Literature DB >> 21917452

Synthesis and preliminary biological evaluation of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives as potential antimycobacterial agents: an operational Topliss Tree approach.

Manoj D Kakwani1, Nutan H Palsule Desai, Arundhati C Lele, Muktikant Ray, M G R Rajan, Mariam S Degani.   

Abstract

A series of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives were designed on basis of structural similarity to the known FAS II inhibitors. Topliss operational method was used to optimize the potency of molecules. The minimum inhibitory concentration (MIC) of all synthesized compounds was determined against Mycobacterium tuberculosis H(37)R(v) using resazurin microtitre assay (REMA) plate method. The synthesized compounds exhibit antimycobacterial activity in the range of 5-95μM with a good safety profile.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21917452     DOI: 10.1016/j.bmcl.2011.08.076

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Synthesis of 3-(5-amino-1H-1,2,4-triazol-3-yl)propanamides and their tautomerism.

Authors:  Felicia Phei Lin Lim; Lin Yuing Tan; Edward R T Tiekink; Anton V Dolzhenko
Journal:  RSC Adv       Date:  2018-06-19       Impact factor: 3.361

2.  Development of a radioiodinated triazolopyrimidine probe for nuclear medical imaging of fatty acid binding protein 4.

Authors:  Kantaro Nishigori; Takashi Temma; Satoru Onoe; Sotaro Sampei; Ikuo Kimura; Masahiro Ono; Hideo Saji
Journal:  PLoS One       Date:  2014-04-14       Impact factor: 3.240

3.  Quantitative Structure-Cytotoxic Activity Relationship 1-(Benzoyloxy)urea and Its Derivative.

Authors:  Suko Hardjono; Siswandono Siswodihardjo; Purwanto Pramono; Win Darmanto
Journal:  Curr Drug Discov Technol       Date:  2016
  3 in total

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