- Synthesis and structural studies of isomeric Δ2- pyrazolines
-
1-(2′-Thienyl)-3-(4″-dimethylamino phenyl)-2-propen-1-one(la-e) react with hydrazine hydrochloride in DMF medium to give isomeric 1-H pyrazolines (lla-e), react with phenyl hydrazine hydrochloride in DMF medium to give isomeric 1 -phenyl pyrazolines (Illa
- Ingle,Doshi,Raut
-
experimental part
p. 1517 - 1520
(2011/10/13)
-
- Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis
-
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.
- Stirrett, Karen L.,Ferreras, Julian A.,Jayaprakash, Venkatesan,Sinha, Barij N.,Ren, Tao,Quadri, Luis E.N.
-
p. 2662 - 2668
(2008/12/21)
-
- Pyrazoline-based mycobactin analogues as MAO-inhibitors
-
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.
- Jayaprakash, Venkatesan,Sinha, Barij N.,Ucar, Gulberk,Ercan, Ayse
-
scheme or table
p. 6362 - 6368
(2009/09/30)
-
- Thienyl acrylamides and thienyl pyrazolines as potential schistosomicidal agents
-
α Thienyl N substituted acrylamides that possess analogous structures to known schistosomicidal agents were synthesized. Two chalcones were prepared by condensing α thiophenealdehyde and acetophenone or its o hydroxy derivative. Cyclization of the chalcon
- El Kerdawy,Samour,El Agamey
-
-