Antimicrobial and <i>in vitro</i> cytotoxicity of novel sulphanilamide condensed 1,2,3,4-tetrahydropyrimidines

Elumalai, Karthikeyan; Ali, Mohammed Ashraf; Srinivasan, S.; Elumalai, Manogaran; Eluri, Kalpana

doi:10.1016/j.jtusci.2015.01.005

Cited by 10 publications

(5 citation statements)

References 21 publications

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“…70 Some synthesized tetrahydropyrimidines showed excellent antimicrobial activities on Gram-negative and Gram-positive bacteria. 71,72 Williams et al assessed the inhibitory potency of some synthetic tetrahydropyrimidines on A. baumannii by measuring the MIC values. 73…”

Section: Discussionmentioning

confidence: 99%

Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe₃O₄@SiO₂ Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii

et al. 2020

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Background: Acinetobacter baumannii is a common infectious agent in hospitals. New antimicrobial agents are identified and prepared to combat these bacterial pathogens. In this context, the blocking potentials of a series of synthesized N-heterocyclic compounds, Cu/Fe3O4@SiO2 nanocomposites, glycine, poly-L-lysine, nisin and hydroalcoholic extracts of Trachyspermum ammi, Curcuma longa and green tea catechins were evaluated against non-resistant and multidrug-resistant strains of A. baumannii. Methods: Solutions of heterocyclic derivatives and hydroalcoholic extracts of Trachyspermum ammi, Curcuma longa and green tea catechins were prepared at initial concentration of 10240 μg ml-1 in 10% DMSO. Other compounds were dissolved in water at the same concentrations. Their in vitro inhibitory activity was assessed by determination of IZD, MIC and MBC values. Results: Glycine, poly-L-lysine, nisin, Curcuma longa and green tea catechins extracts, and thiazoles 3a, 3d and 3f were ineffective at their initial concentrations. Heterocyclic derivatives 7a-f, 3c, 3e and 3h, Cu/Fe3O4@SiO2 nanocomposites and Trachyspermum ammi extract could block the growth of bacterial strains with IZDs (7.40-15.51 mm), MICs (32-1024 µg ml-1) and MBCs (128-2048 µg ml-1). Conclusion: Among synthetic chemicals and natural products, the best antimicrobial effects were recorded with (E)-2-(5-acetyl-4-methylthiazol-2-yl)-2-(thiazolidin-2-ylidene)acetonitrile (7b) and the extract of Trachyspermum ammi. It is imperative that their toxic and histopathologic effects were assessed in future researches. It is predicted that the essential oil of Trachyspermum ammi will improve its antibacterial activities.

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Section: Discussionmentioning

confidence: 99%

Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe₃O₄@SiO₂ Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii

et al. 2020

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“…The synthesized compounds 67 were evaluated for in vitro antimicrobial and cytotoxicity against Bacillus subtilis, Escherichia coli and Vero cells. More recently, these authors published the synthesis, antimicrobial activity, and in vitro cytotoxicity of novel sulphanilamide condensed 1,2,3,4-tetrahydropyrimidines [95].…”

Section: Beta-ketoamides and Beta-ketosulfonamidesmentioning

confidence: 99%

“…The resulting products 69 were evaluated for their antitubercular activity to determine MIC against Mycobacterium tuberculosis (H37Rv) [96]. More recently, these authors published the synthesis, antimicrobial activity, and in vitro cytotoxicity of novel sulphanilamide condensed 1,2,3,4-tetrahydropyrimidines [95].…”

Section: Beta-ketoamides and Beta-ketosulfonamidesmentioning

confidence: 99%

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Synthesis of 3,4-Dihydropyrimidin(thio)one Containing Scaffold: Biginelli-like Reactions

et al. 2022

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The interest in 3,4-dihydropyrimidine-2(1H)-(thio)ones is increasing every day, mainly due to their paramount biological relevance. The Biginelli reaction is the classical approach to reaching these scaffolds, although the product diversity suffers from some limitations. In order to overcome these restrictions, two main approaches have been devised. The first one involves the modification of the conventional components of the Biginelli reaction and the second one refers to the postmodification of the Biginelli products. Both strategies have been extensively revised in this manuscript. Regarding the first one, initially, the modification of one of the components was covered. Although examples of modifications of the three of them were described, by far the modification of the keto ester counterpart was the most popular approach, and a wide variety of different enolizable carbonylic compounds were used; moreover, changes in two or the three components were also described, broadening the substitution of the final dihydropyrimidines. Together with these modifications, the use of Biginelli adducts as a starting point for further modification was also a very useful strategy to decorate the final heterocyclic structure.

