Synthesis and in vitro leishmanicidal activity of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles

Alireza Foroumadi; Shirin Pournourmohammadi; Fatemeh Soltani; Mitra Asgharian-Rezaee; Shahriar Dabiri; Arsalan Kharazmi; Abbas Shafiee

doi:10.1016/j.bmcl.2005.02.073

Synthesis and in vitro leishmanicidal activity of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles

Bioorg Med Chem Lett. 2005 Apr 15;15(8):1983-5. doi: 10.1016/j.bmcl.2005.02.073.

Authors

Alireza Foroumadi¹, Shirin Pournourmohammadi, Fatemeh Soltani, Mitra Asgharian-Rezaee, Shahriar Dabiri, Arsalan Kharazmi, Abbas Shafiee

Affiliation

¹ Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman 76351, Iran.

PMID: 15808452
DOI: 10.1016/j.bmcl.2005.02.073

Abstract

A series of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles (5a-d and 6a-j) were synthesized and evaluated against Leishmania major promastigotes using (3)H-thymidine incorporation. Most of the compounds showed activity better than the reference drug sodium stibogluconate (Pentostam). The most active compound was 6c (IC(50)=0.1 microM).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antiprotozoal Agents / chemical synthesis*
Antiprotozoal Agents / pharmacology*
Leishmania major / drug effects*
Leishmania major / growth & development*
Thiadiazoles / chemical synthesis*
Thiadiazoles / pharmacology*

Substances

Antiprotozoal Agents
Thiadiazoles