Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2.
Basic Information
ID: ALA1135839
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2.
Authors: Ebiike H, Masubuchi M, Liu P, Kawasaki K, Morikami K, Sogabe S, Hayase M, Fujii T, Sakata K, Shindoh H, Shiratori Y, Aoki Y, Ohtsuka T, Shimma N.
Abstract: Modification of the C-2 position of a benzofuran derivative 6 (RO-09-4609), an N-myristoyltransferase (Nmt) inhibitor, has led us to discover antifungal agents that are active in a murine systemic candidiasis model. The drug design is based on the analysis of a crystal structure of a Candida Nmt complex with 2. The optimization has been guided by various biological evaluations including a quasi in vivo assay and pharmacokinetic analysis.
CiteXplore: 11844682
DOI: 10.1016/s0960-894x(01)00808-3
Patent ID: ┄