HALOGEN SUBSTITUTION AT THE ISOXAZOLE RING ENHANCES THE ACTIVITY OF N-(ISOXAZOLYL)SULFONAMIDE ENDOTHELIN ANTAGONISTS

Authors
CHAN MF RAJU B KOIS A CASTILLO RS VERNER EJ WU CD HWANG E OKUN I STAVROS F BALAJI VN
Citation
Mf. Chan et al., HALOGEN SUBSTITUTION AT THE ISOXAZOLE RING ENHANCES THE ACTIVITY OF N-(ISOXAZOLYL)SULFONAMIDE ENDOTHELIN ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(20), 1996, pp. 2393-2398
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
20
Year of publication
1996
Pages
2393 - 2398
Database
ISI
SICI code
0960-894X(1996)6:20<2393:HSATIR>2.0.ZU;2-T
Abstract
Replacement of the 4-methyl group in a series of N-(3, 4-dimethylisoxa zolyl)benzenesulfonamide endothelin antagonists with a bromine or chlo rine atom resulted in a three- to ten-fold increase in the binding aff inity for both the ET(A) and ET(B) receptors. This potentiation in act ivities was also observed for naphthalene and biphenylsulfonamide endo thelin antagonists. Copyright (C) 1996 Elsevier Science Ltd.