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William R. Baker
Researcher at Abbott Laboratories
Publications - 46
Citations - 1129
William R. Baker is an academic researcher from Abbott Laboratories. The author has contributed to research in topics: Renin inhibitor & Farnesyltransferase. The author has an hindex of 18, co-authored 46 publications receiving 1117 citations.
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Cyclobutane derivatives as inhibitors of squalene synthase and protein farnesyltransferase
David L. Arendsen,David J. Augeri,William R. Baker,Stephen A. Fakhoury,K. L. Anthony Fung,David S. Garvey,Mcclellan William J,Stephen J. O'connor,Rajnandan N. Prasad,Todd W. Rockway,Saul H. Rosenberg,Wang Shen,Herman H. Stein,David M. Stout,Gerard M. Sullivan +14 more
TL;DR: In this paper, a compound of formula (I or (II) or a pharmaceutically acceptable salt thereof, which is useful for inhibiting protein farnesyltransferase and the farnesyation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, is presented.
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Modification of macrolide antibiotics. Synthesis of 11-deoxy-11-(carboxyamino)-6-O-methylerythromycin A 11,12-(cyclic esters) via an intramolecular Michael reaction of O-carbamates with an α,β-unsaturated ketone
TL;DR: In this article, le composition du titre est obtenu via un C-12 O-carbamate (issu lui-meme de l'acylation d'un alcool allylique derive de la O-methyl-6 erythromycine A) which se cyclise ensuite entre C-11 and C- 12 by une reaction de Michael intramoleculaire.
Journal ArticleDOI
Discovery of a peptide-based renin inhibitor with oral bioavailability and efficacy
Hollis D. Kleinert,Saul H. Rosenberg,William R. Baker,Herman H. Stein,Vered Klinghofer,Jennifer L. Barlow,Kenneth P. Spina,James S. Polakowski,Peter J. Kovar,Jerome Cohen,Denissen Jon F +10 more
TL;DR: Dose-related reductions in blood pressure, plasma renin activity, and plasma angiotensin II in parallel with increased plasma drug concentrations were observed after oral administration of A-72517 to conscious, salt-depleted dogs, indicating that peptide-based molecules of sizable molecular mass can be absorbed intact into the systemic circulation of animals.
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Annelative ring expansion via intramolecular [2 + 2] photocycloaddition of .alpha.,.beta.-unsaturated .gamma.-lactones and reductive cleavage: synthesis of hydrocyclopentacyclooctene-5-carboxylates
Journal ArticleDOI
1,2,3-Trisubstituted cyclopropanes as conformationally restricted peptide isosteres : application to the design and synthesis of novel renin inhibitors
Stephen F. Martin,Richard E. Austin,Christopher J. Oalmann,William R. Baker,Stephen Condon,Ed DeLara,Saul H. Rosenberg,Kenneth P. Spina,Herman H. Stein,Jerome Cohen,Hollis D. Kleinert +10 more
TL;DR: Evaluated the efficacy of 1,2,3-trisubstituted cyclopropanes as rigid replacements of beta-strand secondary structure in pseudopeptidic ligands and found that a significant number of substances inhibited renin at nanomolar concentrations.