305329-35-5Relevant academic research and scientific papers
Design and synthesis of potent, orally active, inhibitors of carboxypeptidase U (TAFIa)
Polla, Magnus O.,Tottie, Louise,Norden, Carita,Linschoten, Marcel,Muesil, Djordje,Trumpp-Kallmeyer, Susanne,Aukrust, Inger R.,Ringom, Rune,Holm, Kjetil H.,Neset, Siren M.,Sandberg, Marcel,Thurmond, John,Yu, Peng,Hategan, Georgeta,Anderson, Herb
, p. 1151 