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Page 1
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
Albert JS, Aharony D, Andisik D, Barthlow H, Bernstein PR, Bialecki RA, Dedinas R, Dembofsky BT, Hill D, Kirkland K, Koether GM, Kosmider BJ, Ohnmacht C, Palmer W, Potts W, Rumsey W, Shen L, Shenvi A, Sherwood S, Warwick PJ, Russell K. Albert JS, et al. Among authors: aharony d. J Med Chem. 2002 Aug 29;45(18):3972-83. doi: 10.1021/jm020094i. J Med Chem. 2002. PMID: 12190319
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
Edwards PD, Albert JS, Sylvester M, Aharony D, Andisik D, Callaghan O, Campbell JB, Carr RA, Chessari G, Congreve M, Frederickson M, Folmer RH, Geschwindner S, Koether G, Kolmodin K, Krumrine J, Mauger RC, Murray CW, Olsson LL, Patel S, Spear N, Tian G. Edwards PD, et al. Among authors: aharony d. J Med Chem. 2007 Nov 29;50(24):5912-25. doi: 10.1021/jm070829p. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985862
Discovery of novel, orally active dual NK1/NK2 antagonists.
Bernstein PR, Aharony D, Albert JS, Andisik D, Barthlow HG, Bialecki R, Davenport T, Dedinas RF, Dembofsky BT, Koether G, Kosmider BJ, Kirkland K, Ohnmacht CJ, Potts W, Rumsey WL, Shen L, Shenvi A, Sherwood S, Stollman D, Russell K. Bernstein PR, et al. Among authors: aharony d. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2769-73. doi: 10.1016/s0960-894x(01)00572-8. Bioorg Med Chem Lett. 2001. PMID: 11591520
Synthesis, structure-activity relationships, and pharmacological evaluation of a series of fluorinated 3-benzyl-5-indolecarboxamides: identification of 4-[[5-[((2R)-2-methyl-4,4,4-trifluorobutyl)carbamoyl]-1-methyl indol- 3-yl]methyl]-3-methoxy-N-[(2-methylphenyl)sulfonyl]benzamide, a potent, orally active antagonist of leukotrienes D4 and E4.
Jacobs RT, Bernstein PR, Cronk LA, Vacek EP, Newcomb LF, Aharony D, Buckner CK, Kusner EJ. Jacobs RT, et al. Among authors: aharony d. J Med Chem. 1994 Apr 29;37(9):1282-97. doi: 10.1021/jm00035a008. J Med Chem. 1994. PMID: 8176706
The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1.
Veale CA, Alford VC, Aharony D, Banville DL, Bialecki RA, Brown FJ, Damewood JR Jr, Dantzman CL, Edwards PD, Jacobs RT, Mauger RC, Murphy MM, Palmer W, Pine KK, Rumsey WL, Garcia-Davenport LE, Shaw A, Steelman GB, Surian JM, Vacek EP. Veale CA, et al. Among authors: aharony d. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1949-52. doi: 10.1016/s0960-894x(00)00387-5. Bioorg Med Chem Lett. 2000. PMID: 10987424
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.
Brown DG, Bernstein PR, Wu Y, Urbanek RA, Becker CW, Throner SR, Dembofsky BT, Steelman GB, Lazor LA, Scott CW, Wood MW, Wesolowski SS, Nugiel DA, Koch S, Yu J, Pivonka DE, Li S, Thompson C, Zacco A, Elmore CS, Schroeder P, Liu J, Hurley CA, Ward S, Hunt HJ, Williams K, McLaughlin J, Hoesch V, Sydserff S, Maier D, Aharony D. Brown DG, et al. Among authors: aharony d. ACS Med Chem Lett. 2012 Nov 12;4(1):46-51. doi: 10.1021/ml300262e. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900562 Free PMC article.
67 results