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Christopher Fotsch

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TOP 3
David J St Jean; Christopher Fotsch
Mitigating heterocycle metabolism in drug discovery.
Kate S Ashton; Christopher Fotsch; John G Allen; Matthew R Lee; Julie A Lofgren; Steve F Poon; David J St Jean; Shiwen Zhang; Xiaoling Zhang; Randall W Hungate
Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.
Jian Jeffrey Chen; Thomas Nguyen; Derin C D'Amico; Wenyuan Qian; Jason Human; Toshihiro Aya; Kaustav Biswas; Christopher Fotsch; Nianhe Han; Qingyian Liu; Nobuko Nishimura; Tanya A N Peterkin; Kevin Yang; Jiawang Zhu; Babak Bobby Riahi; Randall W Hungate; Neil G Andersen; John T Colyer; Margaret M Faul; Augustus Kamassah; Judy Wang; Janan Jona; Gondi Kumar; Eileen Johnson; Benny C Askew
3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.

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All Publications

2012: David J St Jean; Christopher Fotsch
Mitigating heterocycle metabolism in drug discovery.
Journal of medicinal chemistry 2012;55(13):6002-20.
2011: Kate S Ashton; Christopher Fotsch; John G Allen; Matthew R Lee; Julie A Lofgren; Steve F Poon; David J St Jean; Shiwen Zhang; Xiaoling Zhang; Randall W Hungate
Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.
Bioorganic & medicinal chemistry letters 2011;21(18):5191-6.
2011: Jian Jeffrey Chen; Thomas Nguyen; Derin C D'Amico; Wenyuan Qian; Jason Human; Toshihiro Aya; Kaustav Biswas; Christopher Fotsch; Nianhe Han; Qingyian Liu; Nobuko Nishimura; Tanya A N Peterkin; Kevin Yang; Jiawang Zhu; Babak Bobby Riahi; Randall W Hungate; Neil G Andersen; John T Colyer; Margaret M Faul; Augustus Kamassah; Judy Wang; Janan Jona; Gondi Kumar; Eileen Johnson; Benny C Askew
3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.
Bioorganic & medicinal chemistry letters 2011;21(11):3384-9.
2011: Charles Henley; Yuhua Yang; James Davis; Jenny Ying Lin Lu; Sean Morony; Wei Fan; Monica Florio; Banghua Sun; Edward Shatzen; James K Pretorius; William G Richards; David J St Jean; Christopher Fotsch; Jeff D Reagan
Discovery of a calcimimetic with differential effects on parathyroid hormone and calcitonin secretion.
The Journal of pharmacology and experimental therapeutics 2011;337(3):681-91.
2010: Paul E Harrington; David J St Jean; Jeffrey Clarine; Thomas S Coulter; Michael Croghan; Adam Davenport; James Davis; Chiara Ghiron; Jonathan Hutchinson; Michael G Kelly; Fred Lott; Jenny Ying-Lin Lu; David Martin; Sean Morony; Steve F Poon; Elena Portero-Larragueta; Jeff D Reagan; Kelly A Regal; Andrew Tasker; Minghan Wang; Yuhua Yang; Guomin Yao; Qingping Zeng; Charles Henley; Christopher Fotsch
The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core.
Bioorganic & medicinal chemistry letters 2010;20(18):5544-7.
2010: Qingyian Liu; Wenyuan Qian; Aiwen Li; Kaustav Biswas; Jian Jeffrey Chen; Christopher Fotsch; Nianhe Han; Chester Yuan; Leyla Arik; Gloria Biddlecome; Eileen Johnson; Gondi Kumar; Dianna Lester-Zeiner; Gordon Y Ng; Randall W Hungate; Benny C Askew
Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2010;20(15):4593-7.
