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Dive into the research topics where Aihua Wang is active.

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Featured researches published by Aihua Wang.


Bioorganic & Medicinal Chemistry Letters | 2003

Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.

Bruce E. Tomczuk; Tianbao Lu; Richard Soll; Cynthia L. Fedde; Aihua Wang; Larry Murphy; Carl Crysler; Malini Dasgupta; Stephen Eisennagel; John Spurlino; Roger F. Bone

Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and long half-life have been elusive. We report here a novel series non-peptidic phenyl-based, highly potent, highly selective and orally bioavailable thrombin inhibitors using oxyguanidines as guanidine-mimetics.


Bioorganic & Medicinal Chemistry Letters | 2013

Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists

Brian C. Shook; Devraj Chakravarty; J. Kent Barbay; Aihua Wang; Kristi A. Leonard; Vernon C. Alford; Mark T. Powell; Stefanie Rassnick; Robert H. Scannevin; Karen I. Carroll; Nathaniel H. Wallace; Jeffrey Crooke; Mark Ault; Lisa Lampron; Lori Westover; Kenneth J. Rhodes; Paul F. Jackson

A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A2A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.


Bioorganic & Medicinal Chemistry Letters | 2017

Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt

David A. Kummer; Maxwell D. Cummings; Marta Cristina Abad; Joseph Kent Barbay; Glenda Castro; Ronald L. Wolin; Kevin D. Kreutter; Umar Maharoof; Cynthia M. Milligan; Rachel Nishimura; Joan Pierce; Celine Schalk-Hihi; John Spurlino; Maud Urbanski; Hariharan Venkatesan; Aihua Wang; Craig R. Woods; Xiaohua Xue; James P. Edwards; Anne Fourie; Kristi A. Leonard

A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.


Bioorganic & Medicinal Chemistry Letters | 2017

6-Substituted quinolines as RORγt inverse agonists

J. Kent Barbay; Maxwell D. Cummings; Marta Cristina Abad; Glenda Castro; Kevin D. Kreutter; David A. Kummer; Umar Maharoof; Cynthia M. Milligan; Rachel Nishimura; Joan Pierce; Celine Schalk-Hihi; John Spurlino; Virginia M. Tanis; Maud Urbanski; Hariharan Venkatesan; Aihua Wang; Craig R. Woods; Ronald L. Wolin; Xiaohua Xue; James P. Edwards; Anne Fourie; Kristi A. Leonard

We identified 6-substituted quinolines as modulators of the retinoic acid receptor-related orphan receptor gamma t (RORγt). The synthesis of this class of RORγt modulators is reported, and optimization of the substituents at the quinoline 6-position that produced compounds with high affinity for the receptor is detailed. This effort identified molecules that act as potent, full inverse agonists in a RORγt-driven cell-based reporter assay. The X-ray crystal structures of two full inverse agonists from this chemical series bound to the RORγt ligand binding domain are disclosed, and we highlight the interaction of a hydrogen-bond acceptor on the 6-position substituent of the inverse agonist with Glu379:NH as a conserved binding contact.


Archive | 2000

Heterocyclic protease inhibitors

Aihua Wang; Tianbao Lu; Bruce E. Tomczuk; Richard M. Soll; John Spurlino; Roger F. Bone


Archive | 2013

SECONDARY ALCOHOL QUINOLINYL MODULATORS OF RORyt

Kristi A. Leonard; Kent Barbay; James P. Edwards; Kevin D. Kreutter; David A. Kummer; Umar Maharoof; Rachel Nishimura; Maud Urbanski; Hariharan Venkatesan; Aihua Wang; Ronald L. Wolin; Craig R. Woods; Anne Fourie; Xiaohua Xue; Maxwell D. Cummings


Archive | 2001

Cyclic oxyguanidine pyrazinones as protease inhibitors

Aihua Wang; Bruce E. Tomczuk; Tianbao Lu; Richard M. Soll; John Spurlino; Roger F. Bone


Archive | 2001

Cyclic oxyguanidine protease inhibitors

Aihua Wang; Tianbao Lu; Bruce E. Tomczuk; Richard M. Soll; John Spurlino; Roger F. Bone


Archive | 2013

Methylene linked quinolinyl modulators of RORγt

Kristi A. Leonard; Kent Barbay; James P. Edwards; Kevin D. Kreutter; David A. Kummer; Umar Maharoof; Rachel Nishimura; Maud Urbanski; Hariharan Venkatesan; Aihua Wang; Ronald L. Wolin; Craig R. Woods; Anne Fourie; Xiaohua Xue; Maxwell D. Cummings; William M. Jones; Steven Goldberg


Archive | 2012

Methods of treatment using allosteric processing inhibitors for matrix metalloproteinases

Kristi A. Leonard; Richard Alexander; Joseph Kent Barbay; Roger F. Bone; Carl S. Crysler; Ingrid Christa Deckman; Paul F. Jackson; Lawrence C. Kuo; Frank A. Lewandowski; Diane M. Maguire; Carl L. Manthey; Cynthia M. Milligan; Beverley A. Moore; Kenneth J. Rhodes; Robert H. Scannevin; Celine Schalk-Hihi; Barry Springer; John Spurlino; Matthew J. Todd; Brett A. Tounge; Aihua Wang

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