Benzylamine-based selective and orally bioavailabl...[Bioorg Med Chem Lett. 1998]

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1: Bioorg Med Chem Lett. 1998 Sep 22;8(18):2563-8. Links

Benzylamine-based selective and orally bioavailable inhibitors of thrombin.

Lee K, Jung WH, Park CW, Hong CY, Kim IC, Kim S, Oh YS, Kwon OH, Lee SH, Park HD, Kim SW, Lee YH, Yoo YJ.

Biotech Research Institute, LG Chemical Ltd./Research Park, Taejon, Korea.

A series of p-aminomethylphenylalanine derivatives were investigated as novel thrombin inhibitors. This study led to potent inhibitors of thrombin (Ki up to 3.3 nM) that are trypsin-selective, highly orally bioavailable in rats, and highly permeable across Caco-2 cells. The P1 benzylamine binding mode in the thrombin active site was identified by X-ray crystallographic analysis.

PMID: 9873581 [PubMed - indexed for MEDLINE]

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