Literature DB >> 28160944

Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Titiksh L Devale1, Jignesh Parikh2, Pankaj Miniyar3, Pankaj Sharma4, Birendra Shrivastava5, Prashant Murumkar6.   

Abstract

A novel series of substituted N-(2-(2,3-dioxoindolin-1-yl)acetyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide was designed, synthesized and evaluated for in vitro Reverse Transcriptase (RT) inhibitory activity. This series is a combination of peculiar structural features from leading scaffolds of [(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) and oxyindole. In vitro screening led to identification of two hybrids (9c and 9d) possessing higher RT inhibitory activity than the standard rilpivirine. Docking study was performed to study the binding orientations of synthesized hybrids towards RT enzyme.
Copyright © 2017 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  G-score; Hybrid approach; Microwave assisted synthesis; Molecular docking; NNRTI

Mesh：

Substances：

Year:  2017        PMID： 28160944     DOI： 10.1016/j.bioorg.2017.01.006

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN： 0045-2068            Impact factor:   5.275


  7 in total

1.  1H-1,2,3-Triazole Tethered Nitroimidazole-Isatin Conjugates: Synthesis, Docking, and Anti-Proliferative Evaluation against Breast Cancer.

Authors:  Sumit Kumar; Sourav Taru Saha; Liang Gu; Gabriella Palma; Shanen Perumal; Ashona Singh-Pillay; Parvesh Singh; Amit Anand; Mandeep Kaur; Vipan Kumar
Journal:  ACS Omega       Date:  2018-09-27

2.  Azide-Alkyne Cycloaddition En Route to 1H-1,2,3-Triazole-Tethered Isatin-Ferrocene, Ferrocenylmethoxy-Isatin, and Isatin-Ferrocenylchalcone Conjugates: Synthesis and Antiproliferative Evaluation.

Authors:  Amandeep Singh; Sourav Taru Saha; Shanen Perumal; Mandeep Kaur; Vipan Kumar
Journal:  ACS Omega       Date:  2018-01-30

Review 3.  Molecular Docking Studies of HIV-1 Resistance to Reverse Transcriptase Inhibitors: Mini-Review.

Authors:  Olga Tarasova; Vladimir Poroikov; Alexander Veselovsky
Journal:  Molecules       Date:  2018-05-21       Impact factor: 4.411

4.  Discovery, synthesis, and optimization of an N-alkoxy indolylacetamide against HIV-1 carrying NNRTI-resistant mutations from the Isatis indigotica root.

Authors:  Chengbo Xu; Yijing Xin; Minghua Chen; Mingyu Ba; Qinglan Guo; Chenggen Zhu; Ying Guo; Jiangong Shi
Journal:  Eur J Med Chem       Date:  2020-01-22       Impact factor: 6.514

Review 5.  Isatin derivatives as broad-spectrum antiviral agents: the current landscape.

Authors:  Tilal Elsaman; Malik Suliman Mohamed; Eyman Mohamed Eltayib; Hatem A Abdel-Aziz; Abualgasim Elgaili Abdalla; Muhammad Usman Munir; Magdi Awadalla Mohamed
Journal:  Med Chem Res       Date:  2022-01-13       Impact factor: 2.351

6.  Rational structural modification of the isatin scaffold to develop new and potent antimicrobial agents targeting bacterial peptidoglycan glycosyltransferase.

Authors:  Yong Wang; Zhiguang Liang; Yuanyuan Zheng; Alan Siu-Lun Leung; Siu-Cheong Yan; Pui-Kin So; Yun-Chung Leung; Wing-Leung Wong; Kwok-Yin Wong
Journal:  RSC Adv       Date:  2021-05-19       Impact factor: 4.036

Review 7.  Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery.

Authors:  Rameshwar S Cheke; Vaishali M Patil; Sandip D Firke; Jaya P Ambhore; Iqrar A Ansari; Harun M Patel; Sachin D Shinde; Visweswara Rao Pasupuleti; Md Imtaiyaz Hassan; Mohd Adnan; Adel Kadri; Mejdi Snoussi
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-22
  7 in total

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