Literature DB >> 17251028

Discovery of novel phenoxyacetic acid derivatives as antimycobacterial agents.

Mohamed Ashraf Ali1, Mohammad Shaharyar.   

Abstract

A series of 2-{4-[1-amino (thioxo) methyl-5-(substituted phenyl)-4,5-dihydro-1H-3-pyrazolyl]-2-methoxyphenoxy}acetic acid and 2-{4-[1-carbamoyl-5-(substituted phenyl)-4,5-dihydro-1H-3-pyrazolyl]-2-methoxyphenoxy}acetic acid were synthesized and the in vitro activity of the synthesized compounds against Mycobacterium tuberculosis H37Rv (MTB) and INH-resistant M. tuberculosis (INHR-MTB) was studied. Among the synthesized compounds, compound (3f) 2{-[4-(1-carbamoyl-5-(chlorophenyl)-4,5-dihydro-1H-3-pyrazolyl]-2-methoxyphenoxy}acetic acid was found to be the most active against M. tuberculosis H37Rv (MTB) and INH-resistant M. tuberculosis (INHR-MTB) with minimum inhibitory concentration of 0.06 microg/ml.

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Year:  2007        PMID： 17251028     DOI： 10.1016/j.bmc.2007.01.006

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  5 in total

1.  Stereoselective synthesis of cis- or trans-3,5-disubstituted pyrazolidines via Pd-catalyzed carboamination reactions: use of allylic strain to control product stereochemistry through N-substituent manipulation.

Authors:  Natalie C Giampietro; John P Wolfe
Journal:  J Am Chem Soc       Date:  2008-09-06       Impact factor: 15.419

2.  Synthesis and Antimicrobial Activity of 2-[2-(2,6-dichloro phenyl)amino]benzyl-3-(5-substituted phenyl-4,5-dihydro-1H-pyrazol-3-yl-amino)-6,8-dibromoquinazolin-4(3H)ones.

Authors:  Nb Patel; Jc Patel; Gg Barat
Journal:  J Young Pharm       Date:  2010-04

3.  Formal [4 + 1] cycloaddition of in situ generated 1,2-diaza-1,3-dienes with diazo esters: facile approaches to dihydropyrazoles containing a quaternary center.

Authors:  Bo Chen; Wen-Dao Chu; Quan-Zhong Liu
Journal:  RSC Adv       Date:  2019-01-11       Impact factor: 4.036

4.  1-(4-Bromo-phen-yl)-2-(2-chloro-phen-oxy)ethanone.

Authors:  Seema S Shenvi; Arun M Isloor; Thomas Gerber; Eric Hosten; Richard Betz
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-11-30

5.  Organocatalytic cascade aza-Michael/hemiacetal reaction between disubstituted hydrazines and α,β-unsaturated aldehydes: Highly diastereo- and enantioselective synthesis of pyrazolidine derivatives.

Authors:  Zhi-Cong Geng; Jian Chen; Ning Li; Xiao-Fei Huang; Yong Zhang; Ya-Wen Zhang; Xing-Wang Wang
Journal:  Beilstein J Org Chem       Date:  2012-10-09       Impact factor: 2.883
  5 in total

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