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John Piwinski

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Frank Bennett; Robert Chase; Jeremy L Clark; Stephanie Curry; Anita T Fowler; Feng Geng; F George Njoroge; Viyyoor Girijavallabhan; Hsueh-Cheng Huang; Yuhua Huang; Regina Huelgas; Hollis S Kezar; Cecil D Kwong; Cheng Li; Malcolm MacCoss; Joseph A Maddry; John J Piwinski; Robert C Reynolds; RR Rossman; Abhijit Roychowdhury; John A Secrist; Neng-Yang Shih; Xiao Tong; Subramaniam Ananthan; Ashok Arasappan
Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
Rongze Kuang; Ling Lin; John J Piwinski; Daniel Prelusky; John Schwerdt; Neng-Yang Shih; Ho-Jane Shue; Pauline C Ting; Robert Aslanian; Motasim Billah; David J Blythin; Jianhua Cao; Chander S Celly; Xiao Chen; Danlin Gu; Ping Wu; Li Xiao; Ji Zhang; Xiang Zhang; Peng Wang
Discovery of oxazole-based PDE4 inhibitors with picomolar potency.
Chaoyang Dai; Dansu Li; Janeta Popovici-Muller; Lianyun Zhao; Vinay M Girijavallabhan; Kristin E Rosner; Brian J Lavey; Razia Rizvi; Bandarpalle B Shankar; Michael K C Wong; Zhuyan Guo; Peter Orth; Corey O Strickland; Jing Sun; Xiaoda Niu; Shiying Chen; Joseph A Kozlowski; Daniel Lundell; John J Piwinski; Neng-Yang Shih; M Arshad Siddiqui
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.

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All Publications

2012: Frank Bennett; Robert Chase; Jeremy L Clark; Stephanie Curry; Anita T Fowler; Feng Geng; F George Njoroge; Viyyoor Girijavallabhan; Hsueh-Cheng Huang; Yuhua Huang; Regina Huelgas; Hollis S Kezar; Cecil D Kwong; Cheng Li; Malcolm MacCoss; Joseph A Maddry; John J Piwinski; Robert C Reynolds; RR Rossman; Abhijit Roychowdhury; John A Secrist; Neng-Yang Shih; Xiao Tong; Subramaniam Ananthan; Ashok Arasappan
Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
Bioorganic & medicinal chemistry letters 2012;22(15):5144-9.
2012: Rongze Kuang; Ling Lin; John J Piwinski; Daniel Prelusky; John Schwerdt; Neng-Yang Shih; Ho-Jane Shue; Pauline C Ting; Robert Aslanian; Motasim Billah; David J Blythin; Jianhua Cao; Chander S Celly; Xiao Chen; Danlin Gu; Ping Wu; Li Xiao; Ji Zhang; Xiang Zhang; Peng Wang
Discovery of oxazole-based PDE4 inhibitors with picomolar potency.
Bioorganic & medicinal chemistry letters 2012;22(7):2594-7.
2011: Chaoyang Dai; Dansu Li; Janeta Popovici-Muller; Lianyun Zhao; Vinay M Girijavallabhan; Kristin E Rosner; Brian J Lavey; Razia Rizvi; Bandarpalle B Shankar; Michael K C Wong; Zhuyan Guo; Peter Orth; Corey O Strickland; Jing Sun; Xiaoda Niu; Shiying Chen; Joseph A Kozlowski; Daniel Lundell; John J Piwinski; Neng-Yang Shih; M Arshad Siddiqui
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(10):3172-6.
2010: Wensheng Yu; Ling Tong; Seong Heon Kim; Michael K C Wong; Lei Chen; De-Yi Yang; Bandarpalle B Shankar; Brian J Lavey; Guowei Zhou; Aneta Kosinski; Razia Rizvi; Dansu Li; Robert J Feltz; John J Piwinski; Kristin E Rosner; Neng-Yang Shih; M Arshad Siddiqui; Zhuyan Guo; Peter Orth; Himanshu Shah; Jing Sun; Shelby Umland; Daniel Lundell; Xiaoda Niu; Joseph A Kozlowski
Biaryl substituted hydantoin compounds as TACE inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(17):5286-9.
2010: Wensheng Yu; Zhuyan Guo; Peter Orth; Vincent Madison; Lei Chen; Chaoyang Dai; Robert J Feltz; Vinay M Girijavallabhan; Seong Heon Kim; Joseph A Kozlowski; Brian J Lavey; Dansu Li; Daniel Lundell; Xiaoda Niu; John J Piwinski; Janeta Popovici-Muller; Razia Rizvi; Kristin E Rosner; Bandarpalle B Shankar; Neng-Yang Shih; M Arshad Siddiqui; Jing Sun; Ling Tong; Shelby Umland; Michael K C Wong; De-yi Yang; Guowei Zhou
Discovery and SAR of hydantoin TACE inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(6):1877-80.
