ChemInform Abstract: SYNTHESIS OF SUBSTITUTED 2‐(5′‐OXO/THIOXO‐1′,3′,4′‐OXADIAZOL‐2′‐YL)INDOLES AND 2‐(5′‐OXO/THIOXO‐1,3,4′‐OXADIAZOL‐2′‐YLAMINO)INDOLES

Hiremath, S. P.; Hiremath, D. M.; Purohit, M. G.

doi:10.1002/chin.198346181

Cited by 2 publications

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“…The K i value of 13 falls into the same range as those of 5 and 6 . Compared to 5 and 6 , the carboxylic acid hydrazides are easily accessible via substitution of the free carboxylic acids or esters …”

Section: Resultsmentioning

confidence: 99%

Virtual Screening for Submicromolar Leads of tRNA-guanine Transglycosylase Based on a New Unexpected Binding Mode Detected by Crystal Structure Analysis

et al. 2003

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Eubacterial tRNA-guanine transglycosylase (TGT) is involved in the hypermodification of cognate tRNAs, leading to the exchange of G34 by preQ1 at the wobble position in the anticodon loop. Mutation of the tgt gene in Shigella flexneri results in a significant loss of pathogenicity of the bacterium due to inefficient translation of a virulence protein mRNA. Herein, we describe the discovery of a ligand with an unexpected binding mode. On the basis of this binding mode, three slightly deviating pharmacophore hypotheses have been derived. Virtual screening based on this composite pharmacophore model retrieved a set of potential TGT inhibitors belonging to several compound classes. All nine tested inhibitors being representatives of these classes showed activity in the micromolar range, two of them even in the submicromolar range.

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Section: Resultsmentioning

confidence: 99%

Virtual Screening for Submicromolar Leads of tRNA-guanine Transglycosylase Based on a New Unexpected Binding Mode Detected by Crystal Structure Analysis

et al. 2003

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“…The site and/or regioselectivity during the alkylation of indolyloxadiazole thione 1 27 was dependent on the reaction conditions 28 . Thus, the alkylated derivatives 2 and 3 were prepared.…”

Section: Chemistrymentioning

confidence: 99%

Immunomodulatory properties of S- and N-alkylated 5-(1H-indol-2-yl)-1,3,4-oxadiazole-2(3H)-thione

Ashry

Tamany

Fattah

et al. 2011

Journal of Enzyme Inhibition and Medicinal Chemistry

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ChemInform Abstract: SYNTHESIS OF SUBSTITUTED 2‐(5′‐OXO/THIOXO‐1′,3′,4′‐OXADIAZOL‐2′‐YL)INDOLES AND 2‐(5′‐OXO/THIOXO‐1,3,4′‐OXADIAZOL‐2′‐YLAMINO)INDOLES

Cited by 2 publications

References 0 publications

Virtual Screening for Submicromolar Leads of tRNA-guanine Transglycosylase Based on a New Unexpected Binding Mode Detected by Crystal Structure Analysis

Virtual Screening for Submicromolar Leads of tRNA-guanine Transglycosylase Based on a New Unexpected Binding Mode Detected by Crystal Structure Analysis

Immunomodulatory properties of S- and N-alkylated 5-(1H-indol-2-yl)-1,3,4-oxadiazole-2(3H)-thione

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