Efficient synthesis of imidazoles from aldehydes and 1, 2-diketones using microwave irradiation

SE Wolkenberg, DD Wisnoski, WH Leister… - Organic …, 2004 - ACS Publications
A simple, high-yielding synthesis of 2,4,5-trisubstituted imidazoles from 1,2-diketones and
aldehydes in the presence of NH 4 OAc is described. Under microwave irradiation, alkyl-, aryl-…

Discovery of a first-in-class receptor interacting protein 1 (RIP1) kinase specific clinical candidate (GSK2982772) for the treatment of inflammatory diseases

…, RD Totoritis, A Vossenkämper, P Ward, DD Wisnoski… - 2017 - ACS Publications
RIP1 regulates necroptosis and inflammation and may play an important role in contributing
to a variety of human pathologies, including immune-mediated inflammatory diseases. Small…

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models

…, DJ Bickel, MK Clements, TB Chen, DD Wisnoski… - … of Pharmacology and …, 2005 - ASPET
We found that 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide (CDPPB) is a potent
and selective positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (…

General microwave-assisted protocols for the expedient synthesis of quinoxalines and heterocyclic pyrazines

Z Zhao, DD Wisnoski, SE Wolkenberg, WH Leister… - Tetrahedron …, 2004 - Elsevier
Functionalized quinoxalines and heterocyclic pyrazines are expediently prepared in excellent
yields (69–99%) from common 1,2-diketone intermediates under microwave irradiation. In …

Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of N-(1,3-Diphenyl-1H- pyrazol-5-yl)benzamides That …

CW Lindsley, DD Wisnoski, WH Leister… - Journal of medicinal …, 2004 - ACS Publications
This report describes the discovery of the first centrally active allosteric modulators of the
metabotropic glutamate receptor subtype 5 (mGluR5). Appropriately substituted N-(1,3-diphenyl…

A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain

…, M Wittmann, MA Jacobson, SN Ha, DD Wisnoski… - … of Pharmacology and …, 2004 - ASPET
We found that N-{4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide
(CPPHA), is a potent and selective positive allosteric modulator of the …

Cell-based selection expands the utility of DNA-encoded small-molecule library technology to cell surface drug targets: identification of novel antagonists of the NK3 …

…, J Zhang, VQ Bodmer, DD Wisnoski… - ACS Combinatorial …, 2015 - ACS Publications
DNA-encoded small-molecule library technology has recently emerged as a new paradigm
for identifying ligands against drug targets. To date, this technology has been used with …

Broadening the scope of 1, 2, 4-triazine synthesis by the application of microwave technology

Z Zhao, WH Leister, KA Strauss, DD Wisnoski… - Tetrahedron letters, 2003 - Elsevier
Wisnoski , Craig W. Lindsley … Leister, WH; Strauss, KA; Wisnoski, DD; Zhao, Z.; Lindsley,
CW J. Comb. Chem., submitted. … H NMR (300 MHz, CDCl 3 ): δ 7.56 (m, 4H), 7.36 (m, 6H) …

Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists

…, BW Budzik, SA Ross, DD Wisnoski… - Journal of medicinal …, 2009 - ACS Publications
A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening
campaign as novel, potent small molecule agonists of the human TGR5 G-protein coupled …

Discovery and lead-optimization of 4, 5-dihydropyrazoles as mono-kinase selective, orally bioavailable and efficacious inhibitors of receptor interacting protein 1 (RIP1 …

…, P Ward, N Wellaway, DD Wisnoski… - Journal of Medicinal …, 2019 - ACS Publications
RIP1 kinase regulates necroptosis and inflammation and may play an important role in
contributing to a variety of human pathologies, including inflammatory and neurological diseases. …