2010: Murielle M Véniant; Clarence Hale; Randall W Hungate; Kyung Gahm; Maurice G Emery; Janan Jona; Smriti Joseph; Jeffrey Adams; Andrew Hague; George Moniz; Jiandong Zhang; Michael D Bartberger; Vivian Li; Rashid Syed; Steven Jordan; Renée Komorowski; Michelle M Chen; Rod Cupples; Ki Won Kim; David J St Jean; Lars Johansson; Martin A Henriksson; Meredith Williams; Jerk Vallgårda; Christopher Fotsch; Minghan Wang
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Journal of medicinal chemistry 2010;53(11):4481-7.
2010: John G Allen; Christopher Fotsch; Philip Babij
Emerging targets in osteoporosis disease modification.
Journal of medicinal chemistry 2010;53(11):4332-53.
2010: Raju Subramanian; Matthew R Lee; John G Allen; Matthew P Bourbeau; Christopher Fotsch; Fang-Tsao Hong; Seifu Tadesse; Guomin Yao; Chester C Yuan; Sekhar Surapaneni; Gary L Skiles; Xianghong Wang; G Erich Wohlhieter; Qingping Zeng; Yihong Zhou; Xiaochun Zhu; Chun Li
Cytochrome P450-mediated epoxidation of 2-aminothiazole-based AKT inhibitors: identification of novel GSH adducts and reduction of metabolic activation through structural changes guided by in silico and in vitro screening.
Chemical research in toxicology 2010;23(3):653-63.
2010: Qingping Zeng; John G Allen; Matthew P Bourbeau; Xianghong Wang; Guomin Yao; Seifu Tadesse; James T Rider; Chester C Yuan; Fang-Tsao Hong; Matthew R Lee; Shiwen Zhang; Julie A Lofgren; Daniel J Freeman; Suijin Yang; Chun Li; Elizabeth Tominey; Xin Huang; Douglas Hoffman; Harvey K Yamane; Christopher Fotsch; Celia Dominguez; Randall W Hungate; Xiaoling Zhang
Azole-based inhibitors of AKT/PKB for the treatment of cancer.
Bioorganic & medicinal chemistry letters 2010;20(5):1559-64.
2009: Steve F Poon; David J St Jean; Paul E Harrington; Charles Henley; James Davis; Sean Morony; Fred D Lott; Jeff D Reagan; Jenny Ying-Lin Lu; Yuhua Yang; Christopher Fotsch
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
Journal of medicinal chemistry 2009;52(21):6535-8.
2009: Murielle Véniant; Clarence Hale; R Komorowski; M M Chen; D J St Jean; Christopher Fotsch; Minghan Wang
Time of the day for 11beta-HSD1 inhibition plays a role in improving glucose homeostasis in DIO mice.
Diabetes, obesity & metabolism 2009;11(2):109-17.
2008: Christopher Fotsch; Michael D Bartberger; Eric A Bercot; Michelle Chen; Rod Cupples; Maury Emery; Jenne Fretland; Anil Guram; Clarence Hale; Nianhe Han; Dean Hickman; Randall W Hungate; Michael Hayashi; Renee Komorowski; Qingyian Liu; Guy Matsumoto; David J St Jean; Stefania Ursu; Murielle Véniant; Guifen Xu; Qiuping Ye; Chester Yuan; Jiandong Zhang; Xiping Zhang; Hua Tu; Minghan Wang
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Journal of medicinal chemistry 2008;51(24):7953-67.
2008: Christopher Fotsch; Minghan Wang
Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes.
Journal of medicinal chemistry 2008;51(16):4851-7.
2008: Lars Johansson; Christopher Fotsch; Michael D Bartberger; Victor M Castro; Michelle Chen; Maurice Emery; Sonja Gustafsson; Clarence Hale; Dean Hickman; Evert Homan; Steven R Jordan; Renee Komorowski; Aiwen Li; Kenneth McRae; George Moniz; Guy Matsumoto; Carlos Orihuela; Gunnar Palm; Murielle Veniant; Minghan Wang; Meredith Williams; Jiandong Zhang
2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.
Journal of medicinal chemistry 2008;51(10):2933-43.
