Literature DB >> 21996518

Rational design of 2-pyrrolinones as inhibitors of HIV-1 integrase.

Kaiqing Ma1, Penghui Wang, Wei Fu, Xiaolong Wan, Lu Zhou, Yong Chu, Deyong Ye.   

Abstract

HIV-1 integrase is an essential enzyme for viral replication and a validated target for the development of drugs against AIDS. With an aim to discover new potent inhibitors of HIV-1 integrase, we developed a pharmacophore model based on reported inhibitors embodying structural diversity. Eight compounds of 2-pyrrolinones fitting all the features of the pharmacophore query were found through the screening of an in-house database. These candidates were successfully synthesized, and three of them showed strand transfer inhibitory activity, in which, one compound showed antiviral activity. Further mapping analysis and docking studies affirmed these results.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21996518     DOI： 10.1016/j.bmcl.2011.09.054

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


  9 in total

1.  Synthesis of functionalized dihydro-2-oxopyrroles using graphene oxide as heterogeneous catalyst.

Authors:  Masoumeh Bavadi; Khodabakhsh Niknam
Journal:  Mol Divers       Date:  2018-01-09       Impact factor: 2.943

2.  Stereoselective, Multicomponent Approach to Quaternary Substituted Hydroindole Scaffolds.

Authors:  Nicholas P Massaro; Joshua G Pierce
Journal:  Org Lett       Date:  2020-06-17       Impact factor: 6.005

3.  Exploring the Synthetic Potential of γ-Lactam Derivatives Obtained from a Multicomponent Reaction-Applications as Antiproliferative Agents.

Authors:  Adrián López-Francés; Xabier Del Corte; Zuriñe Serna-Burgos; Edorta Martínez de Marigorta; Francisco Palacios; Javier Vicario
Journal:  Molecules       Date:  2022-06-05       Impact factor: 4.927

4.  Multicomponent Synthesis of Unsaturated γ-Lactam Derivatives. Applications as Antiproliferative Agents through the Bioisosterism Approach: Carbonyl vs. Phosphoryl Group.

Authors:  Xabier Del Corte; Adrián López-Francés; Ilia Villate-Beitia; Myriam Sainz-Ramos; Edorta Martínez de Marigorta; Francisco Palacios; Concepción Alonso; Jesús M de Los Santos; José Luis Pedraz; Javier Vicario
Journal:  Pharmaceuticals (Basel)       Date:  2022-04-22

5.  Aldol reactions in multicomponent reaction based domino pathways: a multipurpose enabling tool in heterocyclic chemistry.

Authors:  Zhigang Xu; Fabio De Moliner; Alexandra P Cappelli; Christopher Hulme
Journal:  Org Lett       Date:  2013-05-29       Impact factor: 6.005

6.  A Brønsted Acid-Catalyzed Multicomponent Reaction for the Synthesis of Highly Functionalized γ-Lactam Derivatives.

Authors:  Xabier Del Corte; Edorta Martinez de Marigorta; Francisco Palacios; Javier Vicario
Journal:  Molecules       Date:  2019-08-14       Impact factor: 4.411

7.  Amination of 5-Spiro-Substituted 3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones.

Authors:  Ekaterina E Khramtsova; Ekaterina A Lystsova; Evgeniya V Khokhlova; Maksim V Dmitriev; Andrey N Maslivets
Journal:  Molecules       Date:  2021-11-26       Impact factor: 4.411

8.  Synthesis and evaluation of the antioxidant activity of 3-pyrroline-2-ones: experimental and theoretical insights.

Authors:  Nguyen Tran Nguyen; Vo Viet Dai; Adam Mechler; Nguyen Thi Hoa; Quan V Vo
Journal:  RSC Adv       Date:  2022-08-30       Impact factor: 4.036

9.  Structural-Functional Analysis of 2,1,3-Benzoxadiazoles and Their N-oxides As HIV-1 Integrase Inhibitors.

Authors:  S P Korolev; O V Kondrashina; D S Druzhilovsky; A M Starosotnikov; M D Dutov; M A Bastrakov; I L Dalinger; D A Filimonov; S A Shevelev; V V Poroikov; Y Y Agapkina; M B Gottikh
Journal:  Acta Naturae       Date:  2013-01       Impact factor: 1.845
  9 in total

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