to design a fluorescent D-amino carboxamide probe to label B. subtilis PG in vivo and fo

215 the i+2 position) from an aminocyclopropane carboxamide residue (97:3 er) to an aminoisobutyramide r

216 e lead optimization studies of benzoxazolone carboxamides resulting in piperidine 22m, where we demon

217 5-Aminoimidazole-4-carboxamide ribonucleoside (AICAr), a precursor in purin

218 monophosphate derivative 5-amino-4-imidazole carboxamide ribonucleoside 5'-phosphate (ZMP), an interm

219 c activation of AMPK with 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR) or metformin during s

220 We used 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR) to activate AMPK tran

221 5-Aminoimidazole-4-carboxamide ribonucleotide (AICAR), an AMPK activator, e

222 to nutrient depletion or 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), leading to attenuate

223 activation of AMPK using 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), metformin, and a spe

224 ions but an AMPK agonist, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), suppressed both.

225 e with the AMPK activator 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR).

226 osphoribulosyl)formimino]-5-aminoimidazole-4-carboxamide ribonucleotide (PRFAR).

227 phosphoribosyl)formimino]-5-aminoimidazole-4-carboxamide ribonucleotide (ProFAR) to N'-((5'-phosphori

228 in dramatic elevation of 5-aminoimidazole 4-carboxamide ribonucleotide (ZMP) and growth inhibition i

229 gulation of NRF1 alone by 5-aminoimidazone-4-carboxamide ribonucleotide does not rescue the phenotype

230 fic inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT),

231 ions of both GARFTase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase.

232 ated in both insulin- and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohy

233 nhibited in cells lacking 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohy

234 MTX inhibits 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/inosine mon

235 n or with the AMP mimetic 5-aminoimidazole-4-carboxamide ribonucleotide increases the inhibitory phos

236 lyase, Step 8) and ATIC (5-aminoimidazole-4-carboxamide ribonucleotide transformylase/inosine monoph

237 al. (2015) show that ZMP (5-aminoimidazole-4-carboxamide ribonucleotide) binds to and activates a con

238 one or its precursor ZMP (5-aminoimidazole-4-carboxamide ribonucleotide, also known as AICAR) brings

239 ivation with treatment of 5-aminoimidazole-4-carboxamide ribonucleotide, metformin, or pulsatile shea

240 saturated fatty acids, or 5-aminoimidazole-4-carboxamide ribonucleotide.

241 sphoribulosyl) formimino)-5-aminoimidazole-4-carboxamide-ribonucleotide (PRFAR) in the histidine bios

242 gical activator of AMPK, 5-amino-4-imidazole carboxamide riboside (AICAR), inhibited oxidative stress

243 kinase (AMPK) activator, 5-aminoimidazole-4-carboxamide riboside (AICAR), on tumor necrosis factor a

244 id induce accumulation of 5-aminoimidazole-4-carboxamide riboside 5'-monophosphate (ZMP), an intermed

245 Over 30 years ago, ZTP (5-aminoimidazole-4-carboxamide riboside 5'-triphosphate), a modified purine

246 PK activation by A769662, 5-aminoimidazole-4-carboxamide riboside and C13 and by intracellular dialys

247 , activation of AMPK with 5-aminoimidazole-4-carboxamide riboside or salicylate increased nNOS S1412

248 The 5-aminoimidazole-4-carboxamide riboside served to study the impact of AMP-a

249 milar to that observed by 5-aminoimidazole-4-carboxamide riboside treatment.

250 t the distal axon (0.1 mm 5-aminoimidazole-4-carboxamide riboside) induced a depression of the mean f

251 AMPK activation by 5-aminoimidazole-4-carboxamide riboside, A769662 or C13 attenuated Kv 1.5 c

252 Aminoimidazole carboxamide ribotide (AICAR) is a purine biosynthetic in

253 hydrogen bonding, and the heteroatom of the carboxamide ring of the oxicam scaffold interacts with T

254 olin-2(1H)-yl)ethyl)cyclohexyl)-1H-ind ole-2-carboxamide (SB269652) (1) adopts a bitopic pose at one

255 quinolin-2-yl)ethyl]cyclohexyl]-1H- indole-2-carboxamide (SB269652), a compound supposed to interact

256 dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide scaffold provided 17e, a potent (mGlu1 EC50

257 ntinued exploration of the 5-aminopyrazole-4-carboxamide scaffold to find safe and effective drug can

258 l new molecules with the 4-alkylpiperidine-2-carboxamide scaffold were designed, synthesized, and pha

259 (1-alkylpiperidin-4-yl)methyl]-1H-indazole-3-carboxamide scaffold were prepared taking advantage of a

260 tors (PAMs) based on the 4-alkylpiperidine-2-carboxamide scaffold, we optimized the undecyl moiety at

261 Pyrazolopyrimidine and 5-aminopyrazole-4-carboxamide scaffold-based BKIs are effective in acute a

262 ified on the basis of an azaspiro[2.5]octane carboxamide scaffold.

