ライフサイエンスコーパス: oxadiazole

1 for the interconversion of thiazolidinone to oxadiazole.

2 e from 2-(2-nitrophenyl)-5-substituted-1,3,4-oxadiazole.

3 yl amidines as well as a (11)C-labeled 1,2,4-oxadiazole.

4 idopentylamino)-5-((indol-3-yl)methyl)-1,2,4-oxadiazole.

5 ubsequent cyclization to (11)C-labeled 1,2,4-oxadiazoles.

6 ing pyrimidines, imidazoles, tetrazoles, and oxadiazoles.

7 ycloaddition with acetonitrile to give 1,2,4-oxadiazoles.

8 owever, the highest-ranked library compound, oxadiazole 1, was pursued as a potential "near-miss" wit

9 and 1,2,3-triazines; 1,2-diazines; and 1,3,4-oxadiazoles), 1-aza-1,3-butadienes, alpha-pyrones, and c

10 By exploring three heterocycle spacers (oxadiazole, 1,2,3-triazole, and isoxazole) on the ring-f

11 Salts generated from linked 1,2,4-oxadiazole/1,2,5-oxadiazole precursors exhibit good to e

12 adiazoles 9 > tetrazoles, the isomeric 1,2,4-oxadiazoles 10, 1,3,4-thiadiazoles > oxazoles including

13 We report in this study that oxadiazole 11a and salvidivin A (12a), a photooxygenatio

14 + 2]/[3 + 2] cycloaddition cascade of 1,3,4-oxadiazole 15, which provided the highly functionalized

15 eratinocyte hyperproliferation was the 1,2,4-oxadiazole 18, the potency of which was combined with co

16 potency at the DAT to cocaine, ester 1a, and oxadiazole 1b, and both fully substitute for cocaine and

17 phen-2-yl)-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazole (1d) as a novel apoptosis inducer through our

18 otonated hydrazone motif linked to the 1,2,5-oxadiazole 2-oxide subunit was synthesized, indicating t

19 The activity of the oxadiazole 2-oxides was associated with a donation of ni

20 Phosphinic amides and oxadiazole 2-oxides, identified from a quantitative high

21 f the most promising hit (5) resulted in the oxadiazole-2-amine 37 showing pure antagonistic activity

22 Here, we continue our explorations of an oxadiazole-2-oxide class of compounds we recently identi

23 sults of these studies verify the utility of oxadiazole-2-oxides as novel inhibitors of TGR and as ef

24 Analogues of the oxadiazole 24 were synthesized to experimentally corrobo

25 e validated hits, a 2-anilino-5-phenyl-1,3,4-oxadiazole (24) and a phenylmethylene hydantoin (28), bo

26 , 2,5-bis(3,5-dinitro-1H-pyrazol-4-yl)-1,3,4-oxadiazole (3), was achieved through a simple and straig

27 01 C. difficile strains) and narrow-spectrum oxadiazole (3-(4-(cyclopentyloxy)phenyl)-5-(4-nitro-1H-i

28 chistosome-infected mice with 4-phenyl-1,2,5-oxadiazole-3-carbonitrile-2-oxide led to marked reductio

29 t interaction landscape of a series of 1,3,4-oxadiazole-3-ones identified in a phenotypic screen to h

30 3,5-trimethyl-1H-pyrazol-4-y l)methyl)-1,3,4-oxadiazole (34c) is a high affinity inhibitor of both Pl

31 Although 1,2,5-oxadiazole 37 and pyrazine 39 are iso-pi-electronic with

32 nt of the Z-phenylhydrazones of 3-acyl-1,2,4-oxadiazoles 3a-c into the relevant 2-phenyl-2 H-1,2,3-tr

33 igh density, 5,5'-dinitramino-3,3'-azo-1,2,4-oxadiazole (4), was obtained by the nitration of 5,5'-di

34 soluble guanylyl cyclase, because 1H-(1,2,4)oxadiazole (4,3-alpha) quinoxaline-1-one (soluble guanyl

