Novel series of O-substituted 8-quinolines and 4-benzothiazoles as potent antagonists of the bradykinin B2 receptors.
The synthesis and the SAR study of novel O-substituted 8-quinolines and 4-benzothiazoles as highly potent non-peptide bradykinin B2 receptor antagonists are described. Several members of this series of antagonists efficiently inhibited the BK-induced vasoconstriction on different isolated organ preparations.
Heitsch
H
H
Hoechst Marion Roussel GmbH, Frankfurt/Main, Germany. holger.heitsch@hmrag.com
Wagner
A
A
Schölkens
B A
BA
Wirth
K
K
D052160:Benzothiazoles; D065168:Bradykinin Receptor Antagonists; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D043782:Receptor, Bradykinin B2; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D052160:Benzothiazoles; D065168:Bradykinin Receptor Antagonists; D011804:Quinolines; D043782:Receptor, Bradykinin B2; D013844:Thiazoles; C005465:benzothiazole