title: Orally active antimalarials: synthesis and bioevaluation of a new series of steroid-based 1,2,4-trioxanes against multi-drug resistant malaria in mice.
abstract: A new series of steroid-based 1,2,4-trioxanes 7a-f, 8a-f and 9b-e have been synthesized and evaluated for their antimalarial activity against multi-drug resistant Plasmodium yoelii in Swiss mice by oral route. The biological activity shows a strong dependence on the size and the nature of the steroidal side chain. Pregnane-based trioxanes 8a-f show better activity profile than trioxanes 7a-f and 9b-e, derived from cholesterol and tigogenine, respectively.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. chandancdri@yahoo.com
authors.forename: Chandan
authors.initials: C
authors.lastname: Singh
authors.forename: Upasana
authors.initials: U
authors.lastname: Sharma
authors.forename: Gunjan
authors.initials: G
authors.lastname: Saxena
authors.forename: Sunil K
authors.initials: SK
authors.lastname: Puri
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D018432:Drug Resistance, Multiple; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D010967:Plasmodium yoelii / Q000187:drug effects; D013256:Steroids / Q000737:chemistry*
chemical_list: C503429:1,2,4-trioxane; D000962:Antimalarials; D006571:Heterocyclic Compounds; D013256:Steroids