Novel 1,2,4-triazole-3-mercaptoacetic acid derivatives as potential anti-mycobacterial and antimicrobial agents

Novel Schiff bases of 4-methyl 1,2,4-triazole-3-mercaptoacetic acid hydrazide were synthesized. Their chemical identities were elucidated by elemental analyses, IR, [1] H-NMR, [13] C-NMR and mass spectral data. The percentage of the geometrical isomers was also elucidated using the [1] H-NMR. The synthesized compounds were selected for screening at the Tuberculosis Antimicrobial Acquisition and Coordination Facility [TAACF] against Mycobacterium tuberculosis H [37] R [v] strain in which they showed moderate activity at a concentration of 6.25 micro g/ml. Moreover, antimicrobial screenings against E. coli [ATCC 25922], S. aureus [ATCC 19433] and C. albicans identified compound 4g as the most effective showing similar antibacterial activity as ampicillin against S. aureus

Allophenylnorstatine-containing HIV-1 protease inhibitors: design, synthesis and structure-activity relationships for selected P

The design and development of potent HIV protease inhibitors remain an attractive target for antiviral therapy. A novel class of HIV protease inhibitors containing allophenylnorstatine [Apns; [2S,3S]-3-amino-2-hydroxy-4-phenylbutyric acid] as a transition state mimic have been reported. In this work we fixed P 2' [as tert-butylamino or 2-methylbenzylamino] and changed P 2 moiety to provide two series of dipeptide analogs. Preliminary evaluation of the activity of the synthesized derivatives were determined as percentage of enzyme inhibition at 5 microM level. The results showed that the introduction of 2-methylbenzylamino moiety as P 2' ligand 6a-e considerably improved HIV inhibitory activity in comparison with the tert-butyl amino analogs 5a-e. It was found that compounds in both series retained activity still less than the lead compounds KNI-577 and KNI-727