J
Joseph DiBrino
Researcher at Pfizer
Publications - 12
Citations - 615
Joseph DiBrino is an academic researcher from Pfizer. The author has contributed to research in topics: Oleandomycin & Capromorelin. The author has an hindex of 10, co-authored 12 publications receiving 603 citations.
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Journal ArticleDOI
Synthesis, in vitro and in vivo activity of novel 9-deoxo-9a-AZA-9a-homoerythromycin A derivatives; a new class of macrolide antibiotics, the azalides.
G. Michael Bright,Arthur Adam Nagel,Jon Bordner,Desai Kishor A,Joseph DiBrino,Jolanta Nowakowska,Lawrence A. Vincent,Richard M. Watrous,Frank C. Sciavolino,Arthur R. English,James A. Retsema,M Anderson,Lori Brennan,Roberta J. Borovoy,Caroline R. Cimochowski,J A Faiella,Arthur E. Girard,Dennis Girard,Carol Herbert,Mary Manousos,Rachel J. Mason +20 more
TL;DR: The overall in vitro/in vivo performance of N-methyl, C- 4'' epimers 3a and 9; and C-4'' amine 11 identify these compounds as the most interesting erythromycin A-superior agents.
Journal ArticleDOI
Design and Synthesis of Novel FKBP Inhibitors
TL;DR: Small molecule FKBP inhibitors were prepared with inhibitory activity ranging from micromolar to nanomolar by a protocol which includes the synthesis of chiral propargylic amines and their subsequent conversion into vinyl zirconium reagents.
Journal ArticleDOI
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
David A. Griffith,John R. Hadcock,Shawn C Black,Philip A. Iredale,Philip A. Carpino,Paul DaSilva-Jardine,Robert F. Day,Joseph DiBrino,Robert L. Dow,Margaret S. Landis,Rebecca E. O’Connor,Dennis O. Scott +11 more
TL;DR: In vivo, compound 3a reversed cannabinoid agonist-mediated responses, reduced food intake, and increased energy expenditure and fat oxidation in rodents.
Journal ArticleDOI
Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin.
Philip A. Carpino,Bruce Allen Lefker,Steven M. Toler,Lydia C. Pan,John R. Hadcock,Ewell R. Cook,Joseph DiBrino,Anthony Michael Campeta,Shari L. DeNinno,K.L. Chidsey-Frink,Hada William Andrew,John Inthavongsay,F.Michael Mangano,Michelle A. Mullins,David F. Nickerson,Oicheng Ng,C.M. Pirie,John A. Ragan,Colin R. Rose,David A. Tess,Ann S. Wright,Li Yu,Michael P. Zawistoski,Paul DaSilva-Jardine,Theresa C. Wilson,David D. Thompson +25 more
TL;DR: In this article, pyrazolinone-piperidine dipeptide derivatives were synthesized and evaluated as growth hormone secretagogues (GHSs) for the treatment of musculoskeletal frailty in elderly adults.
Journal ArticleDOI
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.
Philip A. Carpino,David A. Griffith,Subas M. Sakya,Robert L. Dow,Shawn C Black,John R. Hadcock,Philip A. Iredale,Dennis O. Scott,Michael Fichtner,Colin R. Rose,Robert F. Day,Joseph DiBrino,Mary Butler,Demetria B. DeBartolo,Darrin Dutcher,Denise Gautreau,Jeff S. Lizano,Rebecca E. O’Connor,Michelle A. Sands,Dawn Kelly-Sullivan,Karen M. Ward +20 more
TL;DR: A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB(1)-R antagonists and inverse agonists, leading to the identification of two compounds with oral activity in rodent feeding models.