scholarly journals Anti-HIV Drug Discovery, Development and Synthesis of Delavirdine: Review Article

2019 ◽  
pp. 1-16 ◽  
Author(s):  
Wollela Behja ◽  
Mudin Jemal
Keyword(s):  
Life Cycle ◽  
Reverse Transcriptase ◽  
Genetic Material ◽  
Amino Acid Sequences ◽  
Surface Binding ◽  
Reverse Transcriptase Inhibitors ◽  
Fusion Inhibitors ◽  
Critical Components ◽  
Hiv Drugs ◽  
Anti Hiv

Viruses are the smallest infectious agents of animal and plant tissues. Viruses are totally dependent on living cells to survive as they utilize the host cell's own replication processes, in order to reproduce themselves. HIV is the causative agent of AIDS. HIV is an unusually difficult to treat because it incorporate its own genetic material into the genome of an infected host cell. It infects T cells that carry the CD4 antigen on their surface. Binding and fusion, reverse transcription, integration, transcription, assembly and budding are the major steps of the HIV life cycle. The HIV/AIDS disease is treated by interrupting the HIV life cycle with specially designed drugs. The discovery of effective drugs against HIV has focused on targeting various critical components of the replication cycle of HIV. Depending on the target within the HIV replicative cycle they interact with, anti-HIV compounds are categorized into six groups. These are: nucleoside (nucleotide) reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), cell entry inhibitors or fusion inhibitors (FIs), co-receptor inhibitors (CRIs) and integrase inhibitors (INIs). The development of effective anti-HIV drugs is difficult due to wide variations in nucleotide and amino acid sequences. The development of anti-HIV drug passes through several important steps. This includes development from α-APA to ITU, ITU to DATA, DAPY to etravirine. Fosdevirine, lersivirine and rilpivirine are among the drugs that were undergoing clinical development and finally only rilpivirine was approved by FDA. The synthesis of delavirdine employs the use of heterocyclic rings like substituted pyridine and indole.

scholarly journals A Review of Electroanalytical Techniques for Determination of Anti-HIV Drugs

2011 ◽  
Vol 2011 ◽  
pp. 1-17 ◽  
Author(s):  
Burçin Bozal ◽  
Bengi Uslu ◽  
Sibel A. Özkan
Keyword(s):  
Reverse Transcriptase ◽  
Immune Deficiency Syndrome ◽  
Deficiency Syndrome ◽  
Reverse Transcriptase Inhibitors ◽  
Pharmaceutical Dosage Forms ◽  
Fusion Inhibitors ◽  
Voltammetric Techniques ◽  
Hiv Drugs ◽  
Anti Hiv

Until now after the human immunodeficiency virus (HIV) was discovered as the then tentative aetiological agent of acquired immune deficiency syndrome (AIDS), exactly 25 anti-HIV compounds have been formally approved for clinical use in the treatment of AIDS. These compounds fall into six categories: nucleoside reverse transcriptase inhibitors (NRTIs: zidovudine, didanosine, zalcitabine, lamivudine, abacavir, stavudine, and emtricitabine), nucleotide reverse transcriptase inhibitors (NtRTIs: tenofovir), nonnucleoside reverse transcriptase inhibitors (NNRTIs: efavirenz, nevirapine, delavirdine, and etravirine), protease inhibitors (PIs: ritonavir, indinavir, saquinavir, nelfinavir, amprenavir, lopinavir, fosamprenavir, atazanavir, tipranavir and darunavir), fusion inhibitors (FIs: enfuvirtide), coreceptor inhibitors (CRIs: maraviroc), and integrase inhibitors (INIs: raltegravir). The present paper submitted the use of various electroanalytical techniques for the determination of anti-HIV drugs. This paper covers the time period from 1990 to 2010 including voltammetric techniques that were reported. Presented application concerns analysis of anti-HIV drugs from pharmaceutical dosage forms and biological samples.

scholarly journals Twenty-six years of HIV science: an overview of anti-HIV drugs metabolism

2011 ◽  
Vol 47 (2) ◽  
pp. 209-230 ◽  
Author(s):  
Carolina Horta Andrade ◽  
Lenis Medeiros de Freitas ◽  
Valéria de Oliveira
Keyword(s):  
Reverse Transcriptase ◽  
Pharmacokinetic Profile ◽  
Antiretroviral Drugs ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Entry Inhibitors ◽  
Fusion Inhibitors ◽  
Hiv Research ◽  
Hiv Drugs ◽  
Anti Hiv

From the identification of HIV as the agent causing AIDS, to the development of effective antiretroviral drugs, the scientific achievements in HIV research over the past twenty-six years have been formidable. Currently, there are twenty-five anti-HIV compounds which have been formally approved for clinical use in the treatment of AIDS. These compounds fall into six categories: nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), cell entry inhibitors or fusion inhibitors (FIs), co-receptor inhibitors (CRIs), and integrase inhibitors (INIs). Metabolism by the host organism is one of the most important determinants of the pharmacokinetic profile of a drug. Formation of active or toxic metabolites will also have an impact on the pharmacological and toxicological outcomes. Therefore, it is widely recognized that metabolism studies of a new chemical entity need to be addressed early in the drug discovery process. This paper describes an overview of the metabolism of currently available anti-HIV drugs.

