Title of article :
Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-yl)-1, 3, 4-Thiadiazole-2-yl]-4-BenzoylePiperazines
Author/Authors :
Foroumadi, Alireza Department of Medicinal Chemistry - Faculty of Pharmacy and Pharmaceutical Sciences Research Center - Tehran University of Medical Sciences, Tehran, Iran , Adibi, Hadi Pharmaceutical Sciences Research Center - Faculty of Pharmacy - Kermanshah University of Medical Sciences, Kermanshah, Iran , Kabudanian Ardestani, Sussan Department of Biochemistry - Institute of Biochemistry and Biophysics - University of Tehran, Tehran, Iran , Shirooie, Samira Student’s Research Committee - Kermanshah University of Medical Sciences, Kermanshah, Iran , Bozorgomid, Arezoo Department of Medical Parasitology and Mycology - School of Public Health - Tehran University of Medical Sciences, Tehran, Iran , Jafari, Ali Pharmaceutical Sciences Research Center - Faculty of Pharmacy - Kermanshah University of Medical Sciences, Kermanshah, Iran
Abstract :
A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a–6e have been
synthesized and screened for in-vitro anti-leishmanial activity against the promastigote form
of L. major. The structure of Schiff bases were confirmed by 1H NMR, IR. Screening results
indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced
the viability of promastigotes of L. major in comparison toglucantime (IC50 3× 103 μg/mL).
Meta and Para substitutions in benzene ring containing compounds were more potent than
other derivative and the most potent compounds were 6d, 6e with IC50 value 94 μm and 77.6
μm, respectively. The experimental data proposes that (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-
2-yl derivatives may be further investigated as a candidate drug for treatment of cutaneous
leishmaniasis.
Keywords :
Promastigote , Leishmania Major , Antileishmanial activity , Nitrofuran , 1, 3, 4-Thiadiazole