35 This increase is blocked by [(1)H](1,2,4)oxadiazole(4,3-a)quinoxalin-1-one (ODQ, 50 microM), an i

36 The oxidation of the sGC heme by 1H-(1,2,4)oxadiazole(4,3-a)quinoxalin-1-one completely inhibited t

37 The effects were inhibited with 1H-(1,2, 4)oxadiazole(4,3-a)quinoxalin-1one (ODQ).

38 ctive guanylate cyclase inhibitor, 1H-(1,2,4)oxadiazole(4,3-alpha)quinoxaline-1-one (ODQ), on the cir

39 (2) and 3,3'-bis(azidomethyl)-5,5'-bis(1,2,4-oxadiazole) (4) were characterized using X-ray diffracti

40 on by laser photolysis of 3,5-diphenyl-1,2,4-oxadiazole-4-oxide (4) and studied by time-resolved infr

41 s, N-hydroxyureas, nitrile oxides, and 1,2,4-oxadiazole-4-oxides were highlighted.

42 ctive guanylyl cyclase inhibitor, 1H-[1,2,4]-oxadiazole-[4,3-a]quinoxalin-1-one, eliminated SNP-induc

43 thelial denudation, deferoxamine, 1H-(1,2,4)-oxadiazole-[4,3-a]quinoxalin-1-one, or glibenclamide had

44 ked PAL activation, inhibition by 1H-(1,2,4)-oxadiazole[4, 3-a]quinoxalin-1-one was not entirely comp

45 The guanylate cyclase inhibitor 1H-[1,2,4]oxadiazole[4,3-a]quinoxalin-1-one (ODQ) inhibited the ef

46 ially prevented PAF shock, neither 1H-[1,2,4]oxadiazole[4,3-a]quinoxalin-1-one (ODQ) nor sGCalpha1 de

47 ollowed by IR group procedure; (4) 1H-[1,2,4]oxadiazole[4,3-a]quinoxalin-1-one (ODQ)+RIPC+IR: ODQ (sG

48 y the guanylate cyclase inhibitor 1H-[1,2,4] oxadiazole[4,3-a]quinoxalin-1-one and the *NO scavenger

49 inhibition of guanylate cyclase by 1H-[1,2,4]oxadiazole[4,3-a]quinoxalin-1-one did not restore neutro

50 6-anilino-5,8-quinolinedione and 1H-(1,2,4)-oxadiazole[4,3-a]quinoxalin-1-one, two inhibitors of gua

51 was reversed by the sGC inhibitor 1H-(1,2,4)-oxadiazole[4,3-a]quinoxalon-1-one (ODQ),suggesting the i

52 S3 cells was abolished by either 1H-(1,2,4)-oxadiazole[4,3-a]quinoxalon-1-one, a potent inhibitor fo

53 NAME pretreatment and partially by 1H-[1,2,4]oxadiazole[4,3-a]quinoxqalin-1-one pretreatment.

54 hiophen-2-yl)-3-(5-chloropyridin-2-yl)-1,2,4-oxadiazole (4l) has been found to have in vivo activity

55 one-pot conversion of aminodioximes to 1,2,3-oxadiazole-5-amines via Mitsunobu-Beckmann rearrangement

56 ridines and pyrazines substituted with 1,2,4-oxadiazole-5-ones, 1,2,4-oxadiazole-5-thiones, and 1,3,4

57 Tetrazole 19 (ED50 0.18 muM) and oxadiazole-5-thione 25 (ED50 0.36 muM) were 12- and 6-fo

58 stituted with 1,2,4-oxadiazole-5-ones, 1,2,4-oxadiazole-5-thiones, and 1,3,4-oxathiazoline-2-ones wer

59 The trifluoromethyl-substituted 1,2,4-oxadiazole 59 showed an IC(90) of 33.5 muM.

60 + 2]/[3 + 2] cycloaddition cascade of 1,3,4-oxadiazole 9, which affords the stereochemically rich an

61 ibitor activity: 1,3,4-oxadiazoles and 1,2,4-oxadiazoles 9 > tetrazoles, the isomeric 1,2,4-oxadiazol

62 iazole screening hit, a series of piperazine oxadiazole ACC inhibitors was developed.

