Benzimidazolil-kinolinil-merkaptotriazoli kao potencijalni antimikrobni i antivirusni agensi

Condensation of ethylaceto acetate (EAA) with resorcinol in concentrated H2SO4 afforded 7-hydroxy-4-methyl coumarin (1) which on reaction with thiosemicarbazide in anhydrous pyridine yielded 7-hydroxy-4-methyl-quinolinyl [1,5-c]-mercaptotriazole (2). Reaction of 2 with formaldehyde solution and amino acid in ethanol yielded 7-hydroxy-4-methyl-8-(N-methyl-aminoacid)-quinolinyl [1,5-c]-2"-mercaptotriazole (3). Interaction of 3 with o-phenylenediamine in pyridine yielded 7-hydroxy-4-methyl-8-(aminobenzimidazolyl)-quinolinyl [1,5-c]-2"-mercaptotriazole derivatives (4a-e). The latter compounds were evaluated for their antiviral and antimicrobial activities.Kondenzacijom etilacetoacetata (EAA) s rezorciolom u koncentriranoj H2SO4 dobiven je 7-hidroksi-4-metil kumarin (1) koji u reakciji s tiosemikarbazidom u bezvodnom piridinu daje 7-hidroksi-4-metil-kinolinil [1,5-c]-merkaptotriazol (2). Reakcijom spoja 2 s otopinom formaldehida i aminokiselinom u etanolu nastao je 7-hidroksi-4-metil-8-(N-metil-aminokiselina)-kinolinil [1,5-c]-2"-merkaptotriazol (3), koji je s o-fenilendiaminom u piridinu dao 7-hidroksi-4-metil-8-(aminobenzimidazolil)-kinolinil [1,5-c]-2\u27\u27-merkaptotriazol derivate (4a-e). Ispitano je antivirusno i antimikrobno djelovanje spojeva 4

Synthesis of some new quinolinylimidazoles for their antiviral and antifungal activities

527-529Condensation of resorcinol with ethyl acetoacetate in conc. H2SO4 yields 7-hydroxy-4-methyl coumarin 1 which on reaction with thiosemicarbazide affords 1-thiouryl-7-hydroxy-4-methyl carbostyril 2. Compound 2 on heating with a dil. NaOH undergoes cyclization to give 7-hydroxy-4-methylquinolinyl[1,5-c]-2-mercaptoimidazole 3. Interaction of 3 with 5-oxo-2-phenyl-3-styryl-1,3 oxazole affords 2-[5'-oxo-2'-phenyl-sulphoarylideno 1,3-oxazolo]-7-hydroxy-4-methylquinolinyl [1,5-c] imidazole 4. Reaction of 4 with aromatic aldehyde yield 2-[5'-oxo-2'-phenyl sulphoarylideno-1,3-oxazolo]-7-hydroxy-4-styryl-quinolinyl [1,5-c] imidazoles 5. The new compounds 5 have been screened for their antiviral and antifungal activities

Synthesis, characterization and biological activity of 1,3,4-substituted 2-azetidinones

158-162Amido/imido alcohol/2-phenyl-3-hydroxyethylquinazolin-4 (3H) -one 1 on treatment with benzoic acid in the presence of conc. H2SO4 yields m-(aralkylamido/imidoalkyl/2-phenyl-3-ethyl-3H-4-oxoquinazolinyl) benzoic acids 2. The acid chloride of 2 on reaction with hydrazine hydrate affords m-(aralkylamido/imidoalkyl/2-phenyl-3-ethyl-3H-4-oxo-quinazolinyl) benzoic acid hydrazides 4 which on condensation with an aromatic aldehyde in acetic acid gives m-(aralkylamido/imidoalkyl/2-phenyl-3-ethyl-3H-4-oxo-quinazolinyl) benzoic acid hydrazones 5. Compounds 5 undergo cyclization with phenoxy acetic acid in the presence of thionyl chloride in dry benzene to furnish 1-[m-(aralkylamido/imidoalkyl/2-phenyl-3-ethyl-3H-4-oxo-quinazolinyl-benzamido)]-3-phenoxy-4-phenyl-2-azetidinones 6. The antiviral and antifungal activities of 6 have been reported