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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Synthesis and in vitro Leishmanicidal Activity of Disulfide Derivatives

Author(s): Khalid Mohammed Khan, Muhammad Taha, Farzana Naz, Momin Khan, Fazal Rahim, Samreen, Shahnaz Perveen and M. Iqbal Choudhary

Volume 7, Issue 6, 2011

Page: [704 - 710] Pages: 7

DOI: 10.2174/157340611797928460

Price: $65

Abstract

Disulfides 1-30 have been synthesized and their in vitro leishmanicidal activity has been evaluated. Compounds 18 (IC50 = 2.70 ± 0.044 μM), 19 (IC50 = 2.85 ± 0.02 μM), 20 (IC50 = 2.92 ± 0.01 μM), 26 (IC50 = 3.69 ± 0.01 μM), 21 (IC50 = 4.45 ± 0.029 μM), and 29 (IC50 = 4.46 ± 0.025 μM) showed a remarkable leishmanicidal activity if compared with standard pentamidine (IC50 = 5.09 ± 0.04 μM). This study has discovered a series of possible molecules as antileishmanial agents. A structure-activity relationship study has also been carried out. The structures of all the synthesized compounds were identified by using spectroscopic techniques, including 1H-NMR and EI MS.

Keywords: Synthesis, disulfides, leishmanicidal activity, Leishmania, spectroscopic techniques, pentamidine, protozoan, Nicolle, genus Leishmania, disulfide linkage


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