63 lcarbazoles and the electron-accepting 1,3,4-oxadiazoles accelerates the charge recombination as the

64 clic bioisosteres, such as substituted 1,3,5-oxadiazoles, afforded compounds with excellent oral bioa

65 We screened a library of 75 oxadiazoles against C. difficile ATCC 43255.

66 NAD(+), and the crystal structure of a 1,2,4-oxadiazole analog in complex with Sirt2 and ADP-ribose r

67 n of a highly potent 3-trifluoromethyl-1,2,4-oxadiazole analogue 23 (PfNF54 IC(50) = 0.012 muM; PfK1

68 to phosphotyrosine) some of the best 1,2, 4-oxadiazole analogues are approximately 1 order of magnit

69 and synthesis of a series of diphenyl-1,2,4-oxadiazole analogues derived from RLX-33.

70 A series of 1,2,4-oxadiazole analogues has been shown to be potent and sel

71 f 90 in rats revealed that the 5-amino-1,3,4-oxadiazole analogues may have limited brain permeability

72 7 nM) and 44 (EC(50) = 7.8 nM), featuring an oxadiazole and a pyridine moiety, respectively, demonstr

73 e bioisosteric replacement of the amide with oxadiazole and alpha,alpha-dimethylation of the carboxyl

74 ion with a single methylene unit between the oxadiazole and heterocyclic ring afforded a SphK1-select

75 The synthetic method for introducing 1,3,4-oxadiazole and the systematic study of 1,3,4-oxadiazole-

76 The oxadiazole and thiadiazole derivatives with the most fav

77 tly influenced the inhibitor activity: 1,3,4-oxadiazoles and 1,2,4-oxadiazoles 9 > tetrazoles, the is

78 ituted-2-[(3,5-dinitrobenzyl)sulfanyl]-1,3,4-oxadiazoles and 1,3,4-thiadiazoles as a new class of ant

79 2-Amino-substituted 1,3,4-oxadiazoles and 1,3,4-thiadiazoles were synthesized via

80 Additional interactions were found for oxadiazoles and alkynyl derivatives with Asn382, suggest

81 scovery of two new types of ligands, pyridyl oxadiazoles and pyridyl oximes.

82 ro groups, namely, 2,5-dinitrobenzylsulfanyl oxadiazoles and tetrazoles, maintained high antimycobact

83 ed amides and azoles, such as oxazole, 1,2,4-oxadiazole, and 1,3,4-oxadiazole, as well as other relat

84 (DART) trioxane derivatives (11 thiazoles, 2 oxadiazoles, and 10 carboxamides) and have screened them

85 5-membered heterocycles such as tetrazoles, oxadiazoles, and triazoles can augment the inhibitory ac

86 compound 57, a new, totally synthetic 1,2,4-oxadiazole antibacterial agent, is described.

87 (4-(4-(trifluoromethyl)phenoxy)phenyl)-1,2,4-oxadiazole (antibiotic 75b) was efficacious in a mouse m

88 We report herein that oxadiazole antibiotics exhibit bactericidal activity aga

89 ntermediates, a broad range of a-amino 1,3,4-oxadiazole architectures were accessed from carboxylic a

90 Oxadiazoles are a class of heterocycle containing one ox

91 + 2]/[3 + 2] cycloaddition cascade of 1,3,4-oxadiazoles are disclosed in which the scope and utility

92 Oxadiazoles are five-membered heteroaromatic rings conta

93 Oxadiazoles are frequently occurring motifs in druglike

94 turing a second stage copper-catalyzed 1,3,4-oxadiazole arylation, was found to tolerate (hetero)aryl

95 Herein, we describe the discovery of an oxadiazole as a bactericidal anti-C. difficile agent tha

96 reening using STRP identified the azetidinyl oxadiazole as a moiety that selectively reacts with cyst

97 s the metal binding group connected to 1,3,4-oxadiazole as the central scaffold.

