| 摘要 |
Tetrazole derivs. of formula (I) and their salts are new: (where (a) R1 is lower alkyl or phenyl and R2 is BCOR4, or (b) R1 is S(O)n-A-(X)m-R3 and R2 is H, lower alkyl, phenyl or cycloalkyl. In case (a), B is lower alkylene and R4 is OH, lower alkoxy or NR1OR11, where R10 and R11 are (i) H, (ii) lower alkyl opt. substd. by OH, furyl, pyridyl, phenyl or mono- or dialkoxyphenyl, (iii) cycloalkyl opt. substd. by OH or alkoxy, (iv) phenyl opt. mono- or disubstd. by alkyl, alkoxy, halogen, NO2, COOH and/or alkylamino, or (v) thiazolyl, or NR1OR11 is a 5- or 6- membered satd. ring opt. contg. another heteroatom (N or O) and opt. substd. by alkyl. In case (b). X is CO or S(O)x; n and x are 0-2; m = 0 or 1; A is 1-8C alkylene; R3 is (i) lower alkyl, cycloalkyl or naphthyl, (ii) C(NH)NHR5, where R5 is alkyl, (iii) phenylalkyl opt. ring-substd. by halogen, (iv) phenyl opt. substd. by 1-3 gps. selected from halogen, alkyl, alkoxy, alkanoylamino, OH, COOH and NH2, (v) pyridyl-, furyl- or thiazolyalkyl opt. substd. by alkyl or NH2, (vi) a heterocyclic gp. with 1-4 heteroatoms selected from N, O and S and opt. 1 or 2 substituents selected from alkyl, halogen, COOH, oxo, NH2, alkoxycarbonyl, alkoxy, OH, NO2, Ph, cycloalkyl and alkylamino, or (vii) NR6R7, where R6 is H, alkyl or phenylalkyl and R7 is H, alkyl, C(Z)NHR8, tetrazolyl, alkyltetrazolyl or COR9, where Z is S, NH or N-alkyl, R8 is alkyl or NH2 and R9 is alkyl, phenyl, mono-, di- or trialkoxyphenyl, cycloalkyl or a 5- or 6- membered unsatd. heterocyclic gp. with a N or O heteroatom, or NR6R7 is phthalimido; with the proviso that m must be O when R3 is NR6R7, and that R3 cannot be unsubstd. phenylalkyl or phenyl when m=O). (I) have anti-ulcer activity, e.g. giving more than 50% redn. in gastric juice vol., total acidity and pepsin activity at doses of 100 mg/kg (s.c., rat) in the Shay pylorus ligation test. - |
