Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 23, Issue 12, Pages 5282-5293Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-014-1082-1
Keywords
Indole hydrazones; Antileishmanial; SAR study
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Funding
- Research Management Institute of UiTM under CIFI Scheme [600-RMI/DANA 5/3/CIFI (141/2013)]
- Higher Education Commission (HEC) Pakistan under the National Research Program for Universities [20-2073]
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Indole-2-hydrazones 3-30 were synthesized and evaluated for their antileishmanial activity. The compounds 24 (IC50 = 1.86 +/- A 0.09 mu M), 12 (IC50 = 2.26 +/- A 0.16 mu M), 23 (IC50 = 3.81 +/- A 0.29 mu M), 8 (IC50 = 4.01 +/- A 0.32 mu M), 17 (IC50 = 4.89 +/- A 0.31 mu M), 20 (IC50 = 4.89 +/- A 0.26 mu M), 3 (IC50 = 5.12 +/- A 0.34 mu M), 15 (IC50 = 5.26 +/- A 0.26 mu M), 6 (IC50 = 6.16 +/- A 0.38 mu M), and 21 (IC50 = 6.18 +/- A 0.045 mu M) showed better activities than standard pentamidine (IC50 = 7.02 +/- A 0. 09 mu M). Compounds 4, 5, 7, 9-11, 13, 16, 18, 19, 22, 25-28, and 30 displayed good activities. The compounds 14 and 29 were found to be inactive. The synthesized compounds were characterized by different spectroscopic techniques.
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