Oxysterols: Synthesis and anti-leishmanial activities

Steroids. 2016 Mar:107:65-73. doi: 10.1016/j.steroids.2015.12.020. Epub 2015 Dec 29.

Abstract

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.

Keywords: A-nor-cholest-6-hydroxy-5,7-olide; Anti-leishmanial activities; Cytotoxicity; Oxygenated sterols.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents* / chemical synthesis
  • Antiprotozoal Agents* / chemistry
  • Antiprotozoal Agents* / pharmacology
  • Leishmania donovani / metabolism*
  • Leishmania major / metabolism*
  • Leishmaniasis, Cutaneous* / drug therapy
  • Leishmaniasis, Cutaneous* / metabolism
  • Leishmaniasis, Cutaneous* / pathology
  • Leishmaniasis, Visceral* / drug therapy
  • Leishmaniasis, Visceral* / metabolism
  • Leishmaniasis, Visceral* / pathology
  • Mice
  • Mice, Inbred BALB C
  • Sterols* / chemical synthesis
  • Sterols* / chemistry
  • Sterols* / pharmacology

Substances

  • Antiprotozoal Agents
  • Sterols