Kevin G. Liu
Princeton University
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Publication
Featured researches published by Kevin G. Liu.
Bioorganic & Medicinal Chemistry Letters | 2009
Kevin G. Liu; Jennifer R. Lo; Thomas A. Comery; Guo Ming Zhang; Jean Y. Zhang; Dianne Kowal; Deborah L. Smith; Li Di; Edward H. Kerns; Lee E. Schechter; Albert J. Robichaud
As part of our continuing efforts to identify therapeutics for CNS diseases such as schizophrenia and Alzheimers disease (AD), we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands as a potential treatment for cognitive dysfunction. Herein we report the identification of a novel series of benzoxazole derivatives as potent 5-HT(6) ligands. The synthesis and detailed SAR of this class of compounds are reported. The compounds have been shown to be full antagonists in a cyclic AMP functional assay.
Journal of Medicinal Chemistry | 2010
Kevin G. Liu; Albert Jean Robichaud; Ronald C. Bernotas; Yinfa Yan; Jennifer R. Lo; Mei-Yi Zhang; Zoe A. Hughes; Christine Huselton; Guo Ming Zhang; Jean Y. Zhang; Dianne Kowal; Deborah L. Smith; Lee E. Schechter; Thomas A. Comery
As part of our efforts to develop agents for CNS diseases, we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands for cognitive enhancement. Herein we report the identification of a novel series of 5-piperazinyl-3-sulfonylindazoles as potent and selective 5-HT(6) antagonists. The synthesis, SAR, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole (WAY-255315 or SAM-315) will be described.
Bioorganic & Medicinal Chemistry Letters | 2008
Kevin G. Liu; Jennifer R. Lo; Thomas A. Comery; Guo Ming Zhang; Jean Y. Zhang; Dianne Kowal; Deborah L. Smith; Li Di; Edward H. Kerns; Lee E. Schechter; Albert J. Robichaud
A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands is reported.
Bioorganic & Medicinal Chemistry Letters | 2009
Kevin G. Liu; Jennifer R. Lo; Thomas A. Comery; Guo Ming Zhang; Jean Y. Zhang; Dianne Kowal; Deborah L. Smith; Li Di; Edward H. Kerns; Lee E. Schechter; Albert J. Robichaud
As part of our continuing efforts to identify therapeutics for CNS diseases, such as schizophrenia and Alzheimers disease (AD), we have been focused on the 5-HT(6) receptor in an attempt to identify ligands as a potential treatment for cognitive dysfunction. Herein we report the identification of a novel series of 1-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists. The synthesis and SAR of this class of compounds are reported. Several potent compounds in both binding and cyclase functional assays also display good selectivity, microsomal stability, solubility, and brain penetration as well as low cytochrome P450 inhibition. One compound exemplified in this series showed 24% oral bioavailability and in vivo efficacy in a NOR cognition model at 10mg/kg following an oral administration in rats.
Journal of Medicinal Chemistry | 2011
Sang-Phyo Hong; Kevin G. Liu; Gil Ma; Michael Sabio; Michelle A. Uberti; Maria D. Bacolod; John R. Peterson; Zack Zou; Albert Jean Robichaud; Dario Doller
There is an increasing amount of evidence to support that activation of the metabotropic glutamate receptor 4 (mGlu4 receptor), either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinsons disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons. As part of our efforts in identifying therapeutics for central nervous system (CNS) diseases such as Parkinsons disease, we have been focusing on metabotropic glutamate receptors. Herein we report our studies with a series of tricyclic thiazolopyrazoles as mGlu4 PAMs.
Bioorganic & Medicinal Chemistry | 2011
Kevin G. Liu; Albert J. Robichaud; Alexander Alexei Greenfield; Jennifer R. Lo; Cristina Grosanu; James F. Mattes; Yanxuan Cai; Guo Ming Zhang; Jean Y. Zhang; Dianne Kowal; Deborah L. Smith; Li Di; Edward H. Kerns; Lee E. Schechter; Thomas A. Comery
As part of our efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands for this purpose. Herein we report the identification of a novel series of 3-sulfonylindazole derivatives with acyclic amino side chains as potent and selective 5-HT(6) antagonists. The synthesis and detailed SAR of this class of compounds are reported.
Bioorganic & Medicinal Chemistry Letters | 2009
Kevin G. Liu; Jennifer R. Lo; Thomas A. Comery; Guo Ming Zhang; Jean Y. Zhang; Dianne Kowal; Deborah L. Smith; Li Di; Edward H. Kerns; Lee E. Schechter; Albert J. Robichaud
Cognitive dysfunction is a characteristic of various forms of dementia such as Alzheimers disease (AD) and a core feature of schizophrenia. As part of our continuing efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT(6) receptor-one of the emerging therapeutic targets in this area. Herein, we report the identification of a novel series of 3-piperidinyl-5-sulfonylindazole derivatives as potent 5-HT(6) antagonists. The synthesis and SAR of this class of compounds are reported.
Drug Development Research | 2009
Kevin G. Liu; Albert J. Robichaud
Organic Letters | 2006
Kevin G. Liu; Albert J. Robichaud; Jennifer R. Lo; and James F. Mattes; Yanxuan Cai
Tetrahedron Letters | 2005
Kevin G. Liu; Albert J. Robichaud