Qianping Peng
Merck & Co.
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Featured researches published by Qianping Peng.
Bioorganic & Medicinal Chemistry Letters | 2010
Jian Liu; Shuwen He; Tianying Jian; Peter H. Dobbelaar; Iyassu K. Sebhat; Linus S. Lin; Allan J. Goodman; Cheng Guo; Peter R. Guzzo; Mark Hadden; Alan J. Henderson; Kevin Pattamana; Megan Ruenz; Bruce J. Sargent; Brian Swenson; Larry Yet; Constantin Tamvakopoulos; Qianping Peng; Jie Pan; Yanqing Kan; Oksana C. Palyha; Theresa M. Kelly; Xiao-Ming Guan; Andrew D. Howard; Donald J. Marsh; Joseph M. Metzger; Marc L. Reitman; Matthew J. Wyvratt; Ravi P. Nargund
This Letter describes a series of potent and selective BRS-3 agonists containing a biarylethylimidazole pharmacophore. Extensive SAR studies were carried out with different aryl substitutions. This work led to the identification of a compound 2-{2-[4-(pyridin-2-yl)phenyl]ethyl}-5-(2,2-dimethylbutyl)-1H-imidazole 9 with excellent binding affinity (IC(50)=18 nM, hBRS-3) and functional agonist activity (EC(50)=47 nM, 99% activation). After oral administration, compound 9 had sufficient exposure in diet induced obese mice to demonstrate efficacy in lowering food intake and body weight via BRS-3 activation.
Bioorganic & Medicinal Chemistry Letters | 2010
Shuwen He; Peter H. Dobbelaar; Jian Liu; Tianying Jian; Iyassu K. Sebhat; Linus S. Lin; Allan J. Goodman; Cheng Guo; Peter R. Guzzo; Mark Hadden; Alan J. Henderson; Megan Ruenz; Bruce J. Sargent; Larry Yet; Theresa M. Kelly; Oksana C. Palyha; Yanqing Kan; Jie Pan; Howard Y. Chen; Donald J. Marsh; Lauren P. Shearman; Alison M. Strack; Joseph M. Metzger; Scott D. Feighner; Carina Tan; Andrew D. Howard; Constantin Tamvakopoulos; Qianping Peng; Xiao-Ming Guan; Marc L. Reitman
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3.
Bioorganic & Medicinal Chemistry Letters | 2010
Shuwen He; Zhixiong Ye; Peter H. Dobbelaar; Raman K. Bakshi; Qingmei Hong; James Dellureficio; Iyassu K. Sebhat; Liangqin Guo; Jian Liu; Tianying Jian; Yingjie Lai; Christopher L. Franklin; Mikhail Reibarkh; Mark A. Holmes; David H. Weinberg; Tanya MacNeil; Rui Tang; Constantin Tamvakopoulos; Qianping Peng; Randy R. Miller; Ralph A. Stearns; Howard Y. Chen; Airu S. Chen; Alison M. Strack; Tung M. Fong; Matthew J. Wyvratt; Ravi P. Nargund
We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses exceptional potency at MC4R and potent anti-obesity efficacy in a mouse model. However, the efficacy is not completely mediated through MC4R. Additional SAR studies led to the discovery of compound 32, which is more potent at MC4R. Compound 32 demonstrates MC4R mediated anti-obesity efficacy in rodent models.
Bioorganic & Medicinal Chemistry Letters | 2010
Mark Hadden; Allan J. Goodman; Cheng Guo; Peter R. Guzzo; Alan J. Henderson; Kevin Pattamana; Megan Ruenz; Bruce J. Sargent; Brian Swenson; Larry Yet; Jian Liu; Shuwen He; Iyassu K. Sebhat; Linus S. Lin; Constantin Tamvakopoulos; Qianping Peng; Yanqing Kan; Oksana C. Palyha; Theresa M. Kelly; Xiao-Ming Guan; Joseph M. Metzger; Marc L. Reitman; Ravi P. Nargund
SAR around non-peptidic potent bombesin receptor subtype-3 (BRS-3) agonist lead 2 is presented. Attempts to replace the carboxylic acid with heterocyclic isosteres to improve oral bioavailability and brain penetration are described.