98 This study unveils 1,2,4-oxadiazoles as a novel class of spore germination inhibi

99 such as oxazole, 1,2,4-oxadiazole, and 1,3,4-oxadiazole, as well as other related five-membered heter

100 A class of 3,5-diphenyl-1,2,4-oxadiazole based compounds have been identified as poten

101 ribe the structure-activity studies on 1,2,4-oxadiazole-based analogues, which are potent inhibitors

102 ionalized, tridentate, and unsymmetric 1,3,4-oxadiazole-based complexants is reported.

103 h-content imaging, we identified novel 1,2,4-oxadiazole-based compounds, which allow human macrophage

104 ere, we describe the synthesis of five 1,3,4-oxadiazole-based donor-acceptor materials, using dendrit

105 We previously identified a 1,2,4-oxadiazole-based scaffold from the screening of the "Kin

106 A series of highly luminescent oxadiazole-based stilbene molecules (OXD4, OXD8, OXD10,

107 cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of no

108 tether linking the initiating dienophile and oxadiazole bears a chiral substituent that controls the

109 We document that the oxadiazole binds to the lytic transglycosylase SleC and

110 by replacing the ester moiety with a methyl oxadiazole bioisostere.

111 mides (e.g., 31) and the corresponding 1,3,4-oxadiazole bioisosteres derived from the 2-AMPP scaffold

112 oxadiazole and the systematic study of 1,3,4-oxadiazole-bridged compounds provide a theoretical basis

113 In this study, a series of 1,3,4-oxadiazole-bridged furazans was prepared.

114 d thermal stabilities of mono- and bis-1,3,4-oxadiazole bridges are considered.

115 bsequently revealed that many members of the oxadiazole class (and surprisingly also 1) act via diver

116 relationship (SAR) for the newly discovered oxadiazole class of antibiotics is described with evalua

117 y)phenyl)-5-(4-nitro-1H-imidazol-2-yl)-1,2,4-oxadiazole; compound 57), which is not active against co

118 ve group with the discovery of an azetidinyl oxadiazole containing a small molecule that augments the

119 ip (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein

120 the preparation of thiazole-, oxazole-, and oxadiazole-containing biarylhydroxamic acids by a short

121 The oxadiazole-containing compound, HSGN-94, has been shown

122 e activity identified a subset of 3,5-diaryl-oxadiazole-containing compounds as FLuc inhibitors.

123 A library of isoxazole and 1,2,4-oxadiazole-containing diheterocyclic compounds has been

124 We describe 1,3,4-oxadiazole-containing hydroxamates (2) and 2-aminoanilid

125 Non-oxadiazole-containing oligomers 9 and 12 showed n-channe

126 Compound 11 is the first example of an oxadiazole-containing organic semiconductor (OSC) oligom

127 However, oxadiazole-core materials 14 and 16 were inactive in tra

128 ions of a suitably substituted 2-amino-1,3,4-oxadiazole defining a novel oxadiazole --> furan --> ben

129 The 5-amino-1,3,4-oxadiazole derivatives (84, 88-90) had significantly imp

130 e describe the discovery of a novel class of oxadiazole derivatives from which potent and selective C

131 3)H (TfOH) results in the formation of 1,2,4-oxadiazole derivatives in yields up to 96%.

132 ition of the 2-keto-oxazole and 2-keto-1,3,4-oxadiazole derivatives significantly enhances binding af

133 Three pyrene-oxadiazole derivatives were synthesized and characterize

134 A series of oxadiazole derivatives were synthesized and evaluated as

135 rein, we report fluorogenic probe 4, a 1,3,4-oxadiazole designed to bind selectively to transthyretin

136 compounds containing a difluoromethyl-1,3,4-oxadiazole (DFMO) moiety are potent and single-digit nan

137 Recently, difluoromethyl-1,3,4-oxadiazoles (DFMOs) were reported as potent and selectiv

138 with benzamidoxime gave the final isoxazole-oxadiazole diheterocyclic product in good yield.