2008: Clarence Hale; Murielle Véniant; Zhulun Wang; Michelle Chen; Jocelyn McCormick; Rod Cupples; Dean Hickman; Xiaoshan Min; Athena Sudom; Haoda Xu; Guy Matsumoto; Christopher Fotsch; David J St Jean; Minghan Wang
Structural characterization and pharmacodynamic effects of an orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor.
Chemical biology & drug design 2008;71(1):36-44.
2007: Chester Yuan; David J St Jean; Qingyian Liu; Lynn Cai; Aiwen Li; Nianhe Han; George Moniz; Benny C Askew; Randall W Hungate; Lars Johansson; Lars Tedenborg; David Pyring; Meredith Williams; Clarence Hale; Michelle Chen; Rod Cupples; Jiandong Zhang; Steven Jordan; Michael D Bartberger; Yaxiong Sun; Maurice Emery; Minghan Wang; Christopher Fotsch
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(22):6056-61.
2007: Elizabeth M Doherty; Christopher Fotsch; Anthony W Bannon; Yunxin Bo; Ning Chen; Celia Dominguez; James Falsey; Narender R Gavva; Jodie Katon; Thomas Nixey; Vassil I Ognyanov; Liping Pettus; Robert M Rzasa; Markian Stec; Sekhar Surapaneni; Rami Tamir; Jiawang Zhu; James J S Treanor; Mark H Norman
Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Journal of medicinal chemistry 2007;50(15):3515-27.
2007: Mark H Norman; Jiawang Zhu; Christopher Fotsch; Yunxin Bo; Ning Chen; Partha P Chakrabarti; Elizabeth M Doherty; Narender R Gavva; Nobuko Nishimura; Thomas Nixey; Vassil I Ognyanov; Robert M Rzasa; Markian Stec; Sekhar Surapaneni; Rami Tamir; Vellarkad Viswanadhan; James J S Treanor
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
Journal of medicinal chemistry 2007;50(15):3497-514.
2007: Katarina Flyrén; Lars O Bergquist; Victor M Castro; Christopher Fotsch; Lars Johansson; David J St Jean; Lori Sutin; Meredith Williams
Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(12):3421-5.
2007: Derin C D'Amico; Toshi Aya; Jason Human; Christopher Fotsch; Jian Jeffrey Chen; Kaustav Biswas; Bobby Riahi; Mark H Norman; Christopher A Willoughby; Randall W Hungate; Paul J Reider; Gloria Biddlecome; Dianna Lester-Zeiner; Carlo Van Staden; Eileen Johnson; Augustus Kamassah; Leyla Arik; Judy Wang; Vellarkad Viswanadhan; Robert D Groneberg; James Zhan; Hideo Suzuki; Andras Toro; David A Mareska; David E Clarke; Darren M Harvey; Laurence E Burgess; Ellen R Laird; Benny C Askew; Gordon Ng
Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.
Journal of medicinal chemistry 2007;50(4):607-10.
2007: David J St Jean; Chester Yuan; Eric Bercot; Rod Cupples; Michelle Chen; Jenne Fretland; Clarence Hale; Randall W Hungate; Renee Komorowski; Murielle Veniant; Minghan Wang; Xiping Zhang; Christopher Fotsch
2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.
Journal of medicinal chemistry 2007;50(3):429-32.
2007: Paul E Harrington; Christopher Fotsch
Calcium sensing receptor activators: calcimimetics.
Current medicinal chemistry 2007;14(28):3027-34.
2006: Minghan Wang; Christopher Fotsch
Small-molecule compounds that modulate lipolysis in adipose tissue: targeting strategies and molecular classes.
Chemistry & biology 2006;13(10):1019-27.
2006: Vassil I Ognyanov; Chenera Balan; Anthony W Bannon; Yunxin Bo; Celia Dominguez; Christopher Fotsch; Vijay K Gore; Lana Klionsky; Vu V Ma; Yi-Xin Qian; Rami Tamir; Xianghong Wang; Ning Xi; Shimin Xu; Dawn Zhu; Narender R Gavva; James J S Treanor; Mark H Norman
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
Journal of medicinal chemistry 2006;49(12):3719-42.