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“…. Los resultados muestran buenos rendimientos hacia el producto de interés, además, el uso de microondas acota los tiempos de reacción a 10 min, en comparación con el convencional de 4 horas, sin embargo se requieren de sustancias auxiliares para la extracción del producto [118] Figura 35. Síntesis de uracilos bajo irradiación por microondas.…”

Section: Síntesis De Uracilosunclassified

Sólidos básicos como catalizadores en la síntesis ecoeficiente de heterociclos potencialmente activos

Vargas¹,

Rocío²

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En los últimos años, el interés por realizar una Química más sostenible y favorable con el ambiente, ha aumentado drásticamente. La contaminación ambiental, el calentamiento global y el esfuerzo por mejorar la protección de cultivos, productos y medicamentos, han causado daños no deseables al planeta y a la salud humana. En este contexto, la Química Verde surge como una disciplina que se esfuerza por lograr la sostenibilidad, desarrollando procesos químicos benignos con la humanidad y con el medio ambiente. Esta nueva forma de hacer Química se aplica en todo el ciclo de un proceso de síntesis, y tiene como fin, eliminar o reducir el consumo energético, el uso de sustancias peligrosas y realizar procesos más seguros. Por lo tanto, la aplicación de estrategias ingeniosas para sintetizar moléculas altamente sustituidas, combinando diversidad molecular con eco-compatibilidad, ha sido uno de los objetivos de muchas investigaciones, por lo que, el diseño de reacciones que transformen sustratos simples y de fácil disposición en estructuras complejas, es uno de los desafíos actuales en la Química Orgánica. Las reacciones multicomponente (RMC) son una herramienta para la síntesis de compuestos biológicamente activos, que resultan de interés para el desarrollo de nuevos fármacos. Estas reacciones se llevan a cabo en un solo paso e involucran el uso de tres o más reactivos que forman un único producto, que contiene a la mayoría de los átomos de los materiales de partida, lo que conlleva a que estos procedimientos presenten alta economía atómica. Además, permiten trabajar con numerosas variaciones estructurales, minimizan tiempos de reacción y en algunos procesos evitan el uso de sustancias auxiliares, permitiendo desarrollar reacciones libres de solvente. Estas ventajas se encaminan dentro de los principios de la Química Verde, por lo que cada día presentan un mayor interés en la Química moderna. Dentro de los principios de la Química Verde se menciona el uso de la catálisis para el desarrollo de tecnologías más limpias y benignas con el medio ambiente, y se hace principal énfasis en el uso de los catalizadores heterogéneos. La sustitución de bases en medios homogéneos por sólidos básicos como alúminas, zeolitas, arcillas y materiales mesoporosos modificados, son una alternativa para reemplazar las metodologías convencionales. Teniendo en cuenta que los sólidos básicos se pueden clasificar como sólidos con propiedades básicas intrínsecas y con propiedades básicas incorporadas, en este trabajo se estudiaron materiales tipo hidrotalcita y polioxometalatos tipo decaniobato, como sólidos con propiedades intrínsecas y se estudió, además, la incorporación de carbonato de calcio en un material mesoporoso tipo MCM-41 como sólido con propiedades básicas incorporadas De esta manera, en este trabajo se plantea como objetivo general sintetizar materiales básicos tipo hidrotalcitas, decaniobato y CaCO3 soportado en un material mesoporoso tipo MCM-41 (Ca-MCM-41), evaluar su activad catalítica en la síntesis multicomponente de tres familias de compuestos de heterociclos, con potencial actividad biológica, aplicando metodologías bajo los principios de la Química Verde. Se plantearon como objetivos específicos, caracterizar los materiales sintetizados por diversas técnicas; estudiar y optimizar las reacciones multicomponentes de la síntesis de 4H-piranos, de derivados de los cromenos y de derivados de uracilos con el catalizador más activo

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Antimicrobial and in vitro cytotoxicity of novel sulphanilamide condensed 1,2,3,4-tetrahydropyrimidines

Cited by 10 publications

References 21 publications

Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe₃O₄@SiO₂ Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii

Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe₃O₄@SiO₂ Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii

Synthesis of 3,4-Dihydropyrimidin(thio)one Containing Scaffold: Biginelli-like Reactions

Sólidos básicos como catalizadores en la síntesis ecoeficiente de heterociclos potencialmente activos

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Antimicrobial and in vitro cytotoxicity of novel sulphanilamide condensed 1,2,3,4-tetrahydropyrimidines

Cited by 10 publications

References 21 publications

Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe3O4@SiO2 Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii

Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe3O4@SiO2 Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii

Synthesis of 3,4-Dihydropyrimidin(thio)one Containing Scaffold: Biginelli-like Reactions

Sólidos básicos como catalizadores en la síntesis ecoeficiente de heterociclos potencialmente activos

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Product

Resources

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Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe₃O₄@SiO₂ Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii

Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe₃O₄@SiO₂ Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii