Posner G H, Maxwell J P, O'Dowd H, Krasavin M, Xie S, Shapiro T A
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA.
Bioorg Med Chem. 2000 Jun;8(6):1361-70. doi: 10.1016/s0968-0896(00)00079-1.
A series of trioxanes featuring sulfide, sulfone, and sulfonamide substituents in diverse positions has been prepared. Structure-activity relationship (SAR) generalizations highlight two major factors controlling the antimalarial potency of these new chemical entities: (1) the proximity of the sulfur-containing substituent to the crucial peroxide bond and (2) the oxidation state of the sulfur-containing substituent. Generally, sulfones are more antimalarially potent than the corresponding sulfides.