2006: Christopher Fotsch; Gloria Biddlecome; Kaustav Biswas; Jian Jeff Chen; Derin C D'Amico; Robert D Groneberg; Nianhe Bruce Han; Feng-Yin Hsieh; Augustus Kamassah; Gondi Kumar; Dianna Lester-Zeiner; Qingyian Liu; David A Mareska; Babak Bobby Riahi; Yueh-Ju Judy Wang; Kevin Yang; James Zhan; Joe Zhu; Eileen Johnson; Gordon Ng; Benny C Askew
A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.
Bioorganic & medicinal chemistry letters 2006;16(8):2071-5.
2005: Ning Xi; Yunxin Bo; Elizabeth M Doherty; Christopher Fotsch; Narender R Gavva; Nianhe Han; Randall W Hungate; Lana Klionsky; Qingyian Liu; Rami Tamir; Shimin Xu; James J S Treanor; Mark H Norman
Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists.
Bioorganic & medicinal chemistry letters 2005;15(23):5211-7.
2005: Christopher Fotsch; Nianhe Han; Premilla Arasasingham; Yunxin Bo; Michelle Carmouche; Ning Chen; James Davis; Martin H Goldberg; Clarence Hale; Feng-Yin Hsieh; Michael G Kelly; Qingyian Liu; Mark H Norman; Duncan M Smith; Markian Stec; Nuria A Tamayo; Ning Xi; Shimin Xu; Anthony W Bannon; James W Baumgartner
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Bioorganic & medicinal chemistry letters 2005;15(6):1623-7.
2005: Elizabeth M Doherty; Christopher Fotsch; Yunxin Bo; Partha P Chakrabarti; Ning Chen; Narender R Gavva; Nianhe Han; Michael G Kelly; John Kincaid; Lana Klionsky; Qingyian Liu; Vassil I Ognyanov; Rami Tamir; Xianghong Wang; Jiawang Zhu; Mark H Norman; James J S Treanor
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
Journal of medicinal chemistry 2005;48(1):71-90.
2004: Ning Xi; Clarence Hale; Michael G Kelly; Mark H Norman; Markian Stec; Shimin Xu; James W Baumgartner; Christopher Fotsch
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.
Bioorganic & medicinal chemistry letters 2004;14(2):377-81.
2003: Christopher Fotsch; Duncan M Smith; Jeffrey A Adams; Janet Cheetham; Michael Croghan; Elizabeth M Doherty; Clarence Hale; Mark Jarosinski; Michael G Kelly; Mark H Norman; Nuria A Tamayo; Ning Xi; James W Baumgartner
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).
Bioorganic & medicinal chemistry letters 2003;13(14):2337-40.
2003: Premilla N Arasasingham; Christopher Fotsch; Xiaohu Ouyang; Mark H Norman; Michael G Kelly; Kevin L Stark; Bill Karbon; Clarence Hale; James W Baumgartner; Martha Zambrano; Janet Cheetham; Nuria A Tamayo
Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.
Journal of medicinal chemistry 2003;46(1):9-11.
2001: Christopher Fotsch; J D Sonnenberg; Ning Chen; Clarence Hale; W Karbon; Mark H Norman
Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists.
Journal of medicinal chemistry 2001;44(14):2344-56.
2000: Mark H Norman; Ning Chen; Z Chen; Christopher Fotsch; Clarence Hale; Nianhe Han; R Hurt; T Jenkins; J Kincaid; L Liu; Y Lu; O Moreno; Vincent J Santora; J D Sonnenberg; W Karbon
Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists.
Journal of medicinal chemistry 2000;43(22):4288-312.
2000: N Chen; Y Lu; K Gadamasetti; C R Hurt; Mark H Norman; Christopher Fotsch
A short, facile synthesis of 5-substituted 3-amino-1H-pyrrole-2-carboxylates.
The Journal of organic chemistry 2000;65(8):2603-5.