2009: Robert Aslanian; John J Piwinski; Xiaohong Zhu; Tony Priestley; Steve Sorota; Xiao-Yi Du; Xue-Song Zhang; Robbie L McLeod; Robert E West; Shirley M Williams; John A Hey
Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.
Bioorganic & medicinal chemistry letters 2009;19(17):5043-7.
2009: Guodong Chen; Ibrahim Daaro; Birendra Pramanik; John J Piwinski
Structural characterization of in vitro rat liver microsomal metabolites of antihistamine desloratadine using LTQ-Orbitrap hybrid mass spectrometer in combination with online hydrogen/deuterium exchange HR-LC/MS.
Journal of mass spectrometry : JMS 2009;44(2):203-13.
2009: Srikanth Venkatraman; Francisco Velazquez; Wanli Wu; Melissa Blackman; Kevin X Chen; Stéphane L Bogen; Latha Nair; Xiao Tong; Robert Chase; A Hart; Sony Agrawal; John Pichardo; Andrew Prongay; Kuo-Chi Cheng; Viyyoor Girijavallabhan; John J Piwinski; Neng-Yang Shih; F George Njoroge
Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease.
Journal of medicinal chemistry 2009;52(2):336-46.
2008: Robert Aslanian; Xiaohong Zhu; Henry A Vaccaro; Neng-Yang Shih; John J Piwinski; Shirley M Williams; Robert E West
Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands.
Bioorganic & medicinal chemistry letters 2008;18(18):5032-6.
2008: Gang Zhou; Pauline Ting; Robert Aslanian; John J Piwinski
A useful Pd-catalyzed Negishi coupling approach to benzylic sulfonamide derivatives.
Organic letters 2008;10(12):2517-20.
2008: F George Njoroge; Kevin X Chen; Neng-Yang Shih; John J Piwinski
Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection.
Accounts of chemical research 2008;41(1):50-9.
2007: Rongze Kuang; Ho-Jane Shue; David J Blythin; Neng-Yang Shih; Danlin Gu; Xiao Chen; John H Schwerdt; Ling Lin; Pauline C Ting; Xiaohong Zhu; Robert Aslanian; John J Piwinski; Li Xiao; Daniel Prelusky; Ping Wu; Ji Zhang; Xiang Zhang; Chander Celly; Michael Minnicozzi; Motasim Billah; Peng Wang
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(18):5150-4.
2006: Waldemar Gonsiorek; David Hesk; Shu-Cheng Chen; David Kinsley; Jay S Fine; James V Jackson; Loretta A Bober; Gregory Deno; Hong Bian; James Fossetta; Charles A Lunn; Joseph A Kozlowski; Brian Lavey; John J Piwinski; Satwant K Narula; Daniel Lundell; R William Hipkin
Characterization of peripheral human cannabinoid receptor (hCB2) expression and pharmacology using a novel radioligand, [35S]Sch225336.
The Journal of biological chemistry 2006;281(38):28143-51.
2006: Michael Berlin; Pauline C Ting; Wayne D Vaccaro; Robert Aslanian; Kevin D McCormick; Joe F Lee; Margaret M Albanese; Mwangi wa Mutahi; John J Piwinski; Neng-Yang Shih; Luli Duguma; Daniel M Solomon; Wei Zhou; Rosy Sher; Leonard Favreau; Matthew Bryant; Walter A Korfmacher; Cymbylene Nardo; Robert E West; John C Anthes; Shirley M Williams; Ren-Long Wu; H Susan She; Maria A Rivelli; Michel R Corboz; John A Hey
Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.
Bioorganic & medicinal chemistry letters 2006;16(4):989-94.
2006: Ho-Jane Shue; Xiao Chen; John H Schwerdt; Sunil Paliwal; David J Blythin; Ling Lin; Danlin Gu; Cheng Wang; Gregory A Reichard; Hongwu Wang; John J Piwinski; Ruth A Duffy; Jean E Lachowicz; Vicki L Coffin; Amin A Nomeir; Cynthia A Morgan; Geoffrey Varty; Neng-Yang Shih
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.
Bioorganic & medicinal chemistry letters 2006;16(4):1065-9.
2006: Wayne D Vaccaro; Rosy Sher; Michael Berlin; Neng-Yang Shih; Robert Aslanian; John H Schwerdt; Kevin D McCormick; John J Piwinski; Robert E West; John C Anthes; Shirley M Williams; Ren-Long Wu; H Susan She; Maria A Rivelli; Jennifer C Mutter; Michel R Corboz; John A Hey; Leonard Favreau
Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
Bioorganic & medicinal chemistry letters 2006;16(2):395-9.