139 e preparation of N-substituted 2-amino-1,3,4-oxadiazoles directly from various hydrazides (32 example

140 This oxadiazole displays highly selective, bactericidal killi

141 uoresceins, rhodamines, coumarins, azo-dyes, oxadiazoles, diverse aromatic dyes as well as selected o

142 -activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors leading to the discovery of p

143 The oxadiazole exhibits efficacy in a mouse model of recurre

144 thesis of medicinally relevant a-amino 1,3,4-oxadiazoles from abundant tertiary amides or lactams, ca

145 ired by the Huisgen reaction to obtain 1,3,4-oxadiazoles from acylated tetrazoles, proceeds via a key

146 d for the synthesis of bis-substituted 1,2,4-oxadiazoles from readily available arylnitriles and acti

147 rategy for accessing 2,5-disubstituted 1,3,4-oxadiazoles, from carboxylic acids, N-isocyaniminotriphe

148 The keto-1,2,4-oxadiazole functionality with a thioether is a novel str

149 ad application in medicinal chemistry, 1,2,5-oxadiazoles (furazans) are less common.

150 Fructose-based 3-acetyl-2,3-dihydro-1,3,4-oxadiazole (GLB) is a novel antitumor agent and belongs

151 this reaction are diverse 2,5-dihydro-1,2,4-oxadiazoles (>40 examples, up to 95% yield).

152 ed 2-amino-1,3,4-oxadiazole defining a novel oxadiazole --> furan --> benzene Diels-Alder strategy.

153 5-disubstituted-1,3,4-thiadiazoles and 1,3,4-oxadiazoles has been developed.

154 Recently, substituted oxadiazoles have attracted attention as a promising nove

155 cently, different nitrato-methyl-substituted oxadiazoles have been described as potential melt-cast e

156 While the 1,2,4- and 1,3,4-oxadiazoles have seen widespread application in medicina

157 A series of carbazole/1,3,4-oxadiazole hybrid molecules is described in which the op

158 + 2]/[3 + 2] cycloaddition cascade of 1,3,4-oxadiazoles ideally suited for use in the assemblage of

159 ility and provides the desired 2-amino-1,3,4-oxadiazole in excellent yields.

160 [4+2]/[3+2] cycloaddition cascade of a 1,3,4-oxadiazole in which the pentacyclic skeleton and all the

161 ee sequential microreactors to produce 1,2,4-oxadiazoles in approximately 30 min in quantities (40-80

162 At the same time, trinitrophenyl-1,2,5-oxadiazoles incorporating three adjacent non-coplanar ni

163 inhibitors as well as a thioether keto-1,2,4-oxadiazole inhibitor for GVIA iPLA2, which will serve as

164 rther confirmed by a crystal structure of an oxadiazole inhibitor in complex with hSirt2.

165 ]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazole inhibitors of TNKS1 and 2.

166 2]/[3 + 2] cycloaddition cascade of a 1,3,4-oxadiazole inspired by the natural product structure, in

167 [4+2]/[3+2] cycloaddition cascade of a 1,3,4-oxadiazole inspired by the natural product structure, in

168 + 2]/[3 + 2] cycloaddition cascade of 1,3,4-oxadiazoles inspired by the natural product structures.

169 Synthesis of tetrazole-, triazole-, and oxadiazole-integrated C1' analogues of remdesivir was at

170 -phenylhydrazone of 3-benzoyl-5-phenyl-1,2,4-oxadiazole into the corresponding triazole at 363 K.

171 Z-phenylhydrazone of 5-amino-3-benzoyl-1,2,4-oxadiazole into the relevant 1,2,3-triazole, in solution

172 The formation of 2-amino-1,3,4-oxadiazole involves the Smiles rearrangement of thiazoli

173 s suggested that the nature of chains on the oxadiazole is important for antitumor potency in vitro.

