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

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

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

7 rom bisdiazaphospholanes containing tertiary carboxamides.

8 onalized indole-2-carboxamides and pyrrole-2-carboxamides.

9 ectron rich anilines but not sulfonamides or carboxamides.

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

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

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

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

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

15 hylpropyl)-1-(2-chlorophenyl)-isoquinoline-3-carboxamide].

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

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

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 yl-3-oxo-2-pheny l-2,3-dihydro-1H-pyrazole-4-carboxamide (1), was identified.

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

24 A series of novel 4-phenylquinazoline-2-carboxamides (1-58) were designed as aza-isosters of PK1

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

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 Activation of AMPK using 5-aminoimidazole-4-carboxamide-1-beta-d-ribofuranoside (AICAR) resulted in

31 lso a molecular target of 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR), which has b

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

33 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside monophosphate (AICAR

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

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 -oxo-3,4-dihydr o-2H-benzo[b][1,4]thiazine-6-carboxamide, 11 (ML276), is a submicromolar inhibitor of

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

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

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 stimulatory activity on CB(1) was exerted by carboxamides 13 (EC(50) = 50 nM) and 21 (EC(50) = 90 nM)

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

46 produced several interesting oxoisoindoline carboxamides (16A, 26B, 28, 51, 60, and 62) that were fu

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

48 perazin-1-yl]ethyl-N-(2-pyridyl) cyclohexane carboxamide ((18)F-FCWAY) PET and CMRglc measurement wit

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

50 ydroacridin-9-yl)amino]decyl}-4 H-chromene-2-carboxamide (19) shows potent combined inhibition of hum

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

52 salvinorin A and the octahydroisoquinolinone carboxamide 1xx.

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

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

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

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

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

58 (2) and (S)-N-(2-oxo-3-oxetanyl)-biphenyl-4-carboxamide (3) inhibit NAAA, prevent FAE hydrolysis in

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

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

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

62 -(3,4-dichlorophenyl)-1-methyl-1H-indazole-5-carboxamide (38a, PSB-1491, IC50 human MAO-B 0.386 nM, >

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

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

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

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

67 -5-(2-(p-tolylamino)thiazol-4-yl)isoxazole-3-carboxamide 7a and N-(pyridin-2-yl)-5-(2-(p-tolylamino)t

68 -1,4-dioxino[2,3-g]thieno[2,3-b]quinoline-8 -carboxamide (8), inhibited this interaction with a measu

69 -5-(2-(p-tolylamino)thiazol-4-yl)isoxazole-3-carboxamide 8a, were found to show high inhibitory activ

70 -1-yl)-2-oxoethox y] thieno[2,3-b]pyridine-2-carboxamide), a M(2)/M(4) receptor-selective positive al

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

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

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

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

75 -chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide (A803467) tonically blocks T-type channels i

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

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

78 lpiperazin-1-yl)phenyl]methyl]-1,2-oxazole-5-carboxamide} acts through a novel mechanism of action, b

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

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

81 conditions, Hofmann rearrangement of various carboxamides affords corresponding carbamates in high yi

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

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

84 , 5-amino-1-beta-d-ribofuranosyl-imidazole-4-carboxamide (AICAR).

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

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

87 )-5-(4-chlorophenyl)-4-methyl-1H-pyrazole -3-carboxamide [AM251] or CB1 gene knockdown) enhanced hMMC

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

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

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

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

92 tter understand the SAR, a group of indole-2-carboxamide analogues were synthesized and assessed for

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

94 y of N-[(4-piperidinyl)methyl]-1H-indazole-3-carboxamide and 4-[(4-piperidinyl)methoxy]-2H-pyrrolo[3,

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

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

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

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

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

100 formation of highly functionalized indole-2-carboxamides and pyrrole-2-carboxamides.

101 2,3-dihydrobenzofuran-7-carboxamide (DHBF-7-carboxamide) and 2,3-dihydrobenzofuran-3(2H)-one-7-carbo

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

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

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

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

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

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

108 Thus, sulfonamides, carbamates, carboxamides, and amines can be successfully employed as

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

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

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

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

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

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

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

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

117 eviously reported a novel series of indole-2-carboxamides as alphavirus replication inhibitors, one o

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

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 We synthesized new N-phenylethyl-1H-indole-2-carboxamides as the first SAR study of allosteric modula

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

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

124 phenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide (BCTC) and clotrimazole or by elevated tempe

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

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

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

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

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

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

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

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

133 ss to prepare 5-aryl-1-benzyl-1H-imidazole-4-carboxamides by the aminocarbonylation of 5-aryl-4-iodo-

134 ; 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide) can suppress HD pathology caused by mutant

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

136 Quinoline-3-carboxamide compounds (Q compounds) have demonstrated ef

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

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

139 of CXCR3 that contain tetrahydroisoquinoline carboxamide cores.

