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Tale R.H.,Swami Ramanand Teerth Marathwada University | Rodge A.H.,Swami Ramanand Teerth Marathwada University | Hatnapure G.D.,Udaygiri Mahavidayla | Keche A.P.,Udaygiri Mahavidayla
Bioorganic and Medicinal Chemistry Letters | Year: 2011

A series of novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of biological interest were prepared by sequential Bigineli's reaction, reduction followed by reaction of resulting amines with different arylisocynates. All the synthesized (1-23) compounds were screened against the pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological activity evaluation study reveled that among all the compounds screened, compounds 12 and 17 found to have promising anti-inflammatory activity (68-62% TNF-α and 92-86% IL-6 inhibitory activity at 10 μM). Interestingly compounds 3, 4, 5, 6, 15, 22 and 23 revealed promising antimicrobial activity at MIC of 10-30 μg/mL against selected pathogenic bacteria and fungi. © 2011 Elsevier Ltd. All rights reserved. Source


Tale R.H.,Swami Ramanand Teerth Marathwada University | Rodge A.H.,Swami Ramanand Teerth Marathwada University | Hatnapure G.D.,Udaygiri Mahavidayla | Keche A.P.,Udaygiri Mahavidayla | And 2 more authors.
Medicinal Chemistry Research | Year: 2012

A series of novel thiourea analogs of 3,4-dihydropyrimidin-2(1-H)-one derivatives of biological interest were prepared by sequential Bigineli's reaction, reduction followed by reaction of resulting amine with different arylisothiocynates. All the synthesized compounds (1-23) were screened against the proinflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological data revealed that among all the compounds screened, compounds 6, 10, 11, 12, 13, 14, 17, and 20 found to have promising anti-inflammatory activity (42-78% TNF-α and 54-96% IL-6 inhibitory activity at 10 μM). Remarkably, compounds 3, 4, 5, 6, 15, 22, and 23 revealed promising antimicrobial activity at minimum inhibitory concentration of 10-40 μg/ml against selected pathogenic bacteria and fungi. © 2012 Springer Science+Business Media, LLC. Source


Keche A.P.,Udaygiri Mahavidayla | Kamble V.M.,Udaygiri Mahavidayla | Kamble V.M.,The Institute of Science Bombay
Arabian Journal of Chemistry | Year: 2014

A variety of novel 2-methylquinazolin-4(3H)-one derivatives (1-. 29) bearing urea, thiourea and sulphonamide functionalities at position 3 of biological interest have been synthesized and screened for their anti-inflammatory (TNF-α and IL-6) and antimicrobial activities (antibacterial and antifungal). “Biological evaluation study revealed that the compounds 3, 4, 6, 9, 16 and 18 were found to have promising anti-inflammatory activity (up to 62-84% TNF-α and 73-92% IL-6 inhibitory activity) at concentration of 10. μM with reference to standard dexamethasone (75% TNF-α and 84% IL-6 inhibitory activities at 1. μM) and 7, 10, 12, 23, 25 and 28 have antimicrobial activity at MIC of 10-30. μg/mL against selected pathogenic bacteria and fungi.“. © 2014. Source

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