Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Nianhe Han"'
Autor:
Jun Tang, Erjuan Wang, Zhimin Jin, Kevin W. Brown, David M. Irlbeck, Jerry L. Jeffery, Rui Li, Heping Yang, Cristin M. Galardi, Sonia R. Miranda, Bin Shen, Charlene B. McDanal, Yajun Yu, Daxin Gao, Brian A. Johns, Chunyu Liu, Yongyong Wu, Yufei Sun, Caiming Xi, Nianhe Han, Stacey A. Jones
Publikováno v:
The Open Medicinal Chemistry Journal
A macrocycle provides diverse functionality and stereochemical complexity in a conformationally preorganized ring structure, and it occupies a unique chemical space in drug discovery. However, the synthetic challenge to access this structural class i
Autor:
Maurice Emery, Rod Cupples, David J. St. Jean, George A. Moniz, David Pyring, Randall W. Hungate, Chester Chenguang Yuan, Lars Johansson, Aiwen Li, Michelle Chen, Qingyian Liu, Meredith Williams, Steven R. Jordan, Lynn Cai, Lars Tedenborg, Minghan Wang, Christopher H. Fotsch, Nianhe Han, Michael D. Bartberger, Jiandong Zhang, Clarence Hale, Yaxiong Sun, Ben C. Askew
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6056-6061
A series of 2-anilinothiazolones were prepared as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). The most potent compounds contained a 2-chloro or 2-fluoro group on the aniline ring with an isopropyl substituent on the 5-posi
Autor:
Burgess Laurence E, Leyla Arik, Chester Chenguang Yuan, Nianhe Han, Randall W. Hungate, Derin C. D'amico, David A. Mareska, Feng-Yin Hsieh, Eileen Johnson, Hong Sun, Qingyian Liu, Barton H. Manning, Bobby Riahi, Christopher H. Fotsch, Gloria Biddlecome, Mark H. Norman, Augustus Kamassah, Ming Huang, Richard Loeloff, Gondi N. Kumar, Andras Toro, Jian J. Chen, Jason Brooks Human, Hideo Suzuki, Robert D. Groneberg, Benny C. Askew, Aiwen Li, Gordon Ng, James Zhan, Kaustav Biswas, Dianna Lester-Zeiner, Hong Dong, David E. Clarke
Publikováno v:
Journal of Medicinal Chemistry. 50:2200-2212
The bradykinin B1 receptor is induced following tissue injury and/or inflammation. Antagonists of this receptor have been studied as promising candidates for treatment of chronic pain. We have identified aryl sulfonamides containing a chiral chroman
Autor:
Qingyian Liu, Randall W. Hungate, Rami Tamir, Shimin Xu, Elizabeth M. Doherty, James J. S. Treanor, Christopher H. Fotsch, Mark H. Norman, Lana Klionsky, Yunxin Bo, Nianhe Han, Ning Xi, Narender R. Gavva
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5211-5217
A thiazole derivative, 2-(2,6-dichlorobenzyl)-N-(4-isopropylphenyl) thiazole-4-carboxamide (1), was identified as a TRPV1 antagonist. We synthesized various thiazole analogs and evaluated them for their ability to block capsaicin- or acid-induced cal
Autor:
Nuria A. Tamayo, Shimin Xu, Michael G. Kelly, Duncan M. Smith, Ning Chen, Michelle Carmouche, Mark H. Norman, Martin H. Goldberg, James Davis, Christopher H. Fotsch, Clarence Hale, Ning Xi, Markian Stec, James W. Baumgartner, Premilla Arasasingham, Nianhe Han, Feng-Yin Hsieh, Qingyian Liu, Yunxin Bo, Anthony W. Bannon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1623-1627
The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Compounds from this set had binding and functional activities at MC4R less than 30 nM.
Autor:
Yuelie Lu, Ling Wang, Michael Handley, Ning Xi, Stephen Arvedson, Andrew Tasker, Jiandong Zhang, Tingjian Xiang, Osslund Timothy D, Celia Dominguez, Qi Huang, Liang Huang, David Powers, Nianhe Han, Gladys Nunez, Qingyian Liu, Jiawang Zhu, Shawn Eisenberg, Shimin Xu, Alexander S. Kiselyov, Richard Kendall
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2905-2909
Novel αvβ3 antagonists based on the N-aryl-γ-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for αvβ3 receptor with excellent selectivity against the structurally related αIIbβ3 receptor. Additional i
Autor:
William Karbon, Nianhe Han, Ning Chen, Mark H. Norman, Vincent Santora, John Kincaid, Clarence Hale, Longbin Liu, Ofir A. Moreno, Christopher H. Fotsch, Tracy J. Jenkins, Zhidong Chen, Ray Hurt, Jennifer D. Sonnenberg, Yuelie Lu
Publikováno v:
Journal of Medicinal Chemistry. 43:4288-4312
Neuropeptide Y (NPY) has been shown to play an important role in the regulation of food intake and energy balance. Pharmacological data suggests that the Y5 receptor subtype contributes to the effects of NPY on appetite, and therefore a Y5 antagonist
Autor:
Dale L. Boger, Christine M. Tarby, Paul A. Kitos, Jeffrey A. McKie, Nianhe Han, Haiqiong W. Riggs
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:659-664
A quantitative Hammett study of the magnitude of the electronic effects of a C7 substituent on the functional reactivity of N-BOC-CBI (5, RH), its impact on biological properties, details of the mechanism of the acid-catalyzed nucleophilic additio
Publikováno v:
Bioorganic & Medicinal Chemistry. 3:1429-1453
An extensive study of analogs of the potent antitumor antibiotics CC-1065 and the duocarmycins which incorporate the 1,2,9,9 a -tetrahydrocyclopropa[c]benz [e]indol-4-one (CBI) alkylation subunit are detailed. In contrast to early speculation, deep-s
Publikováno v:
Journal of the American Chemical Society. 117:4881-4893
The product distributions produced by the photoinduced dichlorination of n-dodecane (nD) and the photoinduced monochlorination of 1 -chlorododecane (1CD) adsorbed on two pentasil zeolites (silicalite and LZ- 105) have been investigated. The results a