10.4172/jaa.1000036

P, Naga Anusha

doi:10.4172/jaa.1000036

J Antivir Antiretrovir

2011

DOI: 10.4172/jaa.1000036

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10.4172/jaa.1000036

Naga Anusha P¹

Abstract: Since 1981 when first AIDS cases were identified in United States followed by Africa there has been growing understanding in the trajectory of HIV/AIDS across the world. The disease has caused unpredicted suffering, loss of life and disruption of family, social and economic abilities. Many therapies were introduced to treat AIDS. Those therapies have provided many insights in development of vaccine to decrease the pathogenecity and virulence of HIV. Here I will be discussing the strategies involved in the deve… Show more

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Cited by 2 publications

References 71 publications

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Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4′-Ethynyl-2-fluoro-2′-deoxyadenosine)

Alexandre¹,

Rahali²,

Rahali³

et al. 2018

J. Med. Chem.

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MK-8591 (4′-ethynyl-2-fluoro-2′-deoxyadenosine) is a novel nucleoside analog that displays a differentiated mechanism of action as a nucleoside reverse transcriptase translocation inhibitor (NRTTI) compared to approved NRTIs. Herein, we describe our recent efforts to explore the impact of structural changes to the properties of MK-8591 through the synthesis and antiviral evaluation of carbocyclic derivatives. Synthesized analogs were evaluated for their antiviral activity, and the corresponding triphosphates were synthesized and evaluated in a biochemical assay. 4′-Ethynyl-G derivative (±)-29 displayed a promising IC 50 of 33 nM in a hPBMC cell-based antiviral assay, and its triphosphate (TP), (±)-29-TP, displayed an IC 50 of 324 nM in a biochemical RT-polymerase assay. Improved TP anabolite delivery resulting in improved in vitro potency was achieved by preparing the corresponding phosphoramidate prodrug of single enantiomer 29b, with 6-ethoxy G derivative 34b displaying a significantly improved IC 50 of 3.0 nM, paving the way for new directions for this novel class of nucleoside analogs.

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Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4′-Ethynyl-2-fluoro-2′-deoxyadenosine)

Alexandre¹,

Rahali²,

Rahali³

et al. 2018

J. Med. Chem.

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show abstract

Incidence of Diabetes and its Control Measures in AIDS Patients

A¹,

Soumya²

2012

J Diabetes Metab

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HIV and diabetes are both chronic diseases that significantly affect the human lifestyle and their quality of living. When these two diseases coexist, their treatment would be overwhelming for patients. Highly active antiretroviral therapy (HAART) became the standard of care in HIV infection. As the treatment for HIV has been developed and the access to therapy has been improved, the incidence of HIV-associated diabetes began to grow. Diabetes can be an important consequence of HAART. This review describes various metabolic complications such as AIDS-related insulin resistance, Glucose Intolerance and Hyperglycemia after HAART and also gives a brief account on the control measures.

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10.4172/jaa.1000036

Cited by 2 publications

References 71 publications

Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4′-Ethynyl-2-fluoro-2′-deoxyadenosine)

Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4′-Ethynyl-2-fluoro-2′-deoxyadenosine)

Incidence of Diabetes and its Control Measures in AIDS Patients

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