Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment

作者：Andrews Katherine T^*; Fisher Gillian M; Sumanadasa Subathdrage D M; Skinner Adams Tina; Moeker Janina; Lopez Marie; Poulsen Sally Ann

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(22): 6114-6117.

DOI：10.1016/j.bmcl.2013.09.015

• Sulfonamide
• Primary sulfonamide
• Antimalarial
• Plasmodium falciparum
• SAR
• Carbonic anhydrase

Despite the urgent need for effective antimalarial drugs with novel modes of action no new chemical class of antimalarial drug has been approved for use since 1996. To address this, we have used a rational approach to investigate compounds comprising the primary benzene sulfonamide fragment as a potential new antimalarial chemotype. We report the in vitro activity against Plasmodium falciparum drug sensitive (3D7) and resistant (Dd2) parasites for a panel of fourteen primary benzene sulfonamide compounds. Our findings provide a platform to support the further evaluation of primary benzene sulfonamides as a new antimalarial chemotype, including the identification of the target of these compounds in the parasite.

• 出版日期2013-11-15
• 单位河北医科大学