214192-61-7Relevant academic research and scientific papers
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates
Semple, J. Edward
, p. 2501 - 2506 (1998)
Potent serine protease inhibitor la featuring a hybrid P3-P4 quaternary lactam dipeptide surrogate was prepared based upon SAR and molecular modeling investigations and in order to further probe the S2/S3 thrombin and FXa subsites. An efficient and concise synthetic route to the key aminolactam intermediate 4 was developed. The design, synthesis, and biological activity of this target and its P3-P4 diastereomer 1b is presented.
Efficient construction of novel quaternary lactam dipeptide surrogates
Semple, J. Edward
, p. 6645 - 6648 (2007/10/03)
Concise, facile synthetic routes to the hindered quaternary α- aminolactam intermediates 2, 10 and 12 were developed. These functionalized intermediates ultimately serve as novel types of Phe/nor-Asp-Pro dipeptide surrogates which in turn are useful as enzyme active site probes.
