Literature DB >> 21737269

The novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of N-aryl urea: synthesis, anti-inflammatory, antibacterial and antifungal activity evaluation.

Rajesh H Tale1, Atish H Rodge, Girish D Hatnapure, Ashish P Keche.   

Abstract

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21737269     DOI: 10.1016/j.bmcl.2011.03.062

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Development of energetic pharmacophore for the designing of 1,2,3,4-tetrahydropyrimidine derivatives as selective cyclooxygenase-2 inhibitors.

Authors:  Deepak Lokwani; Reecha Shah; Santosh Mokale; Padma Shastry; Devanand Shinde
Journal:  J Comput Aided Mol Des       Date:  2012-01-05       Impact factor: 3.686

Review 2.  Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review.

Authors:  Ramandeep Kaur; Sandeep Chaudhary; Kapil Kumar; Manish K Gupta; Ravindra K Rawal
Journal:  Eur J Med Chem       Date:  2017-03-19       Impact factor: 6.514

3.  Synthesis and In Vitro Antiproliferative Activity of New 1-Phenyl-3-(4-(pyridin-3-yl)phenyl)urea Scaffold-Based Compounds.

Authors:  Mohammad M Al-Sanea; Mohammed Safwan Ali Khan; Ahmed Z Abdelazem; So Ha Lee; Pooi Ling Mok; Mohammed Gamal; Mohamed E Shaker; Muhammad Afzal; Bahaa G M Youssif; Nesreen Nabil Omar
Journal:  Molecules       Date:  2018-01-31       Impact factor: 4.411

  3 in total

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