摘要 |
PURPOSE:To provide a new imidazole derivative exhibiting a strong angiotensin II receptor antagonism and useful for improving hypertension, congestive heart failure or intraocular hejpertension. CONSTITUTION:A compound of formula I [R1 is a lower alkyl; R2 is H, a halogen or NO2; R3 is a lower alkyl, a substitutive aryl or a substitutive heteroaryl; R4, R5 and R7 are each H, OH, a halogen, hydroxymethyl, formyl, carboxyl, a lower alkoxy, a lower alkoxycarbonyl, tetrazol-5-yl, carbamoyl or formula II; A is CO or CH2; B is CO or (CH2)mCHR6 (R6 is H, a lower alkyl or a substitutive aryl; (m) is 0 to 2); (n) is 1 or 2], e.g. N-benzyl-2-n-butyl-1-(4- carbomethoxyphenyl) methyl-N-(1H-tetrazol-5-yl)-5-imidazolecarboxamide. In the case of A=CH2, the compound of formula I can be obtained by reacting a compound of formula III (X is an eliminable group) with a compound of formula IV. |