75201-03-5Relevant academic research and scientific papers
Pyrazoline-based mycobactin analogues as MAO-inhibitors
Jayaprakash, Venkatesan,Sinha, Barij N.,Ucar, Gulberk,Ercan, Ayse
scheme or table, p. 6362 - 6368 (2009/09/30)
3,5-Diaryl carbothioamide pyrazolines designed as mycobactin analogs (mycobacterial siderophore) were reported to be potent antitubercular agents under iron limiting condition in our earlier study. Clinical complications of newly introduced antibiotic Linezolid, due its MAO inhibitory activity, prompted us to evaluate our compounds for their MAO-inhibitory activity against rat liver MAO-A and MAO-B as pyrazolines were reported to be antidepressants and MAO inhibitors. The present study carried out with this pilot library of 32 compounds will provide us with necessary information for designing antitubercular molecules with reduced MAO-inhibitory activity and also help us in identifying a selective MAO-B inhibitor which has potential clinical utility in neurodegenerative disorders. Thirty-two compounds analyzed has shown spectrum of activity from selective to nonselective against two isoforms of rat liver MAO-A and MAO-B and also as competitive, reversible to non-competitive, irreversible. It is also interesting to note that anti-tubercular compound 11, 14 and 16 were also found to be selective inhibitors of rat liver MAO-B. Docking studies with human MAO shows that compound 11 interacts with the catalytic site of both the isoforms, suggesting compound 11 as nonselective inhibitor of human MAO isoforms.
Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis
Stirrett, Karen L.,Ferreras, Julian A.,Jayaprakash, Venkatesan,Sinha, Barij N.,Ren, Tao,Quadri, Luis E.N.
, p. 2662 - 2668 (2008/12/21)
Drugs inhibiting the iron scarcity-induced, siderophore-mediated iron-scavenging systems of Mycobacterium tuberculosis (Mtb) and Yersinia pestis (Yp) may provide new therapeutic lines of defense. Compounds with structural similarities to siderophores were synthesized and evaluated as antimicrobials against Mtb and Yp under iron-limiting conditions, which mimic the iron scarcity these pathogens encounter and must adapt to in the host, and under standard iron-rich conditions for comparison. New antimicrobials were identified, some of which warrant exploration as initial leads against potentially novel targets and small-molecule tools to assist in the elucidation of targets specific to iron-scarcity adapted Mtb and Yp.
Synthesis and Antimicrobial Activity of Hydroxyarylpyrazoles
Sharma, T. C.,Bokadia, M. M.,Reddy, N. J.
, p. 228 - 229 (2007/10/02)
Hydroxyarylpyrazolines (III) and Pyrazoles (IV) have been synthesized.Compounds IVa and IVd exhibit marked antifungal activity against A. niger, C. albicans, C. neoformans, T. mentagraphytes and M. canis whereas compound IVc shows activity against the last three fungi.None of the compounds shows any noteworthy antibacterial activity against Staphy. aureus, Staphi. typhi and Esch. coli even at 100 μg/ml.
