Synthesis and in vitro leishmanicidal activity of disulfide derivatives.
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.
H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. khalid.khan@iccs.edu
Khalid Mohammed
KM
Khan
Muhammad
M
Taha
Farzana
F
Naz
Momin
M
Khan
Fazal
F
Rahim
Samreen
Shahnaz
S
Perveen
M Iqbal
MI
Choudhary
D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004220:Disulfides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007891:Leishmania / Q000187:drug effects*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D004220:Disulfides