Results 201 to 210 of about 23,536 (264)
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Highly Efficient Synthesis of HIV NNRTI Doravirine
Organic Letters, 2015The development of an efficient and robust process for the production of HIV NNRTI doravirine is described. The synthesis features a continuous aldol reaction as part of a de novo synthesis of the key pyridone fragment. Conditions for the continuous flow aldol reaction were derived using microbatch snapshots of the flow process.
Donald R, Gauthier +7 more
openaire +3 more sources
The search for potent, small molecule NNRTIs: A review
Bioorganic and Medicinal Chemistry, 2009AIDS has become the leading pandemic disease, and is the cause of death worldwide. Presently, HAART treatment, a combination of reverse transcriptase (RT) and protease inhibitors is also unsuccessful due to the virus getting resistant to the drugs because of mutational changes.
Ramajayam Ramachandran +2 more
exaly +3 more sources
HIV Clinical Trials, 2002
The efficacy of treatment containing nonnucleoside reverse transcriptase inhibitors (NNRTIs) could be compromised in NNRTI-naïve patients already harboring a virus resistant to NNRTIs. On the contrary, hypersusceptibility to NNRTIs in patients having failed nucleoside reverse transcriptase inhibitor (NRTI)-containing regimens has been described and has
P Clevenbergh, E Cua, J Cottalorda
exaly +3 more sources
The efficacy of treatment containing nonnucleoside reverse transcriptase inhibitors (NNRTIs) could be compromised in NNRTI-naïve patients already harboring a virus resistant to NNRTIs. On the contrary, hypersusceptibility to NNRTIs in patients having failed nucleoside reverse transcriptase inhibitor (NRTI)-containing regimens has been described and has
P Clevenbergh, E Cua, J Cottalorda
exaly +3 more sources
Proteins: Structure, Function and Bioinformatics, 2017 Non‐nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase (RT), NNRTIs, which bind to the p66/p51 heterodimeric RT, also interact with the p66/p66 homodimer, whose structure is unknown.
Angela Gronenborn +2 more
exaly +2 more sources
Médecine et Maladies Infectieuses, 2012
One of the choice criteria for antiretroviral therapy, once the viral load is controlled, is long-term treatment safety. Safety, despite similarities in each therapeutic class, can differ significantly from one agent to another, according to their respective pharmacokinetic and pharmacodynamic properties. We reviewed data on two very well-known NNRTIs,
P, Dellamonica, G, Di Perri, R, Garraffo
openaire +2 more sources
One of the choice criteria for antiretroviral therapy, once the viral load is controlled, is long-term treatment safety. Safety, despite similarities in each therapeutic class, can differ significantly from one agent to another, according to their respective pharmacokinetic and pharmacodynamic properties. We reviewed data on two very well-known NNRTIs,
P, Dellamonica, G, Di Perri, R, Garraffo
openaire +2 more sources
Médecine et Maladies Infectieuses, 2012
The contribution of efavirenz and nevirapine remains clinically relevant and is the reason for the frequent prescription of these two agents. Recent clinical data on efavirenz and nevirapine in naive patients confirms their effectiveness compared to protease inhibitors such as lopinavir/r (ACTG 5142) or atazanavir/r (ACTG 5202) for efavirenz, or such ...
P, Dellamonica, G, Di Perri, R, Garraffo
openaire +2 more sources
The contribution of efavirenz and nevirapine remains clinically relevant and is the reason for the frequent prescription of these two agents. Recent clinical data on efavirenz and nevirapine in naive patients confirms their effectiveness compared to protease inhibitors such as lopinavir/r (ACTG 5142) or atazanavir/r (ACTG 5202) for efavirenz, or such ...
P, Dellamonica, G, Di Perri, R, Garraffo
openaire +2 more sources
Will NNRTIs be driving forward again?
The Lancet HIV, 2018Comment on : Molina JM, Squires K, Sax PE, Cahn P, Lombaard J, DeJesus E, Lai MT, Xu X, Rodgers A, Lupinacci L, Kumar S, Sklar P, Nguyen BY, Hanna GJ, Hwang C; DRIVE-FORWARD Study Group. Doravirine versus ritonavir-boosted darunavir in antiretroviral-naive adults with HIV-1 (DRIVE-FORWARD): 48-week results of a randomised, double-blind, phase 3, non ...
Calmy, Alexandra, Tarr, Philip E
openaire +3 more sources
The AIDS reader, 2005
Hypersusceptibility to the nonnucleoside reverse transcriptase inhibitors (NNRTIs) is a recently described observation in which approximately 30% of HIV isolates with resistance to nucleoside reverse transcriptase inhibitors exhibit greater phenotypic susceptibility to the NNRTI class than does wild-type HIV.
Jamael, Delgado, Nancy, Shulman
openaire +1 more source
Hypersusceptibility to the nonnucleoside reverse transcriptase inhibitors (NNRTIs) is a recently described observation in which approximately 30% of HIV isolates with resistance to nucleoside reverse transcriptase inhibitors exhibit greater phenotypic susceptibility to the NNRTI class than does wild-type HIV.
Jamael, Delgado, Nancy, Shulman
openaire +1 more source
Pyrazole NNRTIs 3: Optimisation of physicochemical properties
Bioorganic & Medicinal Chemistry Letters, 2009Our efforts to reduce overall lipophilicity and increase ligand-lipophilicity efficiency (LLE) by modification of the 3- and 5-substituents of pyrazole 1, a novel non-nucleoside HIV reverse transcriptase inhibitor (NNRTI) prototype were unsuccessful. In contrast replacement of the substituted benzyl group with corresponding phenylthio or phenoxy groups
Charles E, Mowbray +9 more
openaire +2 more sources
Clinical Therapeutics, 2009
Since 1981, the AIDs epidemic has continued to expand and, at the end of 2007, there were ~33 million people worldwide living with HIV, including 1.2 million in North America.This article provides a comprehensive overview of the nonnucleoside reverse transcriptase inhibitor (NNRTI) etravirine when used in treatment-experienced adult patients with ...
Daryl S, Schiller +1 more
openaire +2 more sources
Since 1981, the AIDs epidemic has continued to expand and, at the end of 2007, there were ~33 million people worldwide living with HIV, including 1.2 million in North America.This article provides a comprehensive overview of the nonnucleoside reverse transcriptase inhibitor (NNRTI) etravirine when used in treatment-experienced adult patients with ...
Daryl S, Schiller +1 more
openaire +2 more sources