title: Synthesis and antimycobacterial activity of 3-aryl-, 3-cyclohexyl- and 3-heteroaryl- substituted-2-(1H(2H)-benzotriazol-1(2)-yl)prop-2-enenitriles, prop-2-enamides and propenoic acids. II.
abstract: A series of 32 3-aryl-, 3-cyclohexyl-, and 3-heteroaryl-substituted-2-(1H(2H)-benzotriazol-1(2)-yl)-prop-2-enenitriles, prop-2-enamides and propenoic acids, was synthesized as a part of our research in the antitubercular field, according to an international program with the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF). This work reports the preparation and analytical and spectroscopic characterization (MS, UV, IR, 1H NMR) of all compounds synthesized. Among these only a few compounds (E-4b,c, E-5a, E-7e and E-8d) were found to be endowed with modest growth inhibition of Mycobacterium tuberculosis. However, the obtained results allowed to acquire interesting structure-activity relationships.
authors.affiliation: Dipartimento Farmaco-Chimico-Tossicologico, Università degli Studi, Sassari, Italy. psanna@ssmain.uniss.it
authors.forename: Paolo
authors.initials: P
authors.lastname: Sanna
authors.forename: Antonio
authors.initials: A
authors.lastname: Carta
authors.forename: Laura
authors.initials: L
authors.lastname: Gherardini
authors.forename: Mohammad
authors.initials: M
authors.lastname: Esmail
authors.forename: Rahbar
authors.initials: R
authors.lastname: Nikookar
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009570:Nitriles / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D000995:Antitubercular Agents; D009570:Nitriles