Berryman K A, Edmunds J J, Bunker A M, Haleen S, Bryant J, Welch K M, Doherty A M
Department of Chemistry, Parke-Davis Pharmaceutical Research, Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Bioorg Med Chem. 1998 Sep;6(9):1447-56. doi: 10.1016/s0968-0896(98)00080-7.
The development of benzothiazine-1,1-dioxide derivatives as a new structural class of potent endothelin receptor antagonists is described. Structure-activity relationships (SAR) revealed that PD164800 (1) is a potent antagonist of the ETA receptor subtype.
本文描述了苯并噻嗪-1,1-二氧化物衍生物作为一类新型强效内皮素受体拮抗剂的研发情况。构效关系(SAR)表明,PD164800(1)是ETA受体亚型的强效拮抗剂。