Foroumadi Alireza, Adibi Hadi, Kabudanian Ardestani Sussan, Shirooie Samira, Bozorgomid Arezoo, Jafari Ali
Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.
Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.
Iran J Pharm Res. 2017 Summer;16(3):904-909.
A series of 5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a-6e have been synthesized and screened for anti-leishmanial activity against the promastigote form of . The structure of Schiff bases were confirmed by H NMR, IR. Screening results indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced the viability of promastigotes of in comparison toglucantime (IC 3× 10 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 IC 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.
已经合成了一系列5-硝基呋喃-2-基)-1,3,4-噻二唑-2-基衍生物6a - 6e，并针对杜氏利什曼原虫前鞭毛体形式筛选了抗利什曼活性。席夫碱的结构通过核磁共振氢谱（H NMR）、红外光谱（IR）得以确认。筛选结果表明，与葡甲胺（IC为3×10μg/mL）相比，所有设计并合成的最终化合物（6a - 6e）均显著降低了杜氏利什曼原虫前鞭毛体的活力。含苯环化合物中的间位和对位取代比其他衍生物更具活性，最具活性的化合物是6d、6e，其IC值分别为94µm和77.6µm。实验数据表明，5-硝基呋喃-2-基)-1,3,4-噻二唑-2-基衍生物可作为治疗皮肤利什曼病的候选药物作进一步研究。
