New azasterols against Trypanosoma brucei: Role of 24-sterol methyltransferase in inhibitor action

by Gros L, Castillo-Acosta VM, Jimenez Jimenez C, Sealey-Cardona M, Vargas S, Manuel Estevez A, Yardley V, Rattray L, Croft SL, Ruiz-Perez LM, Urbina JA, Gilbert IH, Gonzalez-Pacanowska D. Antimicrob Agents Chemother, August 2006, 50(8):2595-601.

Summary: A series of azasterol derivatives, designed as potential inhibitors of the Δ24 –sterol methyltransferase enzyme (24-SMT), were synthesized and evaluated for their activities against parasitic protozoa. We conclude that the designed compounds act at sites other than 24-SMT in Trypanosoma brucei.

Click here to download the full article [PDF]