Literature DB >> 26775541

Synthesis and evaluation of 3-hydroxy-3-phenylpropanoate ester–AZT conjugates as potential dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors.

Meloddy H Manyeruke, Temitope O Olomola, Swarup Majumder, Shaakira Abrahams, Michelle Isaacs, Nicodemus Mautsa, Salerwe Mosebi, Dumisani Mnkandhla, Raymond Hewer, Heinrich C Hoppe, Rosalyn Klein, Perry T Kaye.   

Abstract

Novel 3-hydroxy-3-phenylpropanoate ester-azidothymidine (AZT) conjugates have been prepared using Baylis-Hillman methodology, and their potential as dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors has been explored using enzyme inhibition and computer modelling techniques; their activity and HeLa cell toxicity have been compared with those of their cinnamate ester analogues.

Entities:  

Mesh:

Substances:

Year:  2015        PMID: 26775541     DOI: 10.1016/j.bmc.2015.10.039

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  1 in total

1.  Synthesis and Evaluation of Baylis-Hillman Reaction Derived Imidazole and Triazole Cinnamates as Antifungal Agents.

Authors:  Grady L Nelson; Michael J Williams; Shirisha Jonnalagadda; Mohammad A Alam; Gautam Mereddy; Joseph L Johnson; Sravan K Jonnalagadda
Journal:  Int J Med Chem       Date:  2018-10-16
  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.