Author/Authors :
Robert M. Adlington، نويسنده , , Jack E. Baldwin، نويسنده , , Beining Chen، نويسنده , , Stephen L. Cooper، نويسنده , , William McCoull، نويسنده , , Gareth J. Pritchard، نويسنده , , Trevor J. Howe، نويسنده , , Gerald W. Becker، نويسنده , , Robert B. Hermann، نويسنده , , Ann M. McNulty، نويسنده , , Blake L. Neubauer، نويسنده ,
Abstract :
A novel series of monocyclic β-lactam analogues was designed using a homology derived model of prostate specific antigen (PSA) and by application of a multiple copy simultaneous search technique. Syntheses were conducted by assembly of the β-lactam core via a Staüdinger reaction with elaboration at the 1, 3 and 4 positions to probe active site binding. Inhibition against PSA was evaluated.