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Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
Blum CA, Caldwell T, Zheng X, Bakthavatchalam R, Capitosti S, Brielmann H, De Lombaert S, Kershaw MT, Matson D, Krause JE, Cortright D, Crandall M, Martin WJ, Murphy BA, Boyce S, Jones AB, Mason G, Rycroft W, Perrett H, Conley R, Burnaby-Davies N, Chenard BL, Hodgetts KJ. Blum CA, et al. J Med Chem. 2010 Apr 22;53(8):3330-48. doi: 10.1021/jm100051g. J Med Chem. 2010. PMID: 20307063
Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites.
Hodgetts KJ, Blum CA, Caldwell T, Bakthavatchalam R, Zheng X, Capitosti S, Krause JE, Cortright D, Crandall M, Murphy BA, Boyce S, Brian Jones A, Chenard BL. Hodgetts KJ, et al. Among authors: blum ca. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4359-63. doi: 10.1016/j.bmcl.2010.06.069. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20615696
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Zheng X, Hodgetts KJ, Brielmann H, Hutchison A, Burkamp F, Brian Jones A, Blurton P, Clarkson R, Chandrasekhar J, Bakthavatchalam R, De Lombaert S, Crandall M, Cortright D, Blum CA. Zheng X, et al. Among authors: blum ca. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21. doi: 10.1016/j.bmcl.2006.07.010. Epub 2006 Jul 25. Bioorg Med Chem Lett. 2006. PMID: 16870426
Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
Blum CA, Zheng X, Brielmann H, Hodgetts KJ, Bakthavatchalam R, Chandrasekhar J, Krause JE, Cortright D, Matson D, Crandall M, Ngo CK, Fung L, Day M, Kershaw M, De Lombaert S, Chenard BL. Blum CA, et al. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4573-7. doi: 10.1016/j.bmcl.2008.07.036. Epub 2008 Jul 15. Bioorg Med Chem Lett. 2008. PMID: 18662872
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