263 theless, the ability to reduce highly stable carboxamides selectively in the presence of sensitive fu

264 hips (SARs) within the 4-phenylquinazoline-2-carboxamide series of translocator protein (TSPO) ligand

265 creening cascade, a 6-dialkylaminopyrimidine carboxamide series was prioritized for hit to lead optim

266 ies of saturated derivatives from the indole carboxamide series, typified by JNJ 7777120, and incorpo

267 substitutions on both benzoxazolone ring and carboxamide side chain.

268 (2,4-dichlorophenyl)-4-methyl-1H-pyrazol e-3-carboxamide(SR141716A).

269 et hylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide (SR144528, 1), little is known about its bin

270 -N-(4-chlorophenyl)-N, 5-dimethylisoxazole-4-carboxamide stimulated a low level of TGR5 interaction w

271 esis of the 7-oxopyrazolo[1,5-a]pyrimidine-6-carboxamides, structural isomers of our previously repor

272 rize the cAMP signaling response of indole-2-carboxamides structurally correlated to 1 for both CB1 a

273 port a further dissection of the thiophene-3-carboxamide structure.

274 rough the electron-withdrawing effect of the carboxamide substituent.

275 ped for the practical synthesis of unknown 2-carboxamide-substituted dibenzo[d,f][1,3]diazepines.

276 mma-, and delta-C-H bonds of the appropriate carboxamide systems were well documented, there exist on

277 tion of various aliphatic/alicyclic/aromatic carboxamide systems.

278 favorably interact with both carboxylate and carboxamide termini of substrates, in agreement with the

279 ro-phenyl)-benzo[d]imidazo[2,1-b]thiazole-7 -carboxamide), that activated the ISR and dose-dependentl

280 thylnicotinamide, and N1-methyl-4-pyridone-5-carboxamide, that can be used as validation biomarkers f

281 Using 8-aminoquinoline-based aryl carboxamides, the direct ortho-alkylation can be achieve

282 ers and racemates, we find that racemates of carboxamide, thioamide, and their combination adopt self

283 bstituted cyclohexanes as model systems with carboxamide, thioamide, and their combination as functio

284 how that tetrahydropyrazo[1,5-a]pyrimidine-3-carboxamide (THPP) selectively pulls down EchA6 in a ste

285 We developed an indole-carboxamide type mast cell stabilizer, MCS-01, which pro

286 Directing groups such as carbamate, carboxamide, urea, ester, and ketone were found to be ef

287 d prolinamides or N-substituted piperidine-2-carboxamides via a metal-free decarboxylative multicompo

288 -hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, 48, ivacaftor), an investigational

289 onally, a series of alkyl bridged piperazine carboxamides was identified as being of particular inter

290 lecule, 4'-fluoro-N-phenyl-[1,1'-biphenyl]-3-carboxamide, was designed as a generic scaffold that its

291 From a series of hexahydroquinolone-3-carboxamides, we demonstrate that 4-(furan-2-yl)-2-methy

292 a novel class of substituted oxazol-2-one-3-carboxamides were designed and synthesized.

293 A library of 1H-indole-2-carboxamides were discovered as BF3 inhibitors and exhib

294 Indazole- and indole-carboxamides were discovered as highly potent, selective

295 yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide), which has a relatively lower signal-to-noi

296 ed for the synthesis of 5-bromo-1H-pyrrole-2-carboxamides, which are analogues of the pyrrole-2-amino

297 nerally showed higher inhibition compared to carboxamides, which was rationalized based on crystal st

298 alyzed oxidative annulation of 2H-chromene-3-carboxamides with alkynes has been achieved by using the

299 ylene C(sp(3))-H bonds of aliphatic quinolyl carboxamides with alpha-haloacetate and methyl iodide an

300 and cross-coupling of chrysenyl N,N-diethyl carboxamides with o-tolyl and methylnaphthalenyl derivat