| 摘要 |
Benzoylguanidine derivatives (I) and their salts are new. Benzoylguanidine derivatives of formula (I) and their salts are new. [Image] R 1H, halo, NO 2, CN, (X) o-(CH 2) p-(CF 2) q-CF 3, SO m-R 5, COR 6, CONR 6R 7 or SO 2-NR 6R 7; R 3H, halo, NO 2, CN, (X) o-(CH 2) p-(CF 2) q-CF 3, SO m-R 5, COR 6, CONR 6R 7, SO 2-NR 6R 7, 1-6C alkyl or X-R 1 3; X : O, S or NR 1 4; m, p : 0-2; o : 0 or 1; q : 0-6; R 51-8C alkyl, 3-6C alkenyl, (CH 2) n-R 8 or CF 3; R 6H, 1-8C alkyl, 3-6C alkenyl, (CH 2) n-R 8 or CF 3; R 7H or 1-4C alkyl; n : 0-4; R 83-7C cycloalkyl or phenyl (optionally substituted by 1-3 F, Cl, CF 3, CH 3, OCH 3 or NR 9R 1 0 groups); R 2Y-Q; Q : phenyl substituted by heteroaryl which is optionally substituted by 1-3 F, Cl, CF 3, CH 3, OCH 3, OH, NH 2, NHCH 3, N(CH 3) 2 or benzyl groups; Y : O, S or NR 1 2; R 1 2H or 1-4C alkyl; R 1 4H or 1-3C alkyl; R 1 3H, 1-6C alkyl, 3-8C cycloalkyl or (CH 2) b-R 1 5; R 4halo or 1-4C alkyl; b : 0-4; and R 1 5optionally substituted phenyl; or R 6+R 7 or R 1 3+R 1 4 together : (CH 2) 4 or (CH 2) 5, where a CH 2 group can be replaced by S, S, NH, NCH 3 or N-benzyl. - ACTIVITY : Vasotropic; cardiant; antiarrhythmic; antianginal; cerebroprotective; antiallergic; antibacterial; immunosuppressive; antiarteriosclerotic; antidiabetic; cytostatic; hypotensive; anticoagulant; thrombolytic; antilipemic - MECHANISM OF ACTION : Sodium antagonist; vasodilator; LDL antagonist; VLDL antagonist |