174 followed by cyclization to the corresponding oxadiazole, is the predominant nitrene chemistry, occurr

175 In virtually all cases, the 1,3,4-oxadiazole isomer shows an order of magnitude lower lipo

176 , and aqueous solubility, favoring the 1,3,4-oxadiazole isomers.

177 und library led to the identification of the oxadiazole-isopropylamide 1 (PI-1833) which inhibited ch

178 alosporins bear an ester or alternatively an oxadiazole isostere at C-2 of the cephalosporin ring sys

179 in, we describe the discovery of a series of oxadiazole ketones, which upon optimization, led to the

180 l proteasome inhibitor warhead, 2-keto-1,3,4-oxadiazoles (KOD), to produce reversible, subnanomolar p

181 a systematic comparison of 1,2,4- and 1,3,4-oxadiazole matched pairs in the AstraZeneca compound col

182 the effect of the introduction of the 1,3,4-oxadiazole moiety on molecular reactivity and the differ

183 radiolabeling of the 5-trifluoromethyl-1,2,4-oxadiazole moiety that was reported by us previously and

184 hese compounds contained an alpha-keto-1,3,4-oxadiazole moiety to bind covalently to the Ser-195 hydr

185 highly emissive TADF emitters using a 1,3,4-oxadiazole motif.

186 ies of carbazole-(C=C)(n)-2,5-diphenyl-1,3,4-oxadiazoles (n = 1-4) as conjugated pai-systems in gener

187 Furoxans (1,2,5-oxadiazole-N-oxides) are thiol-bioactivated NO-mimetics

188 nity to construct (1H)-1,2,4-triazole, 1,3,4-oxadiazole, or 1,3,4-thiazoles contingent on the electro

189 y substituted imidazoline, a 1,2,4- or 1,3,4-oxadiazole, or an alkylated tetrazole moiety.

190 2,5-Diphenyl-1,3,4-oxadiazole (OXD) derivatives with terminal ethynyl- (4a,

191 PVK) and 2-tert-butylphenyl-5-biphenyl-1,3,4-oxadiazole (PBD).

192 2,7-diyl)-end capped with 2,5-diphenyl-1,2,4-oxadiazole (PFLO) was used as the immobilization matrix

193 hemical optimization of 1 led to a series of oxadiazoles possessing interpretable SAR and potencies a

194 generated from linked 1,2,4-oxadiazole/1,2,5-oxadiazole precursors exhibit good to excellent thermal

195 5-Dinitrobenzylsulfanyl tetrazoles and 1,3,4-oxadiazoles, previously identified as having high in vit

196 ed family of energetic polynitrophenyl-1,2,5-oxadiazoles provides a fruitful foundation for the creat

197 d intact endothelium and was prevented by 1H-oxadiazole quinoxalin-1-one (P<0.05 and P<0.001, respect

198 Screening of 120 oxadiazoles revealed compound 110 (IC(50) = 14 +/- 1 muM

199 f guanidine-based SphK inhibitors bearing an oxadiazole ring in the scaffold.

200 cture and of the 5-substituents in the 1,2,4-oxadiazole ring on the reactivity of the examined rearra

201 of heterocyclic oligomers based on the 1,3,4-oxadiazole ring were synthesized.

202 pyrazole moieties are linked through a 1,3,4-oxadiazole ring.

203 ssumption that by the combination of varying oxadiazole rings, it would be possible to profit from th

204 ombination of explosophoric groups and 1,2,5-oxadiazole rings, the prepared high-energy substances ha

205 d belongs to glycosylated spiro-heterocyclic oxadiazole scaffold derivative.

206 ials incorporating the polynitrophenyl-1,2,5-oxadiazole scaffold enriched with azo/azoxy moieties hav

207 eries of Sirt2 inhibitors based on the 1,2,4-oxadiazole scaffold.

208 ein, we report the identification of a novel oxadiazole series of Pks13 inhibitors, derived from a hi

209 en-2-yl]-3-[3-(trifluoromethyl)phenyl]1,2,4- oxadiazole (SEW2871) were inactive.

