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Design, Synthesis, and Evolution of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors: P1-Argininal Derivatives Incorporating P3-P4 Lactam Sulfonamide Moieties 1

✍ Scribed by Semple, J. Edward; Rowley, David C.; Brunck, Terence K.; Ha-Uong, Theresa; Minami, Nathaniel K.; Owens, Timothy D.; Tamura, Susan Y.; Goldman, Erick A.; Siev, Daniel V.; Ardecky, Robert J.; Carpenter, Stephen H.; Ge, Yu; Richard, Brigitte M.; Nolan, Thomas G.; Håkanson, Kjell; Tulinsky, Al; Nutt, Ruth F.; Ripka, William C.


Book ID
121273491
Publisher
American Chemical Society
Year
1996
Tongue
English
Weight
348 KB
Volume
39
Category
Article
ISSN
0022-2623

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✍ J.Edward Semple; David C. Rowley; Terence K. Brunck; William C. Ripka 📂 Article 📅 1997 🏛 Elsevier Science 🌐 English ⚖ 388 KB

Molecular modeling and topographic considerations of the thrombin-specific sequences Boc-Asp-Pro-Arg-TS or Ac-d-Phe-Pro-Arg-TS (TS = transition state analog electrophilic center) and related scaffolds led to the design of novel P2-P4-azapeptidomimetic Pl-argininal and Pl-ketoargininamide derivatives