Benzo b thiophene derivs antibacterials antivirals

摘要

(A) Medicinal use of benzo(b)thiophenes which are (a) subst. by at least one Z and (b) by at least one Z and (b) by at least one halogen, alkoxy, alkyl, haloalkyl, carboxyl, carboxyalkyl, nitro, cyano, amino, alkylamino, haloalkylamino, acylamino, aryl-acylamino or arylacyloxyamino group, and their addition salts and quaternary ammonium derivs. where Z = (B)n-Y, or together with the thiphene ring of the benzothiphene nucleus forms a 5- or 6-membered heterocyclic ring contng. at least 1 N-atom and opt. subst. by alkyl or aryl (the N-atom can be subst. by 1 or 2 alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, aralkyl, amidine or guanidine groups or can be part of a further heterocyclic ring, i.e. forming a spiro cpd.) n = 0 or 1 B = C1-4 alkylene chain Y = (i) -NHCONH2, (ii) -NHC(=NH)NH2, (iii) -NHC(=NH)NHC(=NH)NH2, (iv) -CONH2, (v) -C(=NH)OR1 (R1=alkyl or aryl), (vi) -C(=NH)NH2, (vii) -C(=NOR2)NH2 (R2=H, alkyl or aryl), (viii) -NHR (R=acyl or arylacyl), (ix) (when B contains 1, 3 or 4 C-atoms) amino, dialkylamino, diaralkylamino, pyrrolidine, piperidine or morpholine residue, or an N-alkyl, N-aryl, N-carboxyalkyl or N-carboxyaryl deriv. of one of groups (I)-(viii). - (B) The above cpds., except: those unsubst. benzothiphenes and alkoxy-benzothiophenes in which Z together with the thiphene ring forms a 6-membered heterocyclic ring contng. an unsubstd. N-atom; those unsubst benzothiphenes in which Z is (B)n-Y, n is 1, B is a 3-methylene group and either Y is (v) in which R1 is Et or Y is (viii) in which R is acetyl; and those unsubst. or subst. benzothiphenes in which Z is (B)n-Y, n is 1 and either B is a 3-methylene group and Y is (ix) or B is a 2-methylene group and Y is amino, dialkylamino or diaralkylamino. - Antibacterials, antivirals, fungicides, anthelmintics and some hypotensives.