Literature DB >> 10386920

Uridine phosphorylase inhibitors: chemical modification of benzyloxybenzyl-barbituric acid and its effects on urdpase inhibition.

D J Guerin1, D Mazeas, M S Musale, F N Naguib, O N Al Safarjalani, M H el Kouni, R P Panzica.   

Abstract

5-(o-Benzyloxy)benzylbarbituric acid (6) and 5-(p-benzyloxy)benzylbarbituric acid (7) were prepared and their inhibitory activities compared to 5-(m-benzyloxy)-benzylbarbituric acid (BBB) a known, potent inhibitor of uridine phosphorylase (UrdPase). Compounds 6 and 7 were 18-fold and 51-fold less active, respectively, than BBB in inhibiting UrdPase. These data provide solid evidence that the 5-benzylbarbituric acids possessing meta substituents are the most active inhibitors. In addition, 2-thioBBB (11) was synthesized and it was shown to be as active an inhibitor as BBB.

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Year:  1999        PMID： 10386920     DOI： 10.1016/s0960-894x(99)00238-3

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


  7 in total

1.  Design and synthesis of novel thiobarbituric acid derivatives targeting both wild-type and BRAF-mutated melanoma cells.

Authors:  Srinivasa Rao Ramisetti; Manoj K Pandey; Sang Y Lee; Deepkamal Karelia; Satya Narayan; Shantu Amin; Arun K Sharma
Journal:  Eur J Med Chem       Date:  2017-11-04       Impact factor: 6.514

2.  Synthesis of 5-alkylated barbituric acids and 3-alkylated indoles via microwave-assisted three-component reactions in solvent-free conditions using Hantzsch 1,4-dihydropyridines as reducing agents.

Authors:  Biswajita Baruah; P Seetham Naidu; Pallabi Borah; Pulak J Bhuyan
Journal:  Mol Divers       Date:  2012-05       Impact factor: 2.943

3.  5-((1-Aroyl-1H-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-diones as potential anticancer agents with anti-inflammatory properties.

Authors:  Narsimha Reddy Penthala; Purushothama Rao Ponugoti; Vinod Kasam; Peter A Crooks
Journal:  Bioorg Med Chem Lett       Date:  2012-12-22       Impact factor: 2.823

4.  Tandem aldol-Michael reactions in aqueous diethylamine medium: a greener and efficient approach to bis-pyrimidine derivatives.

Authors:  Abdullah M Al-Majid; Assem Barakat; Hany J Al-Najjar; Yahia N Mabkhot; Hazem A Ghabbour; Hoong-Kun Fun
Journal:  Int J Mol Sci       Date:  2013-12-05       Impact factor: 5.923

5.  Tandem Aldol-Michael reactions in aqueous diethylamine medium: a greener and efficient approach to dimedone-barbituric acid derivatives.

Authors:  Assem Barakat; Abdullah Mohammed Al-Majid; Abdulaziz Moshabab Al-Ghamdi; Yahia Nasser Mabkhot; Mohammed Rafiq Hussain Siddiqui; Hazem A Ghabbour; Hoong-Kun Fun
Journal:  Chem Cent J       Date:  2014-02-01       Impact factor: 4.215

6.  Synthesis, antifungal activity, and QSAR studies of 1,6-dihydropyrimidine derivatives.

Authors:  Chirag Rami; Laxmanbhai Patel; Chhaganbhai N Patel; Jayshree P Parmar
Journal:  J Pharm Bioallied Sci       Date:  2013-10

7.  Synthesis and characterisation of thiobarbituric acid enamine derivatives, and evaluation of their α-glucosidase inhibitory and anti-glycation activity.

Authors:  M Ali; Assem Barakat; Ayman El-Faham; Hessa H Al-Rasheed; Kholoud Dahlous; Abdullah Mohammed Al-Majid; Anamika Sharma; Sammer Yousuf; Mehar Sanam; Zaheer Ul-Haq; M Iqbal Choudhary; Beatriz G de la Torre; Fernando Albericio
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
  7 in total

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