N1 -[1-Aryl-2-(1H-imidazol-1-yl and 1H-1,2,4-triazol-1-yl)-ethylidene]-pyridine-2-carbo xamidrazone derivatives were synthesized and tested for their in vitro antifungal and antimycobacterial activity. Some compounds showed a very good activity against the tested clinical isolates of Candida albicans 685 and Candida glabrata 523. The same compounds exhibited an interesting, even if moderate, activity against the tested strain of Mycobacterium tuberculosis H 37 Rv. Preliminary molecular modeling investigations yielded free energy of binding values in harmony with the corresponding experimental findings. They further revealed that an optimized balance of opposing electrostatic contributions must be realized to gain tight enzyme-inhibitor binding.
Synthesis and Antimycobacterial Activity of (3,4-Diaryl-3H-thiazol-2-ylidene)-hydrazide Derivatives. -A series of title compounds (I) is obtained via a simple procedure and tested for their in vitro antimycobacterial activity. The results obtained are not suitable for an evaluation of structure-activity relationships, but show that compounds which explicate some degree of activity against almost all of the clinical isolates of M.tubercolosis are those which are p-substituted at one of the phenyl residues. -(MAMOLO*, M. G.; FALAGIANI, V.; ZAMPIERI, D.; VIO, L.; BANFI, E.; SCIALINO, G.; Farmaco 58 (2003) 9, 631-637; Dip. Sci. Farm., Univ. Trieste, I-34127 Trieste, Italy; Eng.) -H. Haber 03-238
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.