Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Doug W. Hobbs"'
Autor:
Xiaolian Xu, Seong Heon Kim, Qingbei Zeng, Joseph A. Kozlowski, Carolyn DiIanni Carroll, Neng-Yang Shih, Baldwin John J, Wensheng Yu, Yueheng Jiang, Guizhen Dong, Yuefei Shao, Brian F. Mcguinness, Gopinadhan N. Anilkumar, Lisa Guise Zawacki, Doug W. Hobbs, Chung-Her Jenh, James W. Hall, Stuart B. Rosenblum, Bandarpalle B. Shankar, De-Yi Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6982-6986
The SAR of a novel pyrazinyl-piperazinyl-piperidine scaffold with CXCR3 receptor antagonist activity was explored. Optimization of the DMPK profile and reduction of hERG inhibition is described. Compound 16e with single-digit CXCR3 affinity, good rat
Autor:
James W. Janetka, William Nolan, Bradley Ford, Tom Ellenberger, Scott A. Wildman, Doug W. Hobbs, Scott J. Hultgren, Corinne K. Cusumano, Jerome S. Pinkner, Robert Obermann, Zhenfu Han
Publikováno v:
Journal of Medicinal Chemistry. 53:4779-4792
FimH-mediated cellular adhesion to mannosylated proteins is critical in the ability of uropathogenic E. coli (UPEC) to colonize and invade the bladder epithelium during urinary tract infection. We describe the discovery and optimization of potent sma
Autor:
Cangming Yang, Biji Jacob-Samuel, Doug W. Hobbs, Joseph A. Kozlowski, Lisa Guise Zawacki, Gopinadhan N. Anilkumar, Guizhen Dong, Carolyn DiIanni Carroll, Brian F. Mcguinness, Stuart B. Rosenblum, Chung-Her Jenh, James W. Hall
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5205-5208
High-throughput screening of an encoded combinatorial aryl piperazine library led to the identification of a novel series of potent piperazinyl-piperidine based CXCR3 antagonists. Analogs of the initial hit were synthesized via solid and solution pha
Autor:
Babu Suresh D, R. Kuvelkar, Yuhua Huang, A.W. Stamford, Qi Zhang, Lili Zhang, P. Gaspari, J. Pan, Wang Lingyan, L. Ozgur, Ge Li, Yusheng Wu, Johannes H. Voigt, Xiao Chen, Kurt W. Saionz, J. Lowrie, Tao Guo, Ulrich Iserloh, N.A. McHugh, D. Tadesse, Le Thuy X H, Matthew E. Kennedy, Doug W. Hobbs, Leonard Favreau, Carolyn DiIanni Carroll, Corey Strickland, Jared N. Cumming, Eric M. Parker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3236-3241
Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1718-1721
Melanin concentrating hormone (MCH) plays an important role in the regulation of food intake and energy balance in mammals. MCH-1 receptor (MCH1R) deficient mice are lean and resistant to diet-induced obesity. As such, MCH1R antagonists are believed
Autor:
Doug W. Hobbs, Tao Guo
Publikováno v:
Current Medicinal Chemistry. 13:1811-1829
Alzheimer's disease (AD) is a progressive neurodegenerative disease and the most common cause of dementia. The production and accumulation of beta-amyloid peptides (Abeta) from the beta-amyloid precursor protein (APP) are believed to play a key role
Publikováno v:
Current Computer Aided-Drug Design. 1:325-345
With recent estimates of drug development costs on the order of $800 million and increased pressure to reduce consumer drug costs, it is not surprising that the pharmaceutical industry is keenly interested in reducing the overall expense associated w
Autor:
Doug W. Hobbs, David J. Diller
Publikováno v:
Journal of Medicinal Chemistry. 47:6373-6383
Deriving general knowledge from high-throughput screening data is made difficult by the significant amount of noise, arising primarily from false positives, in the data. The paradigm established for screening an encoded combinatorial library on polym
Autor:
Wong Michael K C, Yueheng Jiang, Qingbei Zeng, Chung-Her Jenh, Stuart B. Rosenblum, De-Yi Yang, Yuefei Shao, Anilkumar G. Nair, Jingqi Duo, Doug W. Hobbs, Brian F. Mcguinness, Joseph A. Kozlowski, Lisa Guise Zawacki, Neng-Yang Shih, Carolyn DiIanni Carroll, Youheng Shu, Seong Heon Kim
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(4)
The structure-human CXCR3 binding affinity relationship of a series of pyridyl/pyrazinyl-piperazinyl-piperidine derivatives were explored with a focus to improve PK, hERG and metabolic profiles. Several small heterocycles were identified as amide sur
Autor:
Steven N. Gallicchio, James P. Guare, C. J. Woyden, Duane R. Reiss, Carl F. Homnick, Roger M. Freidinger, S Vickers, Michelle S. Kuo, E V Lis, Stuart R. Michelson, Douglas J. Pettibone, Peter D. Williams, Joseph M. Pawluczyk, Erb Jm, Doug W. Hobbs, Ian M. Bell, Rita A. Halpin, David J. Mathre, Maribeth T. Guidotti
Publikováno v:
Journal of Medicinal Chemistry. 41:2146-2163
The previously reported oxytocin antagonist L-371,257 (2) has been modified at its acetylpiperidine terminus to incorporate various pyridine N-oxide groups. This modification has led to the identification of compounds with improved pharmacokinetics a