2 - ENDOTHELIN ANTAGONISTS - EVALUATION OF 2,1,3-BENZOTHIADIAZOLE AS A METHYLENDIOXYPHENYL BIOISOSTER

Authors
MEDERSKI WWKR OSSWALD M DORSCH D ANZALI S CHRISTADLER M SCHMITGES CJ WILM C
Citation
Wwkr. Mederski et al., 2 - ENDOTHELIN ANTAGONISTS - EVALUATION OF 2,1,3-BENZOTHIADIAZOLE AS A METHYLENDIOXYPHENYL BIOISOSTER, Bioorganic & medicinal chemistry letters, 8(1), 1998, pp. 17-22
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
1
Year of publication
1998
Pages
17 - 22
Database
ISI
SICI code
0960-894X(1998)8:1<17:2-EA-E>2.0.ZU;2-R
Abstract
The methylendioxyphenyl group is present in a number of endothelin rec eptor antagonists thus far reported. By means of a Kohonen neural netw ork we discovered with a benzothiadiazole a bioisosteric replacement i nstead. This group should be devoid of the negative metabolic interact ions with cytochrome P450 ascribed to methylendioxyphenyl in vivo. The synthesis of a potent benzothiadiazole analogue EMD 122801 together w ith in vitro studies of different methylendioxyphenyl, benzothiadiazol e and benzofurazan derivatives is described. (C) 1997 Elsevier Science Ltd. All rights reserved.