Mitigating heterocycle metabolism in drug discovery

DJ St. Jean Jr, C Fotsch - Journal of medicinal chemistry, 2012 - ACS Publications
In the past few decades, drug metabolism research has played an ever increasing role in the
design of drugs. 1− 3 In vitro metabolism assays 4 have become an integral part of the …

Medicinal attributes of imidazo [1, 2-a] pyridine derivatives: an update

N Devi, D Singh, RK Rawal, J Bariwal… - Current topics in …, 2016 - ingentaconnect.com
The imidazo [1, 2-a] pyridine scaffold is recognized as a privileged structure as it represents
a promising area for identification of lead structures towards the discovery of new synthetic …

[图书][B] Microwave heating as a tool for sustainable chemistry

NE Leadbeater - 2010 - taylorfrancis.com
Shorter reaction times, higher product yields, and enhanced selectivity are some of the
advantages microwave heating has over conventional methods, causing its use to transition …

Synthesis of imidazo [1, 2-a] pyridin-chromones by a MW assisted Groebke–Blackburn–Bienaymé process

KG Kishore, UMV Basavanag, A Islas-Jácome… - Tetrahedron …, 2015 - Elsevier
A series of nine novel imidazo [1, 2-a] pyridin-chromones and nine novel imidazo [1, 2-a]
pyridin-6-fluorochromones were synthesized in good to excellent yields by a MW assisted …

H+/K+-ATPase inhibitors: a patent review

H Li, L Meng, F Liu, JF Wei… - Expert Opinion on …, 2013 - Taylor & Francis
Introduction: H+/K+-ATPase is a P-type ATP-driven cation transporter which exchanges ions
(protons, chloride ions, and potassium ions) across the cell membrane. Modulators of H+/K+ …

Six-membered ring systems: pyridines and benzo derivatives

PE Alford - Progress in Heterocyclic Chemistry, 2011 - Elsevier
Publisher Summary This chapter describes the synthesis and chemistry of six-membered
ring systems, particularly pyridines and benzo derivatives. Pyridine and pyridine-derived …

Direct preparation of heteroaromatic compounds from alkenes

TJ Donohoe, MA Kabeshov, AH Rathi, IED Smith - Synlett, 2010 - thieme-connect.com
A series of aromatic heterocycles, thiazoles, imidazoles, and dimethoxyindoles, can be
synthesised directly from alkenes via a ketoiodination-cyclisation protocol. The alkene …

Aryl hydrocarbon receptor antagonists and uses thereof

AG Romero - US Patent 10,457,683, 2019 - Google Patents
2 460 805 A 2 651 944 Al WO 94/11026 A2 WO 99/050461 Al WO 00/056729 AL WO
01/085196 A2 WO 01/094420 Al WO 03/090512 A2 WO 2007/095594 A2 WO 2010/059401 …

Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs)

T Panchal, N Bailey, M Bamford, E Demont… - Bioorganic & medicinal …, 2009 - Elsevier
A variety of basic, heterocyclic templates has been reported as potassium-competitive, acid
pump antagonists. Herein, we report a comparison of potencies of these templates and …

Synthesis of 1-pyrroline 1-oxides analogous to pseudouridine

M Koszytkowska-Stawińska, E Mironiuk-Puchalska… - Tetrahedron letters, 2011 - Elsevier
Pseudouridine (ψ-uridine, Ψ) aza′-analogues with a 5, 5-bis (hydroxymethyl)-1-pyrrolin-2-
yl 1-oxide as the glycone mimic were obtained by the addition of (2, 4-dimethoxypyrimidin-5 …