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N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
Altenbach RJ, Khilevich A, Meyer MD, Buckner SA, Milicic I, Daza AV, Brune ME, O'Neill AB, Gauvin DM, Cain JC, Nakane M, Holladay MW, Williams M, Brioni JD, Sullivan JP. Altenbach RJ, et al. Among authors: holladay mw. J Med Chem. 2002 Sep 26;45(20):4395-7. doi: 10.1021/jm025550h. J Med Chem. 2002. PMID: 12238918
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K(ATP) opener that selectively inhibits spontaneous bladder contractions.
Carroll WA, Altenbach RJ, Bai H, Brioni JD, Brune ME, Buckner SA, Cassidy C, Chen Y, Coghlan MJ, Daza AV, Drizin I, Fey TA, Fitzgerald M, Gopalakrishnan M, Gregg RJ, Henry RF, Holladay MW, King LL, Kort ME, Kym PR, Milicic I, Tang R, Turner SC, Whiteaker KL, Yi L, Zhang H, Sullivan JP. Carroll WA, et al. Among authors: holladay mw. J Med Chem. 2004 Jun 3;47(12):3163-79. doi: 10.1021/jm030356w. J Med Chem. 2004. PMID: 15163196
Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP. Altenbach RJ, et al. Among authors: holladay mw. J Med Chem. 2004 Jun 3;47(12):3220-35. doi: 10.1021/jm030551a. J Med Chem. 2004. PMID: 15163201
Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties.
Lin NH, Gunn DE, Ryther KB, Garvey DS, Donnelly-Roberts DL, Decker MW, Brioni JD, Buckley MJ, Rodrigues AD, Marsh KG, Anderson DJ, Buccafusco JJ, Prendergast MA, Sullivan JP, Williams M, Arneric SP, Holladay MW. Lin NH, et al. Among authors: holladay mw. J Med Chem. 1997 Jan 31;40(3):385-90. doi: 10.1021/jm960233u. J Med Chem. 1997. PMID: 9022806
Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo.
Briggs CA, Anderson DJ, Brioni JD, Buccafusco JJ, Buckley MJ, Campbell JE, Decker MW, Donnelly-Roberts D, Elliott RL, Gopalakrishnan M, Holladay MW, Hui YH, Jackson WJ, Kim DJ, Marsh KC, O'Neill A, Prendergast MA, Ryther KB, Sullivan JP, Arneric SP. Briggs CA, et al. Among authors: holladay mw. Pharmacol Biochem Behav. 1997 May-Jun;57(1-2):231-41. doi: 10.1016/s0091-3057(96)00354-1. Pharmacol Biochem Behav. 1997. PMID: 9164577
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.
Lin NH, Gunn DE, Li Y, He Y, Bai H, Ryther KB, Kuntzweiler T, Donnelly-Roberts DL, Anderson DJ, Campbell JE, Sullivan JP, Arneric SP, Holladay MW. Lin NH, et al. Among authors: holladay mw. Bioorg Med Chem Lett. 1998 Feb 3;8(3):249-54. doi: 10.1016/s0960-894x(98)00019-5. Bioorg Med Chem Lett. 1998. PMID: 9871663
Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.
Holladay MW, Bai H, Li Y, Lin NH, Daanen JF, Ryther KB, Wasicak JT, Kincaid JF, He Y, Hettinger AM, Huang P, Anderson DJ, Bannon AW, Buckley MJ, Campbell JE, Donnelly-Roberts DL, Gunther KL, Kim DJ, Kuntzweiler TA, Sullivan JP, Decker MW, Arneric SP. Holladay MW, et al. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2797-802. doi: 10.1016/s0960-894x(98)00504-6. Bioorg Med Chem Lett. 1998. PMID: 9873625
46 results