Statistical molecular design, parallel synthesis, and biological evaluation of a library of thrombin inhibitors

A Linusson, J Gottfries, T Olsson…

Index: Linusson; Gottfries; Olsson; Oernskov; Folestad; Norden; Wold Journal of Medicinal Chemistry, 2001 , vol. 44, # 21 p. 3424 - 3439

Full Text: HTML

Citation Number: 62

Abstract

A library of thrombin inhibitors has been designed using statistical molecular design. An aromatic scaffold was used, with three varied positions corresponding to three pockets at the active site of thrombin (the S-, P-, and D-pockets). The selection was performed in the building block space, and previously acquired data were included in the design procedure. The design resulted in six, four, and six building blocks for the first (S), second (P), and ...