RESUMO
Twelve different derivatives of substituted-{5-[2-(1,2,3,4-tetrahydrocarbazol-9-yl)ethyl]tetrazol-1-yl}alkanones (3-14) were synthesized by reacting 9-[2-(1H-tetrazol-5-yl)-ethyl]-2,3,4,9-tetrahydro-1H-carbazole (2) and the appropriate acid chlorides. 9-[2-(1H-tetrazol-5-yl) ethyl]-2,3,4,9-tetrahydro-1H-carbazole (2) was synthesized by reacting 3-(1,2,3,4-tetrahydrocarbazol-9-yl) propionitrile (1) with sodium azide and ammonium chloride. The chemical structures were confirmed by means of IR, 1H-NMR, mass spectra and elemental analysis. The compounds were screened for antinociceptive activity by acetic acid induced writhing method and hot plate method. 1-Phenyl-2-{5-[2-(1,2,3,4-tetrahydrocarbazol-9-yl)ethyl]tetrazol-1-yl}ethanone (13) was found to be the most active compound of the series.
Assuntos
Analgésicos/síntese química , Analgésicos/farmacologia , Cetonas/síntese química , Cetonas/farmacologia , Dor/prevenção & controle , Ácido Acético/química , Analgésicos/administração & dosagem , Animais , Avaliação Pré-Clínica de Medicamentos , Cetonas/administração & dosagem , Camundongos , Estrutura Molecular , Dor/induzido quimicamente , Medição da Dor/efeitos dos fármacosRESUMO
A series of novel 5[beta-(phenothiazinyl-10-yl)ethyl]-1-(acyl)-1,2,3,4-tetrazoles (3-14) have been synthesized via condensation of 5-[beta-(phenothiazinyl-10-yl)ethyl]-1-2,3,4-tetrazole (2) with various acylating/sulphonating reagents. 5-[beta-(phenothiazinyl-10-yl)ethyl]-1-2,3,4-tetrazole was synthesized by cyanoethylation of phenothiazine with acrylonitrile and Triton B, followed by the cycloaddition of 3-(phenothiazin-10-yl)-propionitrile (1) with sodium azide and ammonium chloride. The compounds were screened for analgesic activity, anti-inflammatory activity and ulcerogenicity index. Out of the 12 compounds synthesized, compound (5) 5[beta-(phenothiazinyl-10-yl)ethyl]-1-(benzoyl)-1,2,3,4-tetrazole, compound (11) 5[beta-(phenothiazinyl-10-yl)ethyl]-1-(p-tolyl)-1,2,3,4-tetrazole showed promising analgesic activity and compound (6) 5[beta-(phenothiazinyl-10-yl)ethyl]-1-(p-chlorobenzoyl)-1,2,3,4-tetrazole and compound (8) 5[beta-(phenothiazinyl-10-yl)ethyl]-1-(p-nitrobenzoyl)-1,2,3,4-tetrazole showed promising anti-inflammatory activity.
Assuntos
Analgésicos/síntese química , Analgésicos/farmacologia , Edema/tratamento farmacológico , Úlcera Gástrica/tratamento farmacológico , Tetrazóis/síntese química , Tetrazóis/farmacologia , Animais , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/farmacologia , Anticonvulsivantes/farmacologia , Carragenina/toxicidade , Edema/induzido quimicamente , Feminino , Masculino , Camundongos , Ratos , Úlcera Gástrica/induzido quimicamenteRESUMO
6-Amino penicillanic acid (6-APA) was condensed with D-alpha-phenyl glycine chloride in presence of E. coli NCIM 2563 to form ampicillin. At pH 5, 30% of 6-APA was converted to ampicillin during 1 hr incubation. When E. coli cells were immobilized in calcium alginate beads, the activity remained unaffected even after six batches of bioconversion. Inclusion of glutaraldehyde as multifunctional cross-linking agent, improved the stability of the biocatalyst beads.
