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alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
Ross TM, Jetter MC, McDonnell ME, Boyd RE, Connelly CD, Martinez RP, Lewis MA, Codd EE, Raffa RB, Reitz AB. Ross TM, et al. Among authors: lewis ma. J Med Chem. 2000 Mar 9;43(5):765-8. doi: 10.1021/jm990569e. J Med Chem. 2000. PMID: 10715142 Corrected and republished. No abstract available.
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
Ross TM, Jetter MC, McDonnell ME, Boyd RE, Connelly CD, Martinez RP, Lewis MA, Codd EE, Raffa RB, Reitz AB. Ross TM, et al. Among authors: lewis ma. J Med Chem. 2000 Apr 6;43(7):1423-6. doi: 10.1021/jm000128r. J Med Chem. 2000. PMID: 10753480 No abstract available.
The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.
Bi Y, Dzierba CD, Fink C, Garcia Y, Green M, Han J, Kwon S, Kumi G, Liang Z, Liu Y, Qiao Y, Zhang Y, Zipp G, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Westphal RS, Kimball D, Bronson JJ, Macor JE. Bi Y, et al. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1443-7. doi: 10.1016/j.bmcl.2015.02.038. Epub 2015 Feb 21. Bioorg Med Chem Lett. 2015. PMID: 25754495
Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Hartz RA, Ahuja VT, Nara SJ, Kumar CMV, Brown JM, Bristow LJ, Rajamani R, Muckelbauer JK, Camac D, Kiefer SE, Hunihan L, Gulianello M, Lewis M, Easton A, Lippy JS, Surti N, Pattipati SN, Dokania M, Elavazhagan S, Dandapani K, Hamman BD, Allen J, Kostich W, Bronson JJ, Macor JE, Dzierba CD. Hartz RA, et al. J Med Chem. 2021 Aug 12;64(15):11090-11128. doi: 10.1021/acs.jmedchem.1c00472. Epub 2021 Jul 16. J Med Chem. 2021. PMID: 34270254
Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors.
Hartz RA, Ahuja VT, Nara SJ, Kumar CMV, Manepalli RKVLP, Sarvasiddhi SK, Honkhambe S, Patankar V, Dasgupta B, Rajamani R, Muckelbauer JK, Camac DM, Ghosh K, Pokross M, Kiefer SE, Brown JM, Hunihan L, Gulianello M, Lewis M, Lippy JS, Surti N, Hamman BD, Allen J, Kostich WA, Bronson JJ, Macor JE, Dzierba CD. Hartz RA, et al. J Med Chem. 2022 Mar 10;65(5):4121-4155. doi: 10.1021/acs.jmedchem.1c01966. Epub 2022 Feb 16. J Med Chem. 2022. PMID: 35171586
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
Dzierba CD, Bi Y, Dasgupta B, Hartz RA, Ahuja V, Cianchetta G, Kumi G, Dong L, Aleem S, Fink C, Garcia Y, Green M, Han J, Kwon S, Qiao Y, Wang J, Zhang Y, Liu Y, Zipp G, Liang Z, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Grace J, Wilson A, Nouraldeen A, Westphal R, Kimball D, Carson K, Bronson JJ, Macor JE. Dzierba CD, et al. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1448-52. doi: 10.1016/j.bmcl.2015.01.036. Epub 2015 Jan 28. Bioorg Med Chem Lett. 2015. PMID: 25690789
979 results