[BOOK][B] Prodrugs: challenges and rewards

V Stella, R Borchardt, M Hageman, R Oliyai, H Maag… - 2007 - books.google.com
Prodrugs are substances administered in an inactive form that is then metabolized in the
body in vivo into the active compound. The rationale behind administering prodrugs is to …

Prodrugs of nucleoside analogues for improved oral absorption and tissue targeting

F Li, H Maag, T Alfredson - Journal of pharmaceutical sciences, 2008 - Elsevier
Nucleoside analogues are widely used for the treatment of antiviral infections and anticancer
chemotherapy. However, many nucleoside analogues suffer from poor oral bioavailability …

Synthesis and anti-HIV activity of 4'-azido-and 4'-methoxynucleosides

H Maag, RM Rydzewski, MJ McRoberts… - Journal of medicinal …, 1992 - ACS Publications
A series of nucleosides were synthesized in which the 4'-hydrogen was substituted with
either an azido or a methoxy group. The key steps in the syntheses of the 4'-azido analogues …

Prodrugs of carboxylic acids

H Maag - Prodrugs: Challenges and Rewards Part 1, 2007 - Springer
Carboxylic acids are often present as a functional group of effective medicines. They are
involved in specific charge-charge interactions and are thus often critical for the binding of …

The design, synthesis, and antiviral activity of monofluoro and difluoro analogues of 4′-azidocytidine against hepatitis C virus replication: the discovery of 4′-azido-2 …

…, XX Zhou, AC Kaiser, H Maag… - Journal of medicinal …, 2009 - ACS Publications
The discovery of 4′-azidocytidine (3) (R1479) ( J. Biol. Chem. 2006 , 281 , 3793 ; Bioorg.
Med. Chem. Lett. 2007 , 17 , 2570 ) as a potent inhibitor of RNA synthesis by NS5B (EC 50 = …

The design, synthesis, and antiviral activity of 4′-azidocytidine analogues against hepatitis C virus replication: the discovery of 4′-azidoarabinocytidine

…, I Najera, K Benkestock, XX Zhou, H Maag… - Journal of Medicinal …, 2009 - ACS Publications
4′-Azidocytidine 3 (R1479) has been previously discovered as a potent and selective
inhibitor of HCV replication targeting the RNA-dependent RNA polymerase of hepatitis C virus, …

Characterization of RO5126946, a Novel α7 Nicotinic Acetylcholine Receptor–Positive Allosteric Modulator

…, R Hirakawa, F Knoflach, D Bertrand, H Maag… - … of Pharmacology and …, 2014 - ASPET
Both preclinical evidence and clinical evidence suggest that α 7 nicotinic acetylcholine
receptor activation (α 7 nAChR) improves cognitive function, the decline of which is associated …

An allylic azide route to 4'-azido carbocyclic nucleosides. Synthesis of (.+-.)-(1'. alpha., 2'. alpha., 3'. beta.)-and (.+-.)-(1'. alpha., 2'. beta., 3'. beta.)-1-[1-azido-2-hydroxy …

H Maag, RM Rydzewski - The Journal of Organic Chemistry, 1992 - ACS Publications
Treatment of (±)-l-[[(tert-butyldiphenylsilyl) oxy] methyl]-3-methoxycyclopent-l-ene (17) with
azidotrimethylsilane under Lewis acid catalyzed conditions gave an equilibrium mixture of …

Solid-state and solution conformations of the potent HIV inhibitor, 4'-azidothymidine

H Maag, JT Nelson, JLR Steiner… - Journal of medicinal …, 1994 - ACS Publications
Results Solid-State Structure. Suitable crystals for X-ray diffraction analyses were obtained
from an acetonitrile solution. A colorless crystal of dimensions 0.30 X 0.35 X 0. 45 mm was …

Controlling the genotoxins ethyl chloride and methyl chloride formed during the preparation of amine hydrochloride salts from solutions of ethanol and methanol

…, P Mason, A Tehim, LE Fisher, H Maag… - … Process Research & …, 2009 - ACS Publications
The genotoxins ethyl chloride (EtCl) and methyl chloride (MeCl) were generated during the
preparation of the hydrochloride salts of two tertiary amines in the presence of ethanol and …