A5084720721- Hepatitis C virus research
- HIV/AIDS drug development and treatment
- Monoclonal and Polyclonal Antibodies Research
- Hepatitis B Virus Studies
- Click Chemistry and Applications
- Organic Chemistry Cycloaddition Reactions
- Chemical Synthesis and Reactions
- Chemical Reaction Mechanisms
- HIV Research and Treatment
- Asymmetric Synthesis and Catalysis
- Asymmetric Hydrogenation and Catalysis
- Connexins and lens biology
- Carbon dioxide utilization in catalysis
- Biochemical and Molecular Research
- Nicotinic Acetylcholine Receptors Study
- Organic and Molecular Conductors Research
- Advanced Drug Delivery Systems
- Immunodeficiency and Autoimmune Disorders
- Advanced Breast Cancer Therapies
- X-ray Diffraction in Crystallography
- Pneumocystis jirovecii pneumonia detection and treatment
- Chronic Lymphocytic Leukemia Research
- Synthesis of β-Lactam Compounds
- Computational Drug Discovery Methods
- Yersinia bacterium, plague, ectoparasites research
Merck & Co., Inc., Rahway, NJ, USA (United States)
2015-2018
Montpellier GenomiX
2011-2014
Centro de Biología Molecular Severo Ochoa
2011
Universidad Autónoma de Madrid
2011
Austin Hospital
2011
The University of Melbourne
2011
Burnet Institute
2011
The University of Texas Medical Branch at Galveston
2009
Idera Pharmaceuticals (United States)
2008
Hôpital Necker-Enfants Malades
2007
Here, we describe the design, synthesis, biological evaluation, and identification of a clinical candidate non-nucleoside reverse transcriptase inhibitors (NNRTIs) with novel aryl-phospho-indole (APhI) scaffold. NNRTIs are recommended components highly active antiretroviral therapy (HAART) for treatment HIV-1. Since major problem associated NNRTI is emergence drug resistant virus, this work focused on optimization APhI against clinically relevant HIV-1 Y181C K103N mutants Y181C/K103N double...
The availability of an effective vaginal microbicide would be a major step toward containment HIV transmission as well allowing women self-protection against infection. Here we evaluated the efficacy application potent nonnucleoside reverse transcriptase inhibitor (NNRTI) MC 1220 challenge macaques with RT-SHIV, chimeric simian immunodeficiency virus (SIV) containing (RT) gene HIV-1. Challenge infection monkeys RT-SHIV currently represents only nonhuman primate model available to test...
MC-1220 is a highly potent and selective non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV. The objective to develop formulations for the vaginal delivery characterize them in vitro vivo (drug uptake, pharmacokinetics, toxicokinetics irritation/inflammation). Due low aqueous solubility MC-1220, emulsion-type liposomal were developed. After rheological property adjustment (by gelling agents), toxicity two types (emulsion [E] [LIP] formulations) at 0.1% (E LIP) 0.5% (LIP) drug...
A new and improved synthetic route to an intermediate in the synthesis of phosphinate ester GSK2248761A is described. In key step, we describe first process-scale example a palladium-catalyzed phosphorus–carbon coupling give entire backbone one telescoped stage 65% average yield on 68 kg scale. This unusual chemistry enabled be reduced from six stages four eliminated number environmentally unfriendly reagents solvents.
Abstract We describe herein a versatile methodology for the synthesis of 1,2‐sulfoximidoyl ethanols thanks to Ca(NTf 2 ) ‐catalyzed epoxide ring‐opening with NH sulfoximines in 2‐MeTHF at 90 °C. The reaction is regioselective by an attack on less hindered position epoxides. chemoselectivity assessed competition reactions other nucleophiles.
Abstract Small molecule macrocyclic kinase inhibitors have attracted significant attention in drug discovery over the past years with drugs approval such as lorlatinib demonstrating clinical relevance of this approach. We developed our expertise to further optimize those cyclic molecules. Having low molecular weight, they favorably alter biological and physiochemical properties well selectivity, compared their linear parent, yielding high-quality candidates. While focused on inhibitors,...
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