210 hienyl]-3-[3-(trifluoromethyl)phenyl]-1,2, 4-oxadiazole (SEW2871).

211 The oxadiazoles show bactericidal activity against vancomyci

212 on of carbon-11 into acyl amidines and 1,2,4-oxadiazoles, structural motifs of pharmacological intere

213 n the natural products served as a key 1,3,4-oxadiazole substituent, activating it for participation

214 Oxadiazole substituted oxindoles were subsequently conve

215 Herein a library of 1,3,4-oxadiazoles substituted at the 2 position with an aryl s

216 ted 26l, 2-nicotinoyl-substituted 26m, and 2-oxadiazole-substituted 35a compared favorably with the a

217 A one-pot 1,3,4-oxadiazole synthesis-arylation strategy for accessing 2,

218 DAMs with N-methoxy imidoyl halide and 1,2,4-oxadiazole systems were attempted.

219 rary of compounds led to the discovery of an oxadiazole that binds to the mature (activated) form of

220 2]/[3 + 2] cycloaddition cascade of a 1,3,4-oxadiazole that provided the functionalized pentacyclic

221 A variety of highly substituted oxadiazoles, thiadiazoles, triazoles, and tetrazoles hav

222 and 3,4-dimethyl-7-oxycoumarin derivatives (oxadiazoles, thiadiazoles, triazoles, and thiazolidinone

223 Here, we report our discovery of a 1,3,4-oxadiazole thioether scaffold called Cyprocide that sele

224 tivity boost upon substitution of oxazole by oxadiazole to reduced steric interactions in the active

225 or ready access of a broad spectrum of 1,3,4-oxadiazoles, under mild conditions, are described.

226 iplet excited state is located mostly on the oxadiazole unit.

227 the nitration of 5,5'-diamino-3,3'-azo-1,2,4-oxadiazole using 100 % nitric acid.

228 2-amino-1,3,4-thiadiazoles and 2-amino-1,3,4-oxadiazoles using CDI as a C=O donor, without the requir

229 extension to the synthesis of aminated 1,3,4-oxadiazoles using N-benzoyloxy amine coupling partners w

230 ol for one-pot synthesis of 2,5-diaryl 1,3,4-oxadiazoles via a radical-promoted cross-dehydrogenative

231 r the synthesis of 1,2,4-triazoles and 1,2,4-oxadiazoles via acyl amidine intermediates are reported.

232 this approach the bromodifluoromethyl-1,2,4-oxadiazole was converted into [18F]TFMO via no-carrier-a

233 DDO-7263.3-Phenyl-5-(4-tolyl)-1,2,4-(5-(11)C)oxadiazole was synthesized and isolated with a clinicall

234 ent on the tether linking the dienophile and oxadiazole was used to control the facial selectivity of

235 eduction/condensation cascade of amino-1,2,5-oxadiazoles was accomplished.

236 A series of novel 1,3,4-oxadiazoles was synthesized and evaluated for their cyto

237 5-Substituted-2-ethoxy-1,3,4-oxadiazoles were conveniently prepared through a one-pot

238 harmacokinetic liabilities of the piperazine oxadiazoles were overcome by blocking predicted sites of

239 The (11)C-labeled 1,2,4-oxadiazoles were synthesized without the isolation of th

240 r the synthesis of 3-amino-5-nitramino-1,2,4-oxadiazole, which has nitramino and amino groups in the

241 This is novel and general synthesis of 1,2,4-oxadiazoles, which are very important compounds for medi

242 ew class of non-beta-lactam antibiotics, the oxadiazoles, which inhibit penicillin-binding protein 2a

243 zolopyrazines, 1,2,3-thiadiazoles, and 1,3,4-oxadiazoles, while other substrate classes (e.g., pyrazo

244 de can be replaced with a bioisosteric 1,3,4-oxadiazole with improved potency.

245 followed by a subsequent ring opening of the oxadiazole yields deprotonated difluoroacetylhydrazide 1