2005: Ho-Jane Shue; Xiao Chen; Neng-Yang Shih; David J Blythin; Sunil Paliwal; Ling Lin; Danlin Gu; John H Schwerdt; Sapna Shah; Gregory A Reichard; John J Piwinski; Ruth A Duffy; Jean E Lachowicz; Vicki L Coffin; Fei Liu; Amin A Nomeir; Cynthia A Morgan; Geoffrey Varty
Cyclic urea derivatives as potent NK1 selective antagonists.
Bioorganic & medicinal chemistry letters 2005;15(17):3896-9.
2005: Brian Lavey; Joseph A Kozlowski; R William Hipkin; Waldemar Gonsiorek; Daniel Lundell; John J Piwinski; Satwant K Narula; Charles A Lunn
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.
Bioorganic & medicinal chemistry letters 2005;15(3):783-6.
2003: Gregory A Reichard; Carmine Stengone; Sunil Paliwal; Ingrid Mergelsberg; Sapna Majmundar; Cheng Wang; Robert Tiberi; Andrew T McPhail; John J Piwinski; Neng-Yang Shih
Asymmetric synthesis of 4,4-disubstituted-2-imidazoli-dinones: potent NK1 antagonists.
Organic letters 2003;5(23):4249-51.
2003: Robert Aslanian; Mwangi wa Mutahi; Neng-Yang Shih; John J Piwinski; Robert West; Shirley M Williams; Susan She; Ren-Long Wu; John A Hey
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.
Bioorganic & medicinal chemistry letters 2003;13(12):1959-61.
2002: David J Blythin; Xiao Chen; John J Piwinski; Neng-Yang Shih; Ho-Jane Shue; John C Anthes; Andrew T McPhail
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.
Bioorganic & medicinal chemistry letters 2002;12(21):3161-5.
2002: Gregory A Reichard; Cheryl A Grice; Neng-Yang Shih; James Spitler; Sapna Majmundar; Steven D Wang; Sunil Paliwal; John C Anthes; John J Piwinski
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.
Bioorganic & medicinal chemistry letters 2002;12(17):2355-8.
2002: John C Anthes; Richard W Chapman; Christian Richard; Stephen Eckel; Michel R Corboz; John A Hey; Xiomara Fernandez; Scott Greenfeder; Robbie McLeod; Susan J Sehring; Charles Rizzo; Yvette Crawley; Neng-Yang Shih; John J Piwinski; Gregory A Reichard; Pauline C Ting; Nicholas I Carruthers; Francis M Cuss; Motasim Billah; William Kreutner; Robert W Egan
SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.
European journal of pharmacology 2002;450(2):191-202.
2002: Pauline C Ting; Joe F Lee; Neng-Yang Shih; John J Piwinski; John C Anthes; Richard W Chapman; Charles A Rizzo; John A Hey; Kwokei Ng; Amin A Nomeir
Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist.
Bioorganic & medicinal chemistry letters 2002;12(16):2125-8.
2002: Motasim Billah; Nicola Cooper; Michael Minnicozzi; Julie B H Warneck; Peng Wang; John A Hey; William Kreutner; Charles A Rizzo; Sidney R Smith; Simon Young; Richard W Chapman; Hazel J Dyke; Neng-Yang Shih; John J Piwinski; Francis M Cuss; John G Montana; Ashit K Ganguly; Robert W Egan
Pharmacology of N-(3,5-dichloro-1-oxido-4-pyridinyl)-8-methoxy-2-(trifluoromethyl)-5-quinoline carboxamide (SCH 351591), a novel, orally active phosphodiesterase 4 inhibitor.
The Journal of pharmacology and experimental therapeutics 2002;302(1):127-37.
2002: Motasim Billah; Nicola Cooper; Francis M Cuss; Richard Davenport; Hazel J Dyke; Robert Egan; Ashit Ganguly; Lewis Gowers; Duncan R Hannah; Alan F Haughan; Hannah J Kendall; Christopher Lowe; Michael Minnicozzi; John G Montana; Robert J Naylor; Janet Oxford; Joanna C Peake; John J Piwinski; Karen A Runcie; Verity Sabin; Andrew Sharpe; Neng-Yang Shih; Julie B H Warneck
Synthesis and profile of SCH351591, a novel PDE4 inhibitor.
Bioorganic & medicinal chemistry letters 2002;12(12):1621-3.
2002: Motasim Billah; George M Buckley; Nicola Cooper; Hazel J Dyke; Robert Egan; Ashit Ganguly; Lewis Gowers; Alan F Haughan; Hannah J Kendall; Christopher Lowe; Michael Minnicozzi; John G Montana; Janet Oxford; Joanna C Peake; C Louise Picken; John J Piwinski; Robert J Naylor; Verity Sabin; Neng-Yang Shih; Julie B H Warneck
8-Methoxyquinolines as PDE4 inhibitors.
