Hydroxyaromatic aldehydes and ketones were used as building blocks to prepare ether oligomers. An iterative two-step protocol involving Mitsunobu coupling and carbonyl reduction provided a protecting-group-free route with high yields. Activity screening of an 84-member library against proteases led to the discovery of micromolar inhibitors for trypsin, chymotrypsin, and subtilisin.
Hydroxyaromatic aldehydes and ketones were used as building blocks to prepare ether oligomers. An iterative two-step protocol involving Mitsunobu coupling and carbonyl reduction provided a protecting-group-free route with high yields. Activity screening of an 84-member library against proteases led to the discovery of micromolar inhibitors for trypsin, chymotrypsin, and subtilisin.
3-ARYL-2-HYDROXYPROPIONIC ACID DERIVATIVES AND ANALOGS AS HYPOGLYCEMIC AGENTS
申请人:PFIZER INC.
公开号:EP0533781A1
公开(公告)日:1993-03-31
US5232945A
申请人:——
公开号:US5232945A
公开(公告)日:1993-08-03
US5306726A
申请人:——
公开号:US5306726A
公开(公告)日:1994-04-26
US5438074A
申请人:——
公开号:US5438074A
公开(公告)日:1995-08-01
[EN] 3-ARYL-2-HYDROXYPROPIONIC ACID DERIVATIVES AND ANALOGS AS HYPOGLYCEMIC AGENTS
申请人:PFIZER INC.
公开号:WO1991019702A1
公开(公告)日:1991-12-26
(EN) Certain 3-(phenyl, chroman-2-yl, benzofuran-5-yl or benzoxazole-5-yl)-2-(hydroxy or mercapto)propionic acid derivatives and analogs are useful as hypoglycemic and hypocholesterolemic agents.(FR) L'invention se rapporte à certains dérivés d'acide 3-(phényle, chroman-2-yle, benzofuran-5-yle ou benzoxazol-5-yle)-2(hydroxy ou -mercapto) propionique et à leurs analogues, qui sont utiles comme agents hypoglycémiques et hypocholestérolémiques.