Zobrazeno 1 - 10
of 144
pro vyhledávání: '"Margaret A. Cascieri"'
Autor:
Richard Jiao, Pasquale P. Vicario, Gabor Butora, Shankaran Kothandaraman, Stephen D. Goble, Mary Struthers, Gregori J. Morriello, Julie A. DeMartino, Sander G. Mills, Malcolm MacCoss, Julia M. Ayala, Margaret A. Cascieri, Karla L. Donnely, Changyou Zhou, Lihu Yang, Alexander Pasternak
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1830-1834
A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found t
Autor:
Margaret A. Cascieri, Sander G. Mills, Malcolm MacCoss, Pasquale P. Vicario, H J Zweerink, William H. Parsons, Lihu Yang, Martin S. Springer, Liangqin Guo, Changyou Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:309-314
A series of racemic and homochiral α-aminothiazole-γ-aminobutyroamides that display high affinities for human and murine CCR2 and functional antagonism by inhibition of monocyte recruitment are described. A representative example is (2S)-2-[2-(acet
Autor:
Deodialsingh Guiadeen, William H. Parsons, Pasquale P. Vicario, Gregori J. Morriello, Malcolm MacCoss, Margaret A. Cascieri, Shankaran Kothandaraman, Alexander Pasternak, Lihu Yang, Gabor Butora
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4715-4722
A systematic examination of the central aromatic portion of the lead (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-(4-fluorophenyl)-4-(1′H-spiro[indene-1,4′-piperidin]-1′-yl)butanamide (9) led to the discovery of a novel class of CCR2 receptor anta
Autor:
Gary G. Chicchi, Paul E. Finke, Joseph M. Metzger, Dorothy Levorse, Malcolm MacCoss, Margaret A. Cascieri, D. Euan MacIntyre, Laura C. Meurer, Kwei-Lan Tsao, Sharon Sadowski, Sander G. Mills
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4497-4503
An initial investigation of the novel cyclopentane scaffold 6 afforded low nanomolar human NK1 antagonists having enhanced water solubility properties compared to morpholine 1. A synthesis of this cyclopentane scaffold, having three contiguous chiral
Autor:
Margaret A. Cascieri, Salvatore J. Siciliano, Karen Holmes, Sandra L. Gould, Kevin T. Chapman, William A. Schleif, J. J. Hale, Richard J. Budhu, Renee Danzeisen, Joseph Kessler, Anthony Carella, Julie A. DeMartino, Christopher A. Willoughby, Daria J. Hazuda, Sander G. Mills, Malcolm MacCoss, Michael W. Miller, Janet Lineberger, Emilio A. Emini, Lorraine Malkowitz, Keith G. Rosauer, Martin S. Springer, Gwen Carver
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:427-431
A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding affinity (1.8 nM) and antiviral activity in PBMC's (IC95=50 nM). Compound 4a also has impro
Autor:
Emilio A. Emini, Julie A. DeMartino, Salvatore J. Siciliano, Karen Holmes, Gwen Carver, Sandra L. Gould, Kevin T. Chapman, Anthony Carella, Renee Danzeisen, Michael W. Miller, Joseph Kessler, Malcolm MacCoss, Christopher L. Lynch, Daria J. Hazuda, Sander G. Mills, Janet Lineberger, Lorraine Malkowitz, Amy Gentry, Richard J. Budhu, Jeffrey J. Hale, William A. Schleif, Margaret A. Cascieri, Martin S. Springer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:3001-3004
A series of alpha-(pyrrolidin-1-yl)acetic acids is presented as selective and potent antivirals against HIV. Several of the pyrrolidine zwitterions demonstrated reasonable in vitro properties, enhanced antiviral activities and improved pharmacokineti
Autor:
Gary G. Chicchi, Barry R. Cunningham, Michelle K. Clements, Marc M. Kurtz, Ruiping Wang, Qingyun Liu, Christopher P. Austin, Margaret A. Cascieri
Publikováno v:
Gene. 296:205-212
Hemokinin-1 (HK-1) is a novel substance P (SP)-like peptide that is encoded by the preprotachykinin C (PPT-C) gene recently identified in mouse B cells and shown to be a potentially important regulator of B cell development (Nat. Immunol. 1 (2000) 39
Autor:
Margaret A. Cascieri
Publikováno v:
Nature Reviews Drug Discovery. 1:122-130
Although drugs that lead to cholesterol and lipid lowering have proved to have significant effects in lowering cardiovascular morbidity and mortality, coronary artery disease remains a principal cause of death worldwide. There is a clear need to disc
Autor:
Jerry Di Salvo, Allan D. Blake, Martin S. Springer, Julie A. DeMartino, Anna Sirotina-Meisher, Bruce L. Daugherty, Margaret A. Cascieri, Greg E. Koch, Kathleen A. Sullivan, Kristine E. Johnson, Yong Liu
Publikováno v:
European Journal of Pharmacology. 409:143-154
The α chemokine receptor CXCR4 and its only characterized chemokine ligand, stromal cell-derived factor-1 (SDF-1), are postulated to be important in the development of the B-cell arm of the immune system. In addition, CXCR4 is a critical coreceptor
Autor:
Linda Brockunier, Ann E. Weber, Suresh B. Singh, Michael H. Fisher, Mari R. Candelore, Yong Liu, Liping Deng, Laurie Tota, Margaret A. Cascieri, Jiafang He, Emma R. Parmee, Matthew J. Wyvratt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2283-2286
Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human beta3 adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta3 AR. Naphthyloxy compound 18 (bet