RESUMEN
A number of novel pyrimido[4,5-d]pyrimidine-2,7-dithone derivatives bearing hydrazino and N-benzylidinehydrazino substitution were efficiently synthesized and screened for in vitro antibacterial activities against the representative panel of three Gram-positive and two Gram-negative bacteria. All the synthesized compounds showed the potent inhibitory action against Gram-positive bacteria. Particularly, N-benzylidinehydrazino-substituted compounds imparted profound effect. Furthermore, the Connolly-accessible surface area values were also calculated for the target compounds and correlated with the expressed biological activity.
Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Dipiridamol/síntesis química , Hidrazinas/síntesis química , Antiinfecciosos/química , Dipiridamol/análogos & derivados , Dipiridamol/farmacología , Escherichia coli/efectos de los fármacos , Escherichia coli/crecimiento & desarrollo , Bacterias Grampositivas/efectos de los fármacos , Bacterias Grampositivas/crecimiento & desarrollo , Hidrazinas/química , Hidrazinas/farmacología , Pruebas de Sensibilidad Microbiana/métodos , Modelos Químicos , Modelos Moleculares , Estructura Molecular , Pseudomonas aeruginosa/efectos de los fármacos , Pseudomonas aeruginosa/crecimiento & desarrollo , Relación Estructura-ActividadRESUMEN
A new series of 10-methyl-6-oxo-5-arylazo-6,7-dihydro-5H-[1,3]azaphospholo[1,5-d][1,4]benzodiazepin-2-phospha-3-ethoxycarbonyl-1-phosphorus dichlorides 11a-p has been synthesized and evaluated as antimicrobial agents. Structures of all the synthesized compounds were established on the basis of elemental analysis and spectroscopic data. Quantitative structure-activity relationship (QSAR) investigations were applied to find out the correlation between the experimentally evaluated activity with various parameters of the compounds studied. QSAR equations showed that the molecular refractivity correlates significantly with the antimicrobial activity.
Asunto(s)
Antiinfecciosos , Relación Estructura-Actividad Cuantitativa , Antiinfecciosos/síntesis química , Antiinfecciosos/química , Antiinfecciosos/farmacología , Aspergillus niger/efectos de los fármacos , Candida albicans/efectos de los fármacos , Cristalografía por Rayos X , Evaluación Preclínica de Medicamentos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Técnicas In Vitro , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Estructura Molecular , Estereoisomerismo , Relación Estructura-ActividadRESUMEN
A new series of 5-[(3'-chloro-4',4'-disubstituted-2-oxoazetidinyl)(N-nitro)amino]-6-hydroxy-3-alkyl/aryl[1,3]azaphospholo[1,5-a]pyridin-1-yl-phosphorus dichlorides has been synthesized and subjected to acute antibacterial and antifungal screening studies. All the derivatives belonging to this series delineated remarkable activity as compared to standard drugs (ampicillin and clotrimazole). Compounds are quantitatively analyzed in relation to their different physicochemical parameters. Significant correlations were obtained between biological activity and polarizability parameter (MR).
Asunto(s)
Antibacterianos/síntesis química , Antifúngicos/síntesis química , Piridinas/síntesis química , Relación Estructura-Actividad Cuantitativa , Antibacterianos/química , Antibacterianos/farmacología , Antifúngicos/química , Antifúngicos/farmacología , Bacterias/efectos de los fármacos , Cloruros , Hongos/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Piridinas/farmacologíaRESUMEN
A number of pyrimido[4,5-d]pyrimidine-2,5-dione derivatives were synthesized and screened for antibacterial and antifungal activities. All the synthesized compounds showed the potent antimicrobial activity. The quantitative structure-activity relationship investigation was applied to find a correlation between the different physicochemical parameters of the compounds studied and their biological activity.
Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Pirimidinas/síntesis química , Pirimidinas/farmacología , Antiinfecciosos/química , Modelos Moleculares , Pirimidinas/química , Relación Estructura-Actividad CuantitativaRESUMEN
A number of 2-hydroxy-6-methyl-7-(arylamino)-1,7-dihydropurin-8-ones have been synthesized. 3-Oxo-2-(arylhydrazono)butyric acid ethyl ester were acetylated and treated with triethyl amine and formamide in presence of 1,4-dioxane to yield N-(5-acetyl-4-ethoxy-2-oxo-2,5-dihydro-imidazol-1-yl)-N-arylacetamide, which on refluxation with urea and freshly prepared sodium ethoxide yielded the title compound. All the newly synthesized compounds have been characterized by spectroscopic and elemental analysis data. The synthesized compounds were screened against a representative panel of susceptible and resistant Gram-positive and Gram-negative bacteria using a standard antibiotic drug purinthol as control. Quantitative structure-activity relationship has also been interpreted in terms of correlation of biological activity with molecular refractive index parameters (M(R)) and Hammett substituent constant (sigma).