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

doi:10.1016/J.BMC.2015.10.039

Paper

DOI: 10.1016/J.BMC.2015.10.039

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

Published Dec 15, 2015 · Meloddy H. Manyeruke, Temitope O. Olomola, Swarup Majumder

Bioorganic & medicinal chemistry

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Abstract

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3-hydroxy-3-phenylpropanoate ester-AZT conjugates show potential as dual-action HIV-1 Integrase and Reverse Transcriptase inhibitors, with promising activity and toxicity compared to their cinnamate ester analogues.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Synthesis of cinnamate ester–AZT conjugates as potential dual-action HIV-1 integrase and reverse transcriptase inhibitors

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Citations

DOI: 10.1016/j.ejmech.2022.114981

Structure based design and evaluation of benzoheterocycle derivatives as potential dual HIV-1 protease and reverse transcriptase inhibitors.

Benzoheterocycle derivatives show potential as dual HIV-1 protease and reverse transcriptase inhibitors, with inhibitor 10f showing a 1: 2 ratio between the enzymes, showing similar potency against both wild-type and drug-resistant mutants.

2023·3citations·Mei Zhu et al.·European journal of medicinal chemistry

European journal of medicinal chemistry

DOI: 10.3390/ph15091092

Hybrid Molecules as Potential Drugs for the Treatment of HIV: Design and Applications

Hybrid molecules targeting integrase, reverse transcriptase, and protease proteins show potential for higher efficacy and lower toxicity than their parent molecules in anti-HIV drug discovery.

2022·4citations·Wissal Liman et al.·Pharmaceuticals

Pharmaceuticals

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HIV-1 Reverse Transcriptase/Integrase Dual Inhibitors: A Review of Recent Advances and Structure-activity Relationship Studies

RT-IN dual inhibitors show potential as a promising approach to combat HIV resistance, offering a more effective and efficient treatment option than complex multidrug programs.

2021·5citations·Mohammad Mahboubi-Rabbani et al.·Iranian Journal of Pharmaceutical Research : IJPR

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DOI: 10.1016/J.TET.2021.132252

Efficient access to 3′-deoxy-3′-(4-substituted-1,2,3-triazol-1-yl)-thymidine derivatives via ligand-promoted CuAAC

This study presents a rapid and efficient method for synthesis of 3′-deoxy-3′-(4-substituted-1,2,3-triazol-1-yl)-thymidine derivatives using copper(I) in a one-pot reaction, yielding 71-100% pure compounds

2021·1citation·Laura Garlatti et al.·Tetrahedron

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Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.

Cinnamic and phenylpropionic amide derivatives show potential as novel dual inhibitors of HIV-1 protease and reverse transcriptase, improving their inhibitory activity and reducing disparity between PR and RT inhibition.

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European journal of medicinal chemistry