Oxysterols: Synthesis and anti-leishmanial activities

• Different oxysterols have been synthesized.
• Anti-leishmanial activities have been reported.
• Some of the derivatives induce nitric oxide in macrophages significantly.
• 3,7-Dihydroxy derivatives showed the best anti-amastigote effect.

Oxygenated sterols (2–16) were synthesized by skeletal rearrangement of steroidal allylic alcohols. All the derivatives were screened for their anti-leishmanial activities. Compounds 3, 11 and 12 showed potent activities. Compound 12 was found least toxic and induced highest nitric oxide (NO) at 48 h. Least toxicity of compound 12 on splenocytes validated its best anti-amastigote effect and induction of NO.

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