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pro vyhledávání: '"H. Schwerdt"'
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Autor:
Samuel Wainhaus, Sang Q. Lam, Rongze Kuang, Paul M. McNicholas, Andrew J. Zych, Joe F. Lee, Gang Zhou, Todd A. Black, R. Jason Herr, Robert G. Aslanian, John H. Schwerdt, David Won-Shik Kim, Scott S. Walker, Jinhai Yang, Pauline C. Ting, He-Ping Wu, Yiming Xu, Jianhua Cao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2890-2893
A novel series of pyridazinone analogs has been developed as potent β-1,3-glucan synthase inhibitors through structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one (1). The ef
Autor:
Jianhua Cao, Anthony Cacciapuoti, Gang Zhou, Yiming Xu, Robert G. Aslanian, David Won-Shik Kim, Todd A. Black, Pauline C. Ting, He-Ping Wu, Scott S. Walker, Rongze Kuang, Samuel Wainhaus, Paul M. McNicholas, Joe F. Lee, John H. Schwerdt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1819-1822
A structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one 1 has resulted in the identification of 2-(3,5-difluorophenyl)-4-(3-fluorocyclopentyloxy)-5-[4-(isopropylsulfonyl)piper
Autor:
Piwinski John J, Chander S. Celly, Rongze Kuang, Ping Wu, Pauline C. Ting, Ling Lin, Li Xiao, David J. Blythin, John H. Schwerdt, Xiang Zhang, Ho-Jane Shue, M. Motasim Billah, Xiaohong Zhu, Michael Minnicozzi, Ji Zhang, Neng-Yang Shih, Daniel Prelusky, Peng Wang, Robert G. Aslanian, Danlin Gu, Xiao Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5150-5154
Substituted quinolyl oxazoles were discovered as a novel and highly potent series of phosphodiesterase 4 (PDE4) inhibitors. Structure-activity relationship studies revealed that the oxazole core, with 4-carboxamide and 5-aminomethyl groups, is a nove
Publikováno v:
Journal of Pharmaceutical and Biomedical Analysis. 40:799-804
Packed-column supercritical fluid chromatography (pSFC) coupled to an atmospheric pressure chemical ionization (APCI) source and a tandem mass spectrometer (MS/MS) for rapid and simultaneous determination of clozapine, ondansetron, tolbutamide and pr
Autor:
Jean E. Lachowicz, Ruth A. Duffy, Ling Lin, Vicki L. Coffin, Neng-Yang Shih, Danlin Gu, Geoffrey B. Varty, Piwinski John J, Ho-Jane Shue, Cynthia A. Morgan, Gregory A. Reichard, David J. Blythin, John H. Schwerdt, Xiao Chen, Sapna S. Shah, Amin A. Nomeir, Sunil Paliwal, Fei Liu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3896-3899
A series of novel five- and six-membered ring urea derivatives have been described as potent and selective NK1 receptor antagonists. Several compounds in this series exhibited good oral activity and brain penetration. Syntheses of these compounds are
Autor:
H. Schwerdt
Dieser Buchtitel ist Teil des Digitalisierungsprojekts Springer Book Archives mit Publikationen, die seit den Anfängen des Verlags von 1842 erschienen sind. Der Verlag stellt mit diesem Archiv Quellen für die historische wie auch die disziplingesch
Publikováno v:
Chirality. 8:364-371
The antipsoriatic 10-(3-chlorophenyl)-6,8,9,10-tetrahydrobenzo[b][1,8] naphthyridin-5(7H)-one, Sch 40120, is chiral only because it lacks planarity and possesses a stereogenic axis. It comprises short-lived, interconverting atropisomeric enantiomers
Autor:
R. Jason Herr, He-Ping Wu, Jianhua Cao, David Won-Shik Kim, Gang Zhou, Samuel Wainhaus, John H. Schwerdt, Robert G. Aslanian, Sang Q. Lam, David M. Jenkins, Scott S. Walker, Yiming Xu, Andrew J. Zych, Joe F. Lee, Samuel A. Sakwa, Jinhai Yang, Rongze Kuang, Pauline C. Ting, Paul M. McNicholas, Anthony Cacciapuoti, Todd A. Black
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(16)
A detailed structure–activity relationship study of a novel series of pyridazine-based small molecule glucan synthase inhibitors is described. The optimization of the PK profile of this series led to the discovery of compound 11g, which demonstrate
Autor:
Pauline C. Ting, Motasim Billah, Ji Zhang, Peng Wang, Daniel Prelusky, David J. Blythin, John H. Schwerdt, John J. Piwinski, Ling Lin, Li Xiao, Xiao Chen, Xiang Zhang, Ho-Jane Shue, Neng-Yang Shih, Jianhua Cao, Ping Wu, Chander S. Celly, Rongze Kuang, Robert G. Aslanian, Danlin Gu
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(7)
Optimization of oxazole-based PDE4 inhibitors has led to the discovery of a series of quinolyl oxazoles, with 4-benzylcarboxamide and 5-α-aminoethyl groups which exhibit picomolar potency against PDE4. Selectivity profiles and in vivo biological act