Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Christopher A. Willoughby"'
The world's countries have committed to assure by 2030 reliable mobility to all, even in the largest cities. Review of experience of three fastest-growing cities in South Asian countries underlines reforms that will need to be applied very widely: mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05a082d029c50f734f310f02a23cc249
https://doi.org/10.4018/978-1-5225-2659-9.ch012
https://doi.org/10.4018/978-1-5225-2659-9.ch012
Autor:
Ana-Paz Marŕna, Antonio García Guzmán, Concepción García, Christopher R. Willoughby, Isabel Demestre
Publikováno v:
Arzneimittelforschung. 53:121-125
Embryotoxicity studies on irloxacin (6-fluorine-7-(pyrrol-1-yl)-1-ethyl-1,4-dihydro-4-oxo-quinolone-3-carboxylic acid, CAS-91524-15-1), a new fluoroquinolone antibacterial agent, were performed in rats and rabbits. Oral administration of irloxacin du
Autor:
Kenneth P. Ellsworth, Kevin T. Chapman, Wayne M. Geissler, Georgianna Harris, Robert W. Myers, Keith G. Rosauer, Anthony Ogawa, Qiaolin Deng, Christopher A. Willoughby, David E. Moller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4385-4388
The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.
Autor:
Kenneth P. Ellsworth, Robert W. Myers, Zhijian Lu, Richard Saperstein, Georgianna Harris, Brian M. McKeever, Wayne M. Geissler, Jun Yao, Kevin T. Chapman, Qiaolin Deng, Joann Bohn, Christopher A. Willoughby, Peggy E. McCann, Raynald Bergeron
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4125-4128
A new class of diacid analogues that binds at the AMP site not only are very potent but have approximately 10-fold selectivity in liver versus muscle glycogen phosphorylase (GP) in the in vitro assay. The synthesis, structure, and in vitro and in viv
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:
Madhumeeta J Dhar, Lorraine Malkowitz, Kevin T. Chapman, Kang Cheng, Steven M. Hutchins, Stephen G. Pacholok, Christopher A. Willoughby, Keith G. Rosauer, Gary G. Chicchi, David H. Weinberg, Sharon Sadowski, Smita Patel, Jerry Di Salvo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:93-96
Preparation and screening of mixture libraries based on a 2-arylindole scaffold resulted in the discovery of potent ligands for a variety of G-protein coupled receptors.
Autor:
Anthony Carella, Kevin T. Chapman, Christopher A. Willoughby, Martin S. Springer, Lorraine Malkowitz, Janet Lineberger, Emilio A. Emini, Karen Holmes, Keith G. Rosauer, Scott C. Berk, Gwen Carver, Michael W. Miller, Silvia Degrado, Sandra L. Gould, Daria J. Hazuda, Renee Danzeisen, Joseph Kessler, William A. Schleif
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:3137-3141
Herein we report the preparation of a combinatorial library of compounds with potent CCR5 binding affinity. The library design was aided by SAR generated in a traditional medicinal chemistry effort. Compounds with novel combinations of subunits were
Autor:
Christopher A. Willoughby, Wayne M. Geissler, Brian M. McKeever, Nancy A. Thornberry, Herb G. Bull, Joseph W. Becker, Margarita Garcia-Calvo, Jennifer Rotonda
Publikováno v:
Chemistry & Biology. 8:357-368
Background: Granzyme B, one of the most abundant granzymes in cytotoxic T-lymphocyte (CTL) granules, and members of the caspase (cysteine aspartyl proteinases) family have a unique cleavage specificity for aspartic acid in P1 and play critical roles
Autor:
Nigel P. Moore, Steven M. Fulcher, Christopher R. Willoughby, Robert A.J. Priston, Dianne M. Creasy, Julian A. Heath
Publikováno v:
Reproductive Toxicology. 14:427-450
Di-(C(7)-C(9) alkyl) phthalate (D79P) and di-(C(9)-C(11) alkyl) phthalate (D911P), based on high-normality linear oxo-alcohols, have been assessed for their impact upon reproductive performance in Sprague-Dawley rats. Rats were continuously exposed t
Publikováno v:
Tetrahedron Letters. 37:7181-7184
A method for the solid phase synthesis of aryl amines is reported. The method involves a palladium mediated coupling reaction between aryl bromides and amines. The products are isolated in high purity and good yields. This method should prove to be a