Literature DB >> 25529736

Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors.

B Narasimhulu Naidu1, Margaret E Sorenson2, Manoj Patel2, Yasutsugu Ueda2, Jacques Banville2, Francis Beaulieu2, Sagarika Bollini3, Ira B Dicker3, Helen Higley3, Zeyu Lin3, Lori Pajor4, Dawn D Parker4, Brian J Terry3, Ming Zheng4, Alain Martel2, Nicholas A Meanwell2, Mark Krystal3, Michael A Walker2.   

Abstract

Integration of viral DNA into the host cell genome is an obligatory process for successful replication of HIV-1. Integrase catalyzes the insertion of viral DNA into the target DNA and is a validated target for drug discovery. Herein, we report the synthesis, antiviral activity and pharmacokinetic profiles of several C2-carbon-linked heterocyclic pyrimidinone-4-carboxamides that inhibit the strand transfer step of the integration process.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  HIV-1; Inhibitor; Integrase; Pyrimidine-4-carboxamide; Strand transfer

Mesh:

Substances:

Year:  2014        PMID: 25529736     DOI: 10.1016/j.bmcl.2014.11.060

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


  4 in total

1.  A new class of half-sandwich ruthenium complexes containing Biginelli hybrids: anticancer and anti-SARS-CoV-2 activities.

Authors:  Nenad Janković; Emilija Milović; Jelena Đorović Jovanović; Zoran Marković; Milan Vraneš; Tatjana Stanojković; Ivana Matić; Marija Đorđić Crnogorac; Olivera Klisurić; Miroslav Cvetinov; Syed Nasir Abbas Bukhari
Journal:  Chem Biol Interact       Date:  2022-06-22       Impact factor: 5.168

Review 2.  Progress in HIV-1 Integrase Inhibitors: A Review of their Chemical Structure Diversity.

Authors:  Zahra Hajimahdi; Afshin Zarghi
Journal:  Iran J Pharm Res       Date:  2016       Impact factor: 1.696

Review 3.  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

4.  One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues.

Authors:  Jessica Bais; Fabio Benedetti; Federico Berti; Iole Cerminara; Sara Drioli; Maria Funicello; Giorgia Regini; Mattia Vidali; Fulvia Felluga
Journal:  Molecules       Date:  2020-09-10       Impact factor: 4.411

  4 in total

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