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New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides.
Prugh JD, Hartman GD, Mallorga PJ, McKeever BM, Michelson SR, Murcko MA, Schwam H, Smith RL, Sondey JM, Springer JP, et al. Prugh JD, et al. Among authors: hartman gd. J Med Chem. 1991 Jun;34(6):1805-18. doi: 10.1021/jm00110a008. J Med Chem. 1991. PMID: 2061922
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.
Egbertson MS, Cook JJ, Bednar B, Prugh JD, Bednar RA, Gaul SL, Gould RJ, Hartman GD, Homnick CF, Holahan MA, Libby LA, Lynch JJ Jr, Lynch RJ, Sitko GR, Stranieri MT, Vassallo LM. Egbertson MS, et al. Among authors: hartman gd. J Med Chem. 1999 Jul 1;42(13):2409-21. doi: 10.1021/jm980722p. J Med Chem. 1999. PMID: 10395482
2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.
Williams TM, Ciccarone TM, MacTough SC, Bock RL, Conner MW, Davide JP, Hamilton K, Koblan KS, Kohl NE, Kral AM, Mosser SD, Omer CA, Pompliano DL, Rands E, Schaber MD, Shah D, Wilson FR, Gibbs JB, Graham SL, Hartman GD, Oliff AI, Smith RL. Williams TM, et al. Among authors: hartman gd. J Med Chem. 1996 Mar 29;39(7):1345-8. doi: 10.1021/jm9508090. J Med Chem. 1996. PMID: 8691462 No abstract available.
Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.
Egbertson MS, Bednar B, Askew BC, Bednar RA, Brashear K, Breslin MJ, Duggan ME, Fisher TE, Halczenko W, Hutchinson JH, Ihle N, Prugh JD, Wai JS, Gould RJ, Hartman GD. Egbertson MS, et al. Among authors: hartman gd. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8. doi: 10.1016/s0960-894x(00)00385-1. Bioorg Med Chem Lett. 2000. PMID: 10987423
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD. Bilodeau MT, et al. Among authors: hartman gd. J Med Chem. 2004 Dec 2;47(25):6363-72. doi: 10.1021/jm049697f. J Med Chem. 2004. PMID: 15566305
171 results