RESUMO
The synthesis of new N,N-disubstituted carbamodithioic acid 2-oxo-2-(diphenylamino) ethyl esters is reported. The structures of these compounds are supported by their UV, IR and 1H-NMR spectra, as well as by elemental analysis. The new compounds were tested for their anticholinergic activities.
Assuntos
Parassimpatolíticos/síntese química , Tiocarbamatos/síntese química , Acetilcolina/farmacologia , Animais , Atropina/farmacologia , Fenômenos Químicos , Físico-Química , Feminino , Íleo/efeitos dos fármacos , Técnicas In Vitro , Masculino , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Ratos , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Tiocarbamatos/farmacologiaRESUMO
The synthesis of new 3-aroylmethyl-2H-1,3-benzoxazinedione derivatives is reported. The structure of these products are supported by their UV, IR and 1H-NMR spectra, as well as by elemental analysis. The new compounds were tested for their anticholinergic and antihistaminic activities.
Assuntos
Antagonistas dos Receptores Histamínicos/síntese química , Oxazinas/síntese química , Parassimpatolíticos/síntese química , Animais , Feminino , Antagonistas dos Receptores Histamínicos/farmacologia , Contração Isométrica/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Masculino , Músculo Liso/efeitos dos fármacos , Oxazinas/farmacologia , Parassimpatolíticos/farmacologia , Coelhos , Ratos , Espectrofotometria Infravermelho , Espectrofotometria UltravioletaAssuntos
Parassimpatolíticos/síntese química , Tiocarbamatos/síntese química , Acetilcolina/antagonistas & inibidores , Acetilcolina/farmacologia , Animais , Atropina/farmacologia , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Ratos , Tiocarbamatos/farmacologiaAssuntos
Acetamidas/síntese química , Acetonitrilas/síntese química , Analgésicos/síntese química , Benzoxazóis/síntese química , Acetamidas/farmacologia , Acetonitrilas/farmacologia , Analgésicos/farmacologia , Animais , Benzoxazóis/farmacologia , Feminino , Camundongos , Peso Molecular , Medição da Dor/efeitos dos fármacos , Espectrofotometria UltravioletaRESUMO
Some new N-arylazole acetamide derivatives have been prepared by the reaction of alpha-bromo-N-arylacetamide with imidazole, pyrazole and 1,2,4-triazole. The structures of these compounds have been confirmed by UV, IR, 1H-NMR and elementary analysis. Their anticonvulsant activities were determined by maximal electroshock (MES) and subcutaneous metrazol (Scmet) tests. Most of the compounds showed anticonvulsant activity with significantly low neurotoxicity according to Phase I tests. Compound 6 carrying alpha-naphthyl and 1,2,4-triazole was found active in the MES test with ED50 = 64.9 mg/kg and TD50 = 221.0 mg/kg but it was not active in corneally stimulated rats. Antibacterial and antifungal activities of the compounds were determined against S. aureus, E. coli, P. aeruginosa, C. albicans, C. parapsilosis, C. pseudotropicalis and C. stellatoidea by using the microdilution broth method. Compounds 8 and 10 showed significant activity (MIC < 32 micrograms/ml) against various Candida species.
Assuntos
Acetamidas/síntese química , Anti-Infecciosos/síntese química , Anticonvulsivantes/síntese química , Acetamidas/química , Acetamidas/farmacologia , Animais , Antibacterianos , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anticonvulsivantes/química , Anticonvulsivantes/farmacologia , Antifúngicos/síntese química , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Córnea/fisiologia , Estimulação Elétrica , Eletrochoque , Fungos/efeitos dos fármacos , Masculino , Camundongos , Testes de Sensibilidade Microbiana , Pentilenotetrazol/antagonistas & inibidores , Equilíbrio Postural/efeitos dos fármacos , RatosRESUMO
Thirteen 3-acetyl-4-aryl-5-oxo-2,7,7-trimethyl-1,4,5,6,7,8- hexahydroquinoline derivatives (5a-m), one of which was synthesized before, have been prepared. The structures of the products 5b-m were characterized by IR,1H-NMR and elemental analysis. The calcium antagonistic activity of these compounds was studied in rabbit taenia coli precontracted with 1 mmol/l Ca+2.
Assuntos
Bloqueadores dos Canais de Cálcio/síntese química , Quinolinas/síntese química , Animais , Bloqueadores dos Canais de Cálcio/química , Bloqueadores dos Canais de Cálcio/farmacologia , Feminino , Cobaias , Técnicas In Vitro , Espectroscopia de Ressonância Magnética , Masculino , Peso Molecular , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Nicardipino/farmacologia , Quinolinas/química , Quinolinas/farmacologia , CoelhosRESUMO
Fourty-three new benzoxazolinone derivatives having a piperazinomethyl group at the third position of the ring were synthesized by using appropriate benzoxazolinones and 4-substituted piperazines via a Mannich reaction. The structures of the compounds were elucidated by spectral data and microanalyses. Analgesic activities were evaluated by a modified Koster test. All compounds, except 7, 14, 21, 32, and 41, showed analgesic activity higher than that of acetylsalicylic acid. The compounds were also screened for their anti-inflammatory activity using a carrageenan paw edema test, and those exhibiting high anti-inflammatory activity were investigated for their ability to inhibit prostaglandin E2 induced paw edema. The results of anti-inflammatory testing indicated that most of the compounds were more active than indometacin. Ulcerogenic activities of the compounds were also studied and no gastrointestinal bleeding was observed at the 100 mg/kg dose level.