SYNTHESIS AND LEISHMANICIDAL ACTIVITY OF 1-[5-(5-NITROFURAN-2-YL)-1, 3, 4-THIADIAZOLE-2-YL]-4-BENZOYLEPIPERAZINES

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FOROUMADI ALIREZA; ADIBI HADI; KABUDANIAN ARDESTANI SUSSAN; SHIROOIE SAMIRA; BOZORGOMID AREZOO; JAFARI ALI

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Journal: Iranian Journal of Pharmaceutical Research Year:2017 | Volume:16 | Issue:3 Page(s): 904-909

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Title

SYNTHESIS AND LEISHMANICIDAL ACTIVITY OF 1-[5-(5-NITROFURAN-2-YL)-1, 3, 4-THIADIAZOLE-2-YL]-4-BENZOYLEPIPERAZINES

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Keywords

THIADIAZOLE;NITROFURAN;ANTILEISHMANIAL ACTIVITY;LEISHMANIA MAJOR;PROMASTIGOTE

Abstract

A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a– 6e have beensynthesized and screened for in-vitro anti-leishmanial activity against the promastigote formof L. major. The structure of Schiff bases were confirmed by 1H NMR, IR. Screening resultsindicate that all of the designed and synthesized final compounds (6a-6e) significantly reducedthe viability of promastigotes of L. major in comparison toglucantime (IC50 3× 103 μ g/mL). Meta and Para substitutions in benzene ring containing compounds were more potent thanother derivative and the most potent compounds were 6d, 6e with IC50 value 94 μ m and 77. 6μ m, 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 cutaneousleishmaniasis.

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APA: Copy

FOROUMADI, ALIREZA, ADIBI, HADI, KABUDANIAN ARDESTANI, SUSSAN, SHIROOIE, SAMIRA, BOZORGOMID, AREZOO, & JAFARI, ALI. (2017). SYNTHESIS AND LEISHMANICIDAL ACTIVITY OF 1-[5-(5-NITROFURAN-2-YL)-1, 3, 4-THIADIAZOLE-2-YL]-4-BENZOYLEPIPERAZINES. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 16(3), 904-909. SID. https://sid.ir/paper/288971/en

Vancouver: Copy

FOROUMADI ALIREZA, ADIBI HADI, KABUDANIAN ARDESTANI SUSSAN, SHIROOIE SAMIRA, BOZORGOMID AREZOO, JAFARI ALI. SYNTHESIS AND LEISHMANICIDAL ACTIVITY OF 1-[5-(5-NITROFURAN-2-YL)-1, 3, 4-THIADIAZOLE-2-YL]-4-BENZOYLEPIPERAZINES. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2017;16(3):904-909. Available from: https://sid.ir/paper/288971/en

IEEE: Copy

ALIREZA FOROUMADI, HADI ADIBI, SUSSAN KABUDANIAN ARDESTANI, SAMIRA SHIROOIE, AREZOO BOZORGOMID, and ALI JAFARI, “SYNTHESIS AND LEISHMANICIDAL ACTIVITY OF 1-[5-(5-NITROFURAN-2-YL)-1, 3, 4-THIADIAZOLE-2-YL]-4-BENZOYLEPIPERAZINES,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 16, no. 3, pp. 904–909, 2017, [Online]. Available: https://sid.ir/paper/288971/en

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