RESUMO
A series of substituted N-arylphthalamic acids 3a-i has been synthesized by the reaction of phthalic anhydride 1 and aryl- or heterocyclic amines 2a-i, in the absence of solvents, in a domestic microwave oven. The formation of nine N-arylphthalamic acids was accomplished in 1-3 min giving excellent yields for compounds 3a-g, but moderate yield of compounds 3h and 3i, respectively. Compounds 3h and 3i are new. Interestingly, N-arylphthalamic acids 3a-i induced hyperlipidemia in Swiss white mice and also increased animals' body weight.
Assuntos
Hipolipemiantes/síntese química , Ácidos Ftálicos/síntese química , Animais , Peso Corporal/efeitos dos fármacos , Hiperlipidemias/induzido quimicamente , Hiperlipidemias/metabolismo , Hipolipemiantes/química , Hipolipemiantes/toxicidade , Camundongos , Micro-Ondas , Modelos Animais , Ácidos Ftálicos/química , Ácidos Ftálicos/toxicidadeRESUMO
A facile synthesis of anomerically pure phthalimidomethyl 2,3,4,6-tetra-O-acetyl- and phthalimidomethyl 2,3-di-O-acetyl-4,6-di-O-benzoyl-alpha-D-mannopyranosides (6 and 9b) starting from N-hydroxymethylphthalimide and tri-O-acetyl-D-glucal is described. Compounds 3, 6, 8, 9a and 9b have been tested for their hypolipidemic activity in mice. All these compound showed significant reduction of plasma cholesterol and triglyceride levels. Compound 9b has been found to possess the highest activity.
Assuntos
Hipolipemiantes/síntese química , Manosídeos/farmacologia , Animais , Colesterol/sangue , Hipolipemiantes/farmacologia , Masculino , Manosídeos/síntese química , Camundongos , Ftalimidas/síntese química , Ftalimidas/farmacologia , Triglicerídeos/sangueRESUMO
A new series of 1,2,4-oxadizoles 6a-g have been synthesised in good yields using the peptide synthesis strategy. The prepared compounds were tested for anti-inflammatory and antimicrobial activities. The anti-inflammatory activities were determined in the rat paw oedema induced by carrageenin. Compounds 6a, c, f and g (i.v.) significantly inhibited the rat paw oedema induced by carrageenin depending upon the dose employed. The compounds were also evaluated for their in vitro antimicrobial activity. Some compounds were found to have significant activity against Gram positive and Gram negative microorganisms.
Assuntos
Anti-Infecciosos/síntese química , Anti-Inflamatórios não Esteroides/síntese química , Oxidiazóis/química , Animais , Antibacterianos , Bactérias/efeitos dos fármacos , Carragenina , Edema/induzido quimicamente , Edema/prevenção & controle , Fungos/efeitos dos fármacos , Masculino , Testes de Sensibilidade Microbiana , Oxidiazóis/farmacologia , Ratos , Ratos WistarRESUMO
Seven new phthalimide derivatives (9a-g) with 1,2,4-oxadiazol-5-yl methyl group attached to nitrogen have been synthesized from N-phthaloylglycine 6 and arylamidoximes 7a-g. All of these showed potent analgesic effect with acetic acid induced "writhing" test in mice. One of the better compounds (ID50 = 2.2 mg/Kg i.p.) has been found to be 9a which also demonstrates analgesic activity against inflammatory pain.
Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Ftalimidas/síntese química , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Camundongos , Ftalimidas/farmacologiaRESUMO
Significant local analgesic and anti-inflammatory activity has been observed after oral administration of 3-[3-(phenyl)-1,2,4-oxadiazol-5-yl] propionic acid (POPA). Doses of 150 and 300 mg/kg body weight administered orally by gavage to adult (25-35 g) albino mice of both sexes can inhibit acetic acid-induced writhing by 31.0% and 49.5%, respectively (mean +/- SEM writhing numbers during 20 min were 52.0 +/- 6.0 and 38.3 +/- 7.2 vs 75.8 +/- 6.6 for control group which received saline; N = 6). Carrageenin-induced inflammation in the female Wistar rat (200-250 g) can be reduced by 43.3% and 42.2% 3 h after oral administration (gavage) of 75 and 150 mg/kg of POPA (mean +/- SEM, 30.0 +/- 1.3% and 30.6 +/- 2.4% vs 52.9 +/- 3.7% for control group which received saline; N = 5). In the hot plate test on adult albino mice (25-35 g) of both sexes, POPA (150 and 300 mg/kg, po) was totally ineffective (N = 10). Our results indicate that POPA appears to offer potential safety and efficacy as a local analgesic and anti-inflammatory agent with no central nervous system involvement
Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios não Esteroides/uso terapêutico , Inflamação/tratamento farmacológico , Oxidiazóis/uso terapêutico , Dor/tratamento farmacológico , Administração Oral , Animais , Anti-Inflamatórios , Feminino , Masculino , Camundongos , Ratos , Ratos Wistar , Fatores de TempoRESUMO
Significant local analgesic and anti-inflammatory activity has been observed after oral administration of 3-[3-(phenyl)-1,2,4-oxadiazol-5-yl] propionic acid (POPA). Doses of 150 and 300 mg/kg body weight administered orally by gavage to adult (25-35 g) albino mice of both sexes can inhibit acetic acid-induced writhing by 31.0 and 49.5, respectively (mean +/- SEM writhing numbers during 20 min were 52.0 +/- 6.0 and 38.3 +/- 7.2 vs 75.8 +/- 6.6 for control group which received saline; N = 6). Carrageenin-induced inflammation in the female Wistar rat (200-250 g) can be reduced by 43.3 and 42.2 3 h after oral administration (gavage) of 75 and 150 mg/kg of POPA (mean +/- SEM, 30.0 +/- 1.3 and 30.6 +/- 2.4 vs 52.9 +/- 3.7 for control group which received saline; N = 5). In the hot plate test on adult albino mice (25-35 g) of both sexes, POPA (150 and 300 mg/kg, po) was totally ineffective (N = 10). Our results indicate that POPA appears to offer potential safety and efficacy as a local analgesic and anti-inflammatory agent with no central nervous system involvement