Bioorganic & Medicinal Chemistry Letters | 2008
Liangqin Guo; Zhixiong Ye; Feroze Ujjainwalla; Heather L. Sings; Iyassu K. Sebhat; John Huber; David H. Weinberg; Rui Tang; Tanya MacNeil; Constantin Tamvakopoulos; Qianping Peng; Euan MacIntyre; Lex H.T. Van der Ploeg; Mark T. Goulet; Matthew J. Wyvratt; Ravi P. Nargund
Discovery of a series of tert-butyl pyrrolidine derived, potent and orally bioavailable melanocortin receptor subtype-4 (MC4R) selective modulators is disclosed.
Bioorganic & Medicinal Chemistry Letters | 2010
Shuwen He; Zhixiong Ye; Peter H. Dobbelaar; Iyassu K. Sebhat; Liangqin Guo; Jian Liu; Tianying Jian; Yingjie Lai; Christopher L. Franklin; Raman K. Bakshi; James Dellureficio; Qingmei Hong; Nancy N. Tsou; Richard G. Ball; William J. Martin; David H. Weinberg; Tanya MacNeil; Rui Tang; Constantin Tamvakopoulos; Qianping Peng; Randy R. Miller; Ralph A. Stearns; Howard Y. Chen; Airu S. Chen; Alison M. Strack; Tung M. Fong; D. Euan MacIntyre; Matthew J. Wyvratt; Ravi P. Nargund
We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.
Bioorganic & Medicinal Chemistry Letters | 2011
Qingmei Hong; Raman K. Bakshi; Brenda L. Palucki; Min K. Park; Zhixiong Ye; Shuwen He; Patrick G. Pollard; Iyassu K. Sebhat; Jian Liu; Liangqin Guo; William J. Martin; David H. Weinberg; Tanya MacNeil; Rui Tang; Constantin Tamvakopoulos; Qianping Peng; Randy R. Miller; Ralph A. Stearns; Howard Y. Chen; Airu S. Chen; Alison M. Strack; Tung M. Fong; D. Euan MacIntyre; Matthew J. Wyvratt; Ravi P. Nargund
We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
Bioorganic & Medicinal Chemistry Letters | 2010
Shuwen He; Zhixiong Ye; Peter H. Dobbelaar; Iyassu K. Sebhat; Liangqin Guo; Jian Liu; Tianying Jian; Yingjie Lai; Christopher L. Franklin; Raman K. Bakshi; James Dellureficio; Qingmei Hong; David H. Weinberg; Tanya MacNeil; Rui Tang; Alison M. Strack; Constantin Tamvakopoulos; Qianping Peng; Randy R. Miller; Ralph A. Stearns; Howard Y. Chen; Airu S. Chen; Tung M. Fong; Matthew J. Wyvratt; Ravi P. Nargund
We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds can afford high potency on MC4R as well as good rodent pharmacokinetic profiles. Compound 1r (MK-0489) demonstrates MC4R mediated reduction of food intake and body weight in mouse models. Compound 1r is efficacious in 14-day diet-induced obese (DIO) rat models.
Bioorganic & Medicinal Chemistry Letters | 2005
Brenda L. Palucki; Min K. Park; Ravi P. Nargund; Zhixiong Ye; Iyassu K. Sebhat; Patrick G. Pollard; Rubana N. Kalyani; Rui Tang; Tanya MacNeil; David H. Weinberg; Aurawan Vongs; Charles Rosenblum; George A. Doss; Randall R. Miller; Ralph A. Stearns; Qianping Peng; Constantin Tamvakopoulos; Erin McGowan; William J. Martin; Joseph M. Metzger; Cherrie Shepherd; Alison M. Strack; D. Euan MacIntyre; Lex H.T. Van der Ploeg; Arthur A. Patchett
Bioorganic & Medicinal Chemistry Letters | 2005
Zhixiong Ye; Liangqin Guo; Khaled J. Barakat; Patrick G. Pollard; Brenda L. Palucki; Iyassu K. Sebhat; Raman K. Bakshi; Rui Tang; Rubana N. Kalyani; Aurawan Vongs; Airu S. Chen; Howard Y. Chen; Charles Rosenblum; Tanya MacNeil; David H. Weinberg; Qianping Peng; Constantin Tamvakopoulos; Randy R. Miller; Ralph A. Stearns; William J. Martin; Joseph M. Metzger; Alison M. Strack; D. Euan MacIntyre; Lex H.T. Van der Ploeg; Arthur A. Patchett; Matthew J. Wyvratt; Ravi P. Nargund