Philip Waid

Publications (2)7.8 Total impact

• Article: Anthranilamide inhibitors of factor Xa.

  David Mendel, Angela L Marquart, Sajan Joseph, Philip Waid, Ying K Yee, Anne Louise Tebbe, Andrew M Ratz, David K Herron, Theodore Goodson, John J Masters, [......], Jennifer M Tinsley, Michael R Wiley, Leonard C Weir, Jeffrey A Kyle, Valentine J Klimkowski, Gerald F Smith, Richard D Towner, Larry L Froelich, John Buben, Trelia J Craft
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  ABSTRACT: SAR about the B-ring of a series of N(2)-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
  Bioorganic & Medicinal Chemistry Letters 10/2007; 17(17):4832-6. · 2.55 Impact Factor
• Article: Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.

  John T Randolph, Philip Waid, Charles Nichols, Daryl Sauer, Fortuna Haviv, Gilbert Diaz, Gary Bammert, Leslie M Besecke, Jason A Segreti, Kurt M Mohning, Eugene N Bush, Craig D Wegner, Jonathan Greer
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  ABSTRACT: The design and synthesis of a series of 11,12-cyclic carbamate derivatives of 6-O-methylerythromycin A that are novel, nonpeptide LHRH antagonists, is described. The macrolide antagonist 1, discovered during a screen of our chemical repository, was compared to a macrocyclic peptide antagonist 2 using molecular modeling, thus providing a model for the design of more potent antagonists. Medicinal chemistry efforts to find a replacement for cladinose at position 3 of the erythronolide core provided a series of oxazolidinone carbamates that were equally as active as the cladinose-containing parent macrolides. The descladinose LHRH antagonist 14 has 1-2 nM affinity for both rat and human LHRH receptors and is a potent inhibitor of LH release (pA2 = 8.76) in vitro. In vivo, 14 was found to produce a dose-dependent suppression of LH in male castrate rats via both i.v. and p.o. dosing.
  Journal of Medicinal Chemistry 03/2004; 47(5):1085-97. · 5.25 Impact Factor