New Perspectives for the Treatment of HIV Infections

1998 ◽  
Vol 63 (4) ◽  
pp. 449-479 ◽  
Author(s):  
Erik De Clercq
Keyword(s):  
Reverse Transcriptase ◽  
Binding Site ◽  
Substrate Binding ◽  
Hiv Infections ◽  
Reverse Transcriptase Inhibitors ◽  
Substrate Binding Site ◽  
Hiv Inhibition ◽  
Hiv Drugs ◽  
Anti Hiv ◽  
Replicative Cycle

The HIV replicative cycle reveals several virus-specific events that could function as targets for chemotherapeutic intervention. The compounds that are presently available as anti-HIV drugs are targeted at either the substrate binding site of the reverse transcriptase (zidovudine, didanosine, zalcitabine, stavudine, lamivudine) or a non-substrate binding site of the reverse transcriptase (nevirapine, delavirdine), or the viral protease (saquinavir, ritonavir, indinavir, nelfinavir). Remarkable clinical efficacy has been observed with combinations of different reverse transcriptase inhibitors and protease inhibitors. It may be anticipated that with the advent of newer and more efficient compounds the effectiveness of HIV inhibition could still be improved upon and the prospects for a definitive cure of the disease may be accomplished. An account with 107 references.

scholarly journals Maraviroc (Celsentri) in HIV treatment

2008 ◽  
Vol 9 (4) ◽  
pp. 219-222
Author(s):  
Viola Sacchi
Keyword(s):  
Reverse Transcriptase ◽  
Treatment Options ◽  
Hiv Treatment ◽  
New Drugs ◽  
Reverse Transcriptase Inhibitors ◽  
Nucleoside Reverse Transcriptase Inhibitors ◽  
Fusion Inhibitors ◽  
Highly Active ◽  
Hiv Drugs ◽  
Immunodeficiency Syndrome

Since 1996, the prognosis of people living with immunodeficiency virus (HIV) and acquired immunodeficiency syndrome (AIDS) has improved significantly, due to highly active antiretroviral therapies (HAART) based on a combination of 3-4 anti-HIV drugs; the use ofthese drugs can achieve a durable suppression of HIV viraemia, turning HIV infection into a chronic illness. The three first licensed classes of antiretroviral agents are nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs) and protease inhibitors (PIs). Until recently, treatment options for individuals developing resistanceto these drugs have been limited, but new drugs in existing classes (second generation NNRTIs and novel PIs) and novel classes of drugs (integrase inhibitors, CCR5 antagonists and fusion inhibitors) have become clinically available.

Design, synthesis, and anti-HIV activity of 4′-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors

2009 ◽  
Vol 17 (4) ◽  
pp. 1739-1746 ◽  
Author(s):  
Constantine G. Boojamra ◽  
Jay P. Parrish ◽  
David Sperandio ◽  
Ying Gao ◽  
Oleg V. Petrakovsky ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Reverse Transcriptase Inhibitors ◽  
Design Synthesis ◽  
Carbocyclic Nucleoside ◽  
Anti Hiv

scholarly journals Fullerene Derivatives of Nucleoside HIV Reverse Transcriptase Inhibitors—In Silico Activity Prediction

2018 ◽  
Vol 19 (10) ◽  
pp. 3231 ◽  
Author(s):  
Aleksandra Dąbrowska ◽  
Tomasz Pieńko ◽  
Przemysław Taciak ◽  
Katarzyna Wiktorska ◽  
Zdzisław Chilmonczyk ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Hiv Reverse Transcriptase ◽  
Reverse Transcriptase Inhibitors ◽  
Activity Prediction ◽  
Hiv Therapy ◽  
C20 Fullerene ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Similar Affinity ◽  
Hiv 1

Here we present new derivatives of nucleoside reverse transcriptase inhibitors with a C20 fullerene. The computational chemistry methods used in this study evaluate affinity of designed compounds towards the HIV-1 reverse transcriptase (RT) binding site and select the most active ones. The best of the designed compounds have superior or similar affinity to RT active site in comparison to most active test compounds, including drugs used in anti-HIV therapy.

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