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

被引:0
作者
Foroumadi, Alireza [1 ,2 ]
Adibi, Hadi [3 ]
Ardestani, Sussan Kabudanian [4 ]
Shirooie, Samira [5 ]
Bozorgomid, Arezoo [6 ]
Jafari, Ali [3 ]
机构
[1] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran
[2] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran, Iran
[3] Kermanshah Univ Med Sci, Pharmaceut Sci Res Ctr, Fac Pharm, Kermanshah, Iran
[4] Univ Tehran, Inst Biochem & Biophys, Dept Biochem, Tehran, Iran
[5] Kermanshah Univ Med Sci, Students Res Comm, Kermanshah, Iran
[6] Univ Tehran Med Sci, Sch Publ Hlth, Dept Med Parasitol & Mycol, Tehran, Iran
来源
IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH | 2017年 / 16卷 / 03期
关键词
1; 3; 4-Thiadiazole; Nitrofuran; Antileishmanial activity; Leishmania Major; Promastigote; IN-VITRO; DERIVATIVES; MOIETY; 1,3,4-THIADIAZOLE; 1,2,4-TRIAZOLE; IRAN;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 H-1 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 3x 10(3) mu g/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 mu m and 77.6 mu m, respectively. The experimental data proposes that (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole2-yl derivatives may be further investigated as a candidate drug for treatment of cutaneous leishmaniasis.
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收藏
页码:904 / 909
页数:6
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