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.
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.
Sanna
Paolo
P
Dipartimento Farmaco-Chimico-Tossicologico, Università degli Studi, Sassari, Italy. psanna@ssmain.uniss.it
Carta
Antonio
A
Gherardini
Laura
L
Esmail
Mohammad
M
Nikookar
Rahbar
R
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
D000890:Anti-Infective Agents; D000995:Antitubercular Agents; D009570:Nitriles