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

141 Starting from a cycloheptathiophene-3-carboxamide derivative recently identified by us for its

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

143 s of 7-oxo-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxamide derivatives as a novel chemotype of selectiv

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

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

146 4-Quinolone-3-carboxamide derivatives have long been recognized as pot

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

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

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

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

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

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

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

154 -2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide, dihydrochloride; Abbott Laboratories, Abbot

155 hiles, is coerced to react smoothly with the carboxamide en route to the oxazole ring by a P,N- or P,

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

157 e anxiogenic drug, N-methyl-beta-carboline-3-carboxamide (FG-7142; a partial inverse agonist at the b

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

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

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

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

162 The presence of the carboxamide functionality was required in order to obtai

163 3-position of (R)- or (S)- tetrahydrofuran-2-carboxamides furnished the corresponding (2R,3R) and (2S

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

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

166 a preferred molecular conformation of the 5-carboxamide group of CBZ and the side chain of Arg62 on

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

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

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

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

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

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

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

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

175 )-4-methyl-N-(piperidin-1-yl)-1H-pyrazo le-3-carboxamide]; however, it had minimal effects on binding

176 N-(4-(benzyloxy)-3-methoxybenzyl)thiophene-2-carboxamide hydrochloride (M8-B), a selective and potent

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

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

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

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

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

182 pounds bearing phenyl and substituted phenyl carboxamides induced lower IL-6 release while maintainin

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

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

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

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

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

188 thyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide) leads to dose-dependent regression of MRTs

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

190 Carboxamide-ligated 8 is shown to be unreactive towards

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

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

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

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

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

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

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

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

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

200 ]-6-fluoro-3-oxo-2,3-dihydro-1H-isoind ole-4-carboxamide (NMS-P118, 20by).

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

202 is are separately specific to carboxylate or carboxamide or have dual specificity.

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

204 thylpropyl)-1-(2-chlorophenyl)isoquinoline-3-carboxamide)] or DPA-714 in excess.

205 e introduction of an ester, an N-substituted carboxamide, or a peptide functionality in the 4-positio

206 )-4-piperidyl]carbamoylamino]ethyl]purine-2 -carboxamide], or adenosine shows that the adenosine moie

207 -N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (ORG27569; 1) represents a new class of indo

208 -[2,4-difluorophenoxy]phenyl)-1H-pyrazo le-4-carboxamide (PF-06250112), a novel highly selective and

209 enyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide (PHCCC) and combined application of mGluR4 P

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

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

212 lamino)-2-oxo-1-(pyridin-3-yl)ethyl)f uran-2-carboxamide, Pubchem CID: 46897844).

213 Thus, indole-2-carboxamides represent a promising new class of antitube

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

215 here that treatment with 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) prevents this heat-in

216 Pre-activation of AMPK by 5-aminoimidazole-4-carboxamide ribonucleoside or transfection with an adeno

217 abolished the ability of 5-aminoimidazole-4-carboxamide ribonucleoside to suppress ethanol-mediated

218 s with the AMPK activator 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR) resulted in increased

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

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

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

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

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

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

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

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

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

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

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

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

231 osphoribulosyl)formimino]-5-aminoimidazole-4-carboxamide ribonucleotide) activates glutaminase cataly

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

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

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

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

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

237 5-Aminoimidazole-4-carboxamide riboside (AICAR), an agent with diverse phar

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

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

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

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

242 hallenge in the presence of aminoimidazole-4-carboxamide riboside and/or after alpha1AMP-activated pr

243 rotein kinase activation by aminoimidazole-4-carboxamide riboside counteracted lipopolysaccharide-ind

244 tion by administration of 5-aminoimidazole-4-carboxamide riboside in Vasp(-/-) mice reduced hepatic s

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

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

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

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

249 ial roles in GSIS such as 5-aminoimidazole-4-carboxamide ribotide (ZMP), GDP-mannose, and farnesyl py

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

251 ion of phosphoribosylsuccinyl-aminoimidazole carboxamide (SAICAR) to phosphoribosylaminoimidazole car

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

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

254 From this study, the cycloheptathiophene-3-carboxamide scaffold emerged as being particularly suita

255 R) studies around the corresponding pyrazole carboxamide scaffold led to the discovery of 2 (AS-136a)

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

257 (1-alkylpiperidin-4-yl)methyl]-1H-indazole-3-carboxamide scaffold were prepared taking advantage of a

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

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

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

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

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

263 hin the (5-hydroxy-2-adamantyl)-pyrimidine-5-carboxamide series.

264 The oxoisoindoline carboxamides series described here may be valuable for f

265 substitutions on both benzoxazolone ring and carboxamide side chain.

266 However, the C3 substituents of the indole-2-carboxamides significantly impact the allostery of the l

267 (2,4-dichlorophenyl)-4-methyl-1H-pyrazol e-3-carboxamide(SR141716A).

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

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

270 -N-(4-chlorophenyl)-N, 5-dimethylisoxazole-4-carboxamide stimulated cAMP formation but did not induce

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 A wide range of N-nucleophiles, including carboxamides, sulfonamides, azoles, and anilines, can be

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

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

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

278 27569; 1) represents a new class of indole-2-carboxamides that exhibit allostery of CB1.

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 found that within the structure of indole-2-carboxamides, the presence of the indole ring is preferr

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

284 Hofmann rearrangement of carboxamides to carbamates using Oxone as an oxidant can

285 itors that utilize various 5-membered cyclic carboxamides to conformationally restrain key pharmacoph

286 ] annulation between a terminal alkyne and a carboxamide using a gold-catalyzed oxidation strategy.

287 mann rearrangement of aromatic and aliphatic carboxamides using (tosylimino)phenyl-lambda(3)-iodane,

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

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

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

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

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

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 ide (SAICAR) to phosphoribosylaminoimidazole carboxamide, which occurs in the de novo synthesis of IM

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

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 ions and high selectivity in the reaction of carboxamides with PhINTs allow the isolation of the init