Výsledky vyhledávání - "Nabil, Asaad"

Quantitative Prediction of Rate Constants for Aqueous Racemization To Avoid Pointless Stereoselective Syntheses

Autor: Andrew G. Leach, Stefania Narduolo, Niklaas J. Buurma, Hiwa O. Ahmad, Simone Tomasi, Andrew Ballard, Nikki Chand, Peter Varkonyi, David A. Cosgrove, Nabil Asaad, Lucy Rosa

Publikováno v: Angewandte Chemie (International Ed. in English)

Racemization has a large impact upon the biological properties of molecules but the chemical scope of compounds with known rate constants for racemization in aqueous conditions was hitherto limited. To address this remarkable blind spot, we have meas

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7eca562e1d74c07061874b0013627f5c
https://pubmed.ncbi.nlm.nih.gov/29072355

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Dipeptidyl nitrile inhibitors of Cathepsin L

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:4280-4283

A series of potent Cathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.

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https://doi.org/10.1016/j.bmcl.2009.05.071

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Mechanistic studies on the synthesis of bicalutamide

Autor: Nabil Asaad, Shaun M. Fillery

Publikováno v: Org. Biomol. Chem.. 7:678-686

Bicalutamide, a therapeutically important anti-androgen used in the treatment of hormone-sensitive cancers, may be synthesised from the appropriate halohydrin or epoxide. We report here studies aimed at demonstrating unambiguously that preparation of

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https://doi.org/10.1039/b815894k

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The search for efficient intramolecular proton transfer from carbon: the kinetically silent intramolecular general base-catalysed elimination reaction ofO-phenyl 8-dimethylamino-1-naphthaldoximes

Autor: Liisa D. Van Vliet, John E. Davies, Anthony J. Kirby, Nabil Asaad, Laura Ottavi, David R. W. Hodgson

Publikováno v: Journal of Physical Organic Chemistry. 18:101-109

The ready elimination of phenol/phenoxide from the O-phenyl oxime 10E derived from 8-dimethylamino-1-naphthaldehyde, necessarily involving proton transfer from carbon, is catalysed by the neighbouring NMe2 group at pH > 9. However, reaction is faster

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https://doi.org/10.1002/poc.858

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Concurrent nucleophilic and general acid catalysis of the hydrolysis of a phosphate triester

Autor: Anthony J. Kirby, Nabil Asaad

Publikováno v: Journal of the Chemical Society, Perkin Transactions 2. :1708-1712

The hydrolysis of diethyl 8-dimethylaminonaphthyl-1-phosphate is catalysed by the neighbouring dimethylammonium group, with a rate acceleration, compared with diethyl naphthyl-1-phosphate, of almost 106. The effective pKa of the naphtholate leaving g

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https://doi.org/10.1039/b204609a

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Aqueous solutions that model the cytosol: studies on polarity, chemical reactivity and enzyme kinetics

Autor: Nabil, Asaad, Marie Jetta, den Otter, Jan B F N, Engberts

Publikováno v: Organicbiomolecular chemistry. 2(9)

Concentrated solutions of a series of organic compounds have been prepared and the effects of these solutes on the properties of the solvent system assessed as a function of their concentration and nature. Polarity, as measured by Reichardt's E(T)(30

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https://pubmed.ncbi.nlm.nih.gov/15105933

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Cytosol-Mimetic Chemistry: Kinetics of the Trypsin-Catalyzed Hydrolysis of p-Nitrophenyl Acetate upon Addition of Polyethylene Glycol and N-tert-Butyl Acetoacetamide

Autor: Nabil Asaad, Jan B. F. N. Engberts

Publikováno v: Journal of the American Chemical Society, 125(23), 6874-6875. AMER CHEMICAL SOC

The sensitivity of an enzyme to its environment has provoked much interest both for its immediate relevance to biochemistry and for the use of enzymes in chemical synthesis. The intercellular or extracellular environment in which an enzyme naturally

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https://doi.org/10.1021/ja034298f

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Enantiomeric pairs reveal that key medicinal chemistry parameters vary more than simple physical property based models can explain

Autor: Simone Tomasi, Nabil Asaad, Elizabeth Pilling, Niklaas J. Buurma, Stefania Narduolo, Andrew Ballard, Andrew G. Leach, Alfred A. Rabow

Publikováno v: MedChemComm. 3:528

An on-going trend in the medicinal chemistry literature is to link physical properties of a molecule that are achiral (such as lipophilicity) to biological or pharmaceutical properties (such as pharmacokinetics and toxicity) which depend upon interac

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https://doi.org/10.1039/c2md20010d

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