Bioorganic & medicinal chemistry letters 2002;12(12):1617-9.
2002: Robert Aslanian; Mwangi wa Mutahi; Neng-Yang Shih; Kevin D McCormick; John J Piwinski; Pauline C Ting; Margaret M Albanese; Michael Berlin; Xiaohong Zhu; Shing-Chung Wong; Stuart B Rosenblum; Yueheng Jiang; Robert West; Susan She; Shirley M Williams; Matthew Bryant; John A Hey
Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.
Bioorganic & medicinal chemistry letters 2002;12(6):937-41.
2002: Gregory A Reichard; James Spitler; Robert Aslanian; Mwangi wa Mutahi; Neng-Yang Shih; Ling Lin; Pauline C Ting; John C Anthes; John J Piwinski
Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.
Bioorganic & medicinal chemistry letters 2002;12(5):833-6.
2002: Neng-Yang Shih; Margaret M Albanese; John C Anthes; Nicholas I Carruthers; Cheryl A Grice; Ling Lin; Pietro Mangiaracina; Gregory A Reichard; John H Schwerdt; Vera Seidl; Shing-Chung Wong; John J Piwinski
Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides.
Bioorganic & medicinal chemistry letters 2002;12(2):141-5.
2001: Pauline C Ting; Joe F Lee; John C Anthes; Neng-Yang Shih; John J Piwinski
Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors.
Bioorganic & medicinal chemistry letters 2001;11(4):491-4.
2000: Pauline C Ting; Joe F Lee; John C Anthes; Neng-Yang Shih; John J Piwinski
Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.
Bioorganic & medicinal chemistry letters 2000;10(20):2333-5.
2000: Gregory A Reichard; Z T Ball; Robert Aslanian; John C Anthes; Neng-Yang Shih; John J Piwinski
The design and synthesis of novel NK1/NK2 dual antagonists.
Bioorganic & medicinal chemistry letters 2000;10(20):2329-32.
1999: Corey L Strickland; Patricia C Weber; William T Windsor; Z Wu; Hung Le; M M Albanese; CS Alvarez; D Cesarz; JD del Rosario; J Deskus; AK Mallams; F George Njoroge; John J Piwinski; SW Remiszewski; RR Rossman; Arthur G Taveras; Bancha Vibulbhan; Ronald J Doll; Viyyoor Girijavallabhan; Ashit K Ganguly
Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.
Journal of medicinal chemistry 1999;42(12):2125-35.
1998: John J Piwinski; JK Wong; MJ Green; James J Kaminski; F Colizzo; Margaret M Albanese; Ashit K Ganguly; Motasim Billah; John C Anthes; Robert E West
Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.
Bioorganic & medicinal chemistry letters 1998;8(24):3469-74.
1998: Neng-Yang Shih; Robert Aslanian; A T Lupo; S Orlando; John J Piwinski; MJ Green; Ashit K Ganguly; Robert West; S Tozzi; William Kreutner; John A Hey
Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.
Bioorganic & medicinal chemistry letters 1998;8(3):243-8.
1997: F George Njoroge; Ronald J Doll; Bancha Vibulbhan; CS Alvarez; W Robert Bishop; J Petrin; Paul Kirschmeier; Nicholas I Carruthers; JK Wong; M M Albanese; John J Piwinski; JJ Catino; Viyyoor Girijavallabhan; Ashit K Ganguly
Discovery of novel nonpeptide tricyclic inhibitors of Ras farnesyl protein transferase.
Bioorganic & medicinal chemistry 1997;5(1):101-13.
1995: Neng-Yang Shih; A T Lupo; Robert Aslanian; S Orlando; John J Piwinski; M J Green; Ashit K Ganguly; M A Clark; S Tozzi; William Kreutner
A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist.
Journal of medicinal chemistry 1995;38(10):1593-9.
1991: Motasim Billah; Robert W Egan; Ashit K Ganguly; M J Green; William Kreutner; John J Piwinski; M I Siegel; F J Villani; J K Wong
Discovery and preliminary pharmacology of Sch 37370, a dual antagonist of PAF and histamine.
Lipids 1991;26(12):1172-4.
1991: John J Piwinski; J K Wong; M J Green; Ashit K Ganguly; Motasim Billah; Robert E West; William Kreutner
Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines.
Journal of medicinal chemistry 1991;34(1):457-61.
1990: Motasim Billah; Richard W Chapman; Robert W Egan; HELEN CAROL GILCHREST; John J Piwinski; J Sherwood; M I Siegel; Robert E West; William Kreutner
Sch 37370: a potent, orally active, dual antagonist of platelet-activating factor and histamine.
The Journal of pharmacology and experimental therapeutics 1990;252(3):1090-6.