V. M. Gohil et al. / Bioorg. Med. Chem. Lett. 22 (2012) 3905–3907
3907
Figure 3. Anti-leishmanial activities of the synthesized compounds: Results are expressed as the concentration inhibiting parasite growth by 50% (IC50) after a 3-day
incubation period (n = 3). Standard (miltefosine) showed IC50 of 12.07 0.82
lM, six compounds (shown in the shaded region) showed an IC50 less than the standard.
tion in the E ring (6 and 16) showed activity comparable to that of
standard (12.35 1.58 and 14.26 0.33 M) whereas those con-
taining bulkier group like tert-butyl (15) were inactive. The cyto-
toxicity of the compounds was evaluated on peritoneal murine
macrophages according to procedure adapted from Peyron et
al.18 with an incubation period of 72 h. The CC50 (cytotoxic concen-
trations 50%) of all compounds were more than 50 lM, indicating
that the selectivity index (CC50/IC50) of the most active compound
(4) was greater than 20.
In conclusion, six compounds (4, 5, 10, 11, 19, and 22) showed
anti-leishmanial activity that was better than the standard
miltefosine and three compounds (6, 14 and 16) showed activity
that was comparable to standard, suggesting that this group of
compounds can be further explored for getting potent anti-leish-
manial compounds.
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VMG is thankful to Council of Scientific and Industiral Research
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Supplementary data
Supplementary data associated with this article can be found,
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