Literature DB >> 16677813

Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase.

Orla K Mc Carthy1, Alessandro Schipani, Alex Musso Buendía, Luis M Ruiz-Perez, Marcel Kaiser, Reto Brun, Dolores González Pacanowska, Ian H Gilbert.   

Abstract

Potential inhibitors of the Trypanosoma cruzi dUTP nucleotidohydrolase were docked into the enzyme using the program FlexX. Compounds that docked selectively were then selected and synthesized using solid phase methodology, giving rise to a novel library of amino acid uracil acetamide compounds which were evaluated for enzyme inhibition and anti-parasitic activity.

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Year:  2006        PMID: 16677813     DOI: 10.1016/j.bmcl.2006.04.027

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


  5 in total

Review 1.  Pyrimidine metabolism in schistosomes: A comparison with other parasites and the search for potential chemotherapeutic targets.

Authors:  Mahmoud H El Kouni
Journal:  Comp Biochem Physiol B Biochem Mol Biol       Date:  2017-07-21       Impact factor: 2.231

2.  Quantitative analysis of hydrogen and chalcogen bonds in two pyrimidine-5-carbonitrile derivatives, potential DHFR inhibitors: an integrated crystallographic and theoretical study.

Authors:  Lamya H Al-Wahaibi; Kushumita Chakraborty; Nora H Al-Shaalan; Mohamed Yehya Annavi Syed Majeed; Olivier Blacque; Aamal A Al-Mutairi; Ali A El-Emam; M Judith Percino; Subbiah Thamotharan
Journal:  RSC Adv       Date:  2020-10-06       Impact factor: 4.036

Review 3.  Fresh insights into the pyrimidine metabolism in the trypanosomatids.

Authors:  Kartikeya Tiwari; Vikash Kumar Dubey
Journal:  Parasit Vectors       Date:  2018-02-08       Impact factor: 3.876

4.  Structural Insights of Three 2,4-Disubstituted Dihydropyrimidine-5-carbonitriles as Potential Dihydrofolate Reductase Inhibitors.

Authors:  Lamya H Al-Wahaibi; Althaf Shaik; Mohammed A Elmorsy; Mohammed S M Abdelbaky; Santiago Garcia-Granda; Subbiah Thamotharan; Vijay Thiruvenkatam; Ali A El-Emam
Journal:  Molecules       Date:  2021-05-29       Impact factor: 4.411

5.  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
  5 in total

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