Synthesis and Leishmanicidal Activity of 1-[5-(5-Nitrofuran-2-Yl)-1, 3, 4-Thiadiazole-2-Yl]-4-Benzoylepiperazines



Foroumadi A¹ ; Adibi H² ; Ardestani SK³ ; Shirooie S⁴ ; Bozorgomid A⁵ ; Jafari A² Show Affiliations
Source: Iranian Journal of Pharmaceutical Research Published:2017

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 by1H 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. © 2017 by School of Pharmacy Shaheed Beheshti University of Medical Sciences and Health Services.