title: 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.
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.
authors.affiliation: Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400 019, India.
authors.forename: Manoj D
authors.initials: MD
authors.lastname: Kakwani
authors.forename: Nutan H
authors.initials: NH
authors.lastname: Palsule Desai
authors.forename: Arundhati C
authors.initials: AC
authors.lastname: Lele
authors.forename: Muktikant
authors.initials: M
authors.lastname: Ray
authors.forename: M G R
authors.initials: MG
authors.lastname: Rajan
authors.forename: Mariam S
authors.initials: MS
authors.lastname: Degani
mesh_terms: D000577:Amides / Q000737:chemistry*; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002934:Cinnamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*
chemical_list: D000577:Amides; D000995:Antitubercular Agents; D002934:Cinnamates; C029010:cinnamic acid