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image of Design, In Silico, and In vitro Evaluation of Polymer-Based Drug Conjugates Incorporated with Derivative of Cinnamic Acid, Zidovudine, and 
4-Aminosalicylic Acid against Pseudo-HIV-1

Abstract

Background

The incorporation of anti-HIV drugs into polymer to form polymer-drug conjugates has been reported to result in improved therapeutic activity. Zidovudine, an anti-HIV drug, was explored alone and in combination with known drug molecules using polyamidoamine-based carriers.

Objective

Polymer-drug conjugates incorporated with zidovudine, cinnamic acid, and 4-aminosalicylic acid were prepared and evaluated for their potential efficacy against pseudo-HIV-1.

Methods

Aqueous Michael addition polymerization reaction was employed to prepare the conjugates. The conjugates were incorporated with zidovudine, cinnamic acid, and 4-aminosalicylic acid. They were characterized by SEM/EDX, XRD, FTIR, NMR, LC-MS, particle size analysis, analysis, computational studies, and toxicity predictions.

Results

The conjugates displayed spherically shaped morphology. The findings showed that polymer-drug conjugates, T15 and T16, with a single drug were effective against pseudo-HIV-1 at high concentrations of 111.11 and 333.33 µg/mL, respectively. Molecular docking studies supported the results. Additionally, SwissADME, ProTox-II, and GUSAR (General Unrestricted Structure-Activity Relationships) analyses revealed that these compounds have promising antiviral potential.

Conclusion

The prepared polymer-drug conjugates with a single drug showed promising effects against the Pseudo-HIV-1, and the conjugates displayed features that make them potential anti-HIV therapeutics that require further studies.

© 2024 Bentham Science Publishers
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2024-11-22

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Design, In Silico, and In vitro Evaluation of Polymer-Based Drug Conjugates Incorporated with Derivative of Cinnamic Acid, Zidovudine, and 
4-Aminosalicylic Acid against Pseudo-HIV-1
Bentham Science Publishers ; https://doi.org/10.2174/011570162X334858241008071722
/content/journals/chr/10.2174/011570162X334858241008071722
/content/journals/chr/10.2174/011570162X334858241008071722
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  • Article Type:     Research Article
Keywords: polymer-drug conjugates ; 4-aminosalicylic acid ; cinnamic acid ; zidovudine ; HIV ; molecular docking
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