Arthur A. Patchett

Arthur Allan Patchett (born May 28, 1929 in Middletown (New York) ) is an American chemist .

Life

Patchett studied chemistry at Princeton University with a bachelor's degree summa cum laude in 1951, was a Fulbright scholar at Cambridge University in 1951/52 and received his doctorate in 1955 from Harvard University with Robert B. Woodward (on the synthesis of lanosterol ). As a post-doctoral student he was with Bernhard Witkop at the National Institutes of Health , where he worked in biochemistry and on the synthesis of amino acid analogs. From 1957 he was with and Merck & Co . In 1962 he became head of the synthetic chemistry department and in 1972 a new central development center (New Lead Discovery Department) in which natural products made from fungi and bacteria ( Streptomycetaceae ) were screened for their effects .

Under his direction, the nonsteroidal anti-inflammatory drug diflunisal ( marketed as Dolobid ) was synthesized. The statin Mevacor ( lovastatin ) was developed and synthesized as a result of the screening projects at Merck & Co. It inhibited HMG-CoA reductase and thus lowered cholesterol and was the first such drug on the market. By adding a methyl group, it was developed into Zocor, a blockbuster for Merck & Co. ( Simvastatin ).

Enzyme inhibitors were also developed under his leadership, especially the ACE inhibitors Vasotec and Prinivil against high blood pressure. From the discovery of the CCK antagonist asperlicin (initially found during screening), Merck & Co. created a new strategy for rational drug development. A “privileged structure” was identified from the synthesis of simpler analogues - in this case based on the benzodiazepine scaffold - and used this as a starting point for other substances with coupling to G-protein-coupled receptors . For this purpose, libraries of derivatives of “privileged structures” with dipeptides as ligands were created. This resulted in agonists for somatostatin and melanocortin and secretagogue substances for growth hormones .

From 2002 he was a consultant at NeoGenesis (taken over by Schering-Plow from 2005).

He has published over 180 papers and holds over 180 US patents. In 1971 he headed the medicinal chemistry section of the ACS. From 1991 to 1998 he was co-editor of Medicinal Research Reviews. In 2001 Merck & Co. donated a professorship named after him at Princeton and he received an honorary doctorate from Bloomfield College.

In 2007 he received the NAS Award for Chemistry in Service to Society (for his role in the development of Mevacor, Vasotec and Prinivil). In 1987 and 1989 he received the Directors Scientific Award from Merck & Co., in 1992 the Discoverers Award from the Pharmaceutical Manufacturers Association, in 1993 the EB Hershberg Award and in 2002 the Alfred Burger Award from the ACS.

Web links

• ACS Medical Chemistry Hall of Fame