RESUMEN
In order to obtain new compounds with potential antimicrobial activity some new (sulfon-amidophenyl)-amide derivatives of N-(m-nitrobenzoil)-D,L-methionine have been synthesized. The compounds have been obtained by decyclization reaction of 2-(m-nitrophenyl)-4-(beta-P-methylthioethyl)- delta2-5-oxazolinone with various sulfonamides. The chemical structure of the new sulfonamides was confirmed by elemental analysis data and IR and 1NMR spectral measurements. The compounds were also investigated for their antimicrobial activity using Staphylococcus aureus, Escherichia coli, Listeria monocytogenes and Proteus vulgaris strains.
Asunto(s)
Antibacterianos/síntesis química , Antibacterianos/farmacología , Metionina/análogos & derivados , Metionina/biosíntesis , Sulfonamidas/síntesis química , Escherichia coli/efectos de los fármacos , Humanos , Listeria monocytogenes/efectos de los fármacos , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana/métodos , Proteus vulgaris/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacosRESUMEN
In order to obtain new compounds with potential antibacterial activity some new (sulfonamidophenyl)-amide derivatives of N-(m-nitrobenzoil)-D,L-asparagine have been synthesized. The compounds have been obtained by decyclization reaction of 2-(m-nitrophenyl)-4-(beta-amidomethyl)-delta2-oxazolinone with various sulfonamides. A toxicity study with determination of DL50 value has also been realized.
Asunto(s)
Asparagina/síntesis química , Asparagina/toxicidad , Sulfonamidas/síntesis química , Sulfonamidas/toxicidad , Animales , Antibacterianos/síntesis química , Antibacterianos/farmacología , Antimetabolitos/síntesis química , Antimetabolitos/farmacología , Asparagina/análogos & derivados , Dosificación Letal Mediana , Masculino , Ratones , Modelos AnimalesRESUMEN
In order to obtain new biologically active compounds some derivatives of 1-[N-(m-nitrobenzoyl)-alpha-D,L-asparaginyl]-2-benzyl-benzimidazole have been synthesized by ring opening reactions of 2-(m-nitrophenyl)-4-(beta-amidomethyl)-delta 2-oxazolin-5-one and 2-(m-nitrophenyl)-4-(beta-carboxymethyl)-delta 2-oxazolin-5-one with 2-benzylbenzimidazole (dibazole).
Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/uso terapéutico , Bencimidazoles/farmacología , Bencimidazoles/uso terapéutico , Inflamación/tratamiento farmacológico , Animales , Antiinflamatorios no Esteroideos/farmacocinética , Bencimidazoles/farmacocinética , Modelos Animales de Enfermedad , RatonesRESUMEN
This study presents the synthesis of ten new hydrazides with 1,2,4-triazole support. The structures of the obtained compounds were elucidates by means of the elemental analysis data as well as by IR spectral measurements. The antimicrobial and antifungal actions of this derivates are also tested. The results show that the compounds with the functional group 4-chlore-2-methoxyphenyle are more active.
Asunto(s)
Antiinfecciosos/síntesis química , Triazoles/síntesis química , Antibacterianos , Antiinfecciosos/química , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Candida albicans/efectos de los fármacos , Pruebas de Sensibilidad Microbiana/estadística & datos numéricos , Relación Estructura-Actividad , Triazoles/química , Triazoles/farmacologíaRESUMEN
To obtain new compounds with biological activity, 1-[N-(p-nitrobenzoyl)-alpha-D,L- asparagyl]-benzimidazole derivatives were synthesized by decyclization of 2-(p-nitrophenyl)-4-[2'- (diethylamino) ethyl-carboxymethyl]-delta 2-oxazolinone-5 with benzimidazole, 2-methylbenzimidazole and 5,6-dimethyl-benzimidazole. The synthesized products show a hypotensive action comparable to that Hipopresol.
Asunto(s)
Antihipertensivos/química , Ácido Aspártico/análogos & derivados , Bencimidazoles/química , Animales , Antihipertensivos/farmacología , Ácido Aspártico/química , Ácido Aspártico/farmacología , Bencimidazoles/farmacología , Presión Sanguínea/efectos de los fármacos , Gatos , Relación Estructura-ActividadAsunto(s)
Alquilantes/síntesis química , Antineoplásicos/síntesis química , Compuestos de Mostaza Nitrogenada/síntesis química , Alquilantes/toxicidad , Animales , Antineoplásicos/toxicidad , Femenino , Dosificación Letal Mediana , Masculino , Ratones , Compuestos de Mostaza Nitrogenada/toxicidad , Relación Estructura-ActividadRESUMEN
New imidazolines derived from sulphonamidated aryloxyalkylcarboxylic acids have been tested for their antihypertensive action and toxicity. The obtained results attest a remarkable biological action, low toxicity and a good absorption in oral administration.