1ackground: An efficient one-pot biocatalysed ultrasound assisted synthesis of dihydropyrimidinones/thiones has been developed under solvent free conditions. Materials and Methods: The use of biodegradable, non toxic, agar-powder as a catalyst provide advantages like high yield, simple operation, mild reaction condition with short reaction time. 1,2,3,4-tetrahydropyrimidine-2-ones/thiones formed were characterized by mass and 1H NMR spectroscopy. Results: The dihydropyrimidinones substituted with electron donating groups like fluorine, hydroxy along with thienyl groups exhibited good antibacterial activity. The compounds exhibited favorable binding interactions with mycobacterium target protein H37Rv. Conclusion: 4-methoxy substituted dihydropyrimidinones derivative showed significant antituberculosis activity.

Biopolymer catalysed synthesis of 6-methyl-4-phenylcarbamoyl-1, 2, 3, 4-tetrahydropyrimidine-2-ones and evaluation of their anti-bacterial and anti-tubercular activities / V. Chabukswar, D. Pawar, K. Handore, S. Shisodia, B. Diwate, P. Adhav, S. Jagdale, A. Chabukswar, V. Gaikwad, S. Dallavalle. - In: CURRENT BIOACTIVE COMPOUNDS. - ISSN 1573-4072. - 15:4(2019), pp. 408-414. [10.2174/1573407214666180503114844]

Biopolymer catalysed synthesis of 6-methyl-4-phenylcarbamoyl-1, 2, 3, 4-tetrahydropyrimidine-2-ones and evaluation of their anti-bacterial and anti-tubercular activities

S. Dallavalle
Ultimo
2019

Abstract

1ackground: An efficient one-pot biocatalysed ultrasound assisted synthesis of dihydropyrimidinones/thiones has been developed under solvent free conditions. Materials and Methods: The use of biodegradable, non toxic, agar-powder as a catalyst provide advantages like high yield, simple operation, mild reaction condition with short reaction time. 1,2,3,4-tetrahydropyrimidine-2-ones/thiones formed were characterized by mass and 1H NMR spectroscopy. Results: The dihydropyrimidinones substituted with electron donating groups like fluorine, hydroxy along with thienyl groups exhibited good antibacterial activity. The compounds exhibited favorable binding interactions with mycobacterium target protein H37Rv. Conclusion: 4-methoxy substituted dihydropyrimidinones derivative showed significant antituberculosis activity.
Anti tubercular activity; Antibacterial activity; Biocatalysed synthesis; Carambine; Green chemistry; Solvent free
Settore CHIM/08 - Chimica Farmaceutica
Settore CHIM/06 - Chimica Organica
2019
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/711083
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