Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate

Mowbray, Charles E.; Burt, Catherine; Corbau, Romuald; Gayton, Simon; Hawes, Michael; Perros, Manos; Tran, Isabelle; Price, David A.; Quinton, Faye J.; Selby, Matthew D.; Stupple, Paul A.; Webster, Rob; Wood, Anthony

doi:10.1016/j.bmcl.2009.08.080

Cited by 97 publications

(46 citation statements)

References 16 publications

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“…The novel pyrazole NNRTI lersivirine, developed following structural optimization of a lead compound [30], was initially identified as a promising candidate for treating drug-resistant mutants of HIV-1 [31]. Phase I clinical trials reported a satisfactory safety and tolerability profile for the drug following 28-day daily-dosing regimen [32].…”

Section: Non-nucleoside Reverse Transcriptase Inhibitorsmentioning

confidence: 99%

Investigational reverse transcriptase inhibitors for the treatment of HIV

Cory

Midde

Rao

et al. 2015

Expert Opinion on Investigational Drugs

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Introduction While considerable advances have been made in the development of antiretroviral agents, there is still work to be done. Reverse transcriptase inhibitors are important drugs for the treatment of HIV, and considerable research is currently ongoing to develop new agents and to modify currently existing agents. Areas covered Herein, the authors discuss both investigational nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs), including agents that are in various stages of development. They also discuss novel formulations that are being investigated for currently available drugs, and discuss the advantages that these new formulations may provide. Expert opinion New formulations and co-formulations of currently existing antiretrovirals will represent an important area of development, as a means to improve adherence for HIV-positive individuals. New formulations will continue to be developed, with a focus on allowing for less-frequent administration, as well increasing drug concentrations at local sites such as vaginal tissue, rectal tissue and sites in the immune system.

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Section: Non-nucleoside Reverse Transcriptase Inhibitorsmentioning

confidence: 99%

Investigational reverse transcriptase inhibitors for the treatment of HIV

Cory

Midde

Rao

et al. 2015

Expert Opinion on Investigational Drugs

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“…Recently, pyrazole derivatives have attracted a great attention due to their several chemicals and pharmacological importance [1][2][3]. Moreover, many pyrazole derivatives exhibit a wide range of therapeutic activities including anticonvulsant [4], analgesic, anti-inflammatory [5][6][7], antimicrobial [8], anticoagulant activity [9], antioxidant [10], antiamoebic [11,12], Antidepressant [13], antihyperglycemic [14], antihistaminic [15], anti-viral [16], anti-HIV [17], and anticancer [18][19][20][21][22]. (Fig.…”

Section: Introductionmentioning

confidence: 99%

“…The solvent was evaporated under reduced pressure. The solid product was washed three times with 30 mL methanol and recrystallized from dioxane to produce 17 …”

Section: Methyl-3-[(3-cyano-4-(3-methyl-1-phenyl-5h -Pyrazol-4-yl)-4hmentioning

confidence: 99%

Microwave-Assisted Synthesis and Cytotoxicity Evaluation of Some Novel Pyrazole Containing Imidiazole, Pyrazole, Oxazole, Thiadiazole and Benzochromene derivatives

Hafez

2017

Egypt. J. Chem.

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“…Designing drug-like molecules that can fit to the non nucleoside inhibitory binding pocket (NNIBP) of HIV -1-RT will be a promising starting point in developing anti HIV drugs. Recently NNRTIs like lersiverine, bearing pyrazole moiety has received great attention in the field of anti HIV research [4]. This paper aims to put forth in designing newer pyrazole analogs as possible HIV-1RT inhibitors.…”

Section: Introductionmentioning

confidence: 99%

Molecular Docking Studies of Novel Pyrazole Analogs as Possible HIV-1-RT Inhibitors

Ganguly

2014

Proceedings of the 18th International Electronic Conference on Synthetic Organic Chemistry

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Human immunodeficiency virus (HIV) is the causative agent of the acquired immunodeficiency syndrome (AIDS) that has been affected 34 million people worldwide. Though an unprecedented growth has been taken place in the development of anti-HIV drugs during the last two decades, there is still no cure for this deadly disease. Cross resistance to anti HIV drugs is also a major concern in the development of anti AIDS pharmaceuticals. Therefore, nowadays studies are being focused mainly on the development of

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Pyrazole NNRTIs 4: Selection of UK-453,061 (lersivirine) as a Development Candidate

Cited by 97 publications

References 16 publications

Investigational reverse transcriptase inhibitors for the treatment of HIV

Investigational reverse transcriptase inhibitors for the treatment of HIV

Microwave-Assisted Synthesis and Cytotoxicity Evaluation of Some Novel Pyrazole Containing Imidiazole, Pyrazole, Oxazole, Thiadiazole and Benzochromene derivatives

Molecular Docking Studies of Novel Pyrazole Analogs as Possible HIV-1-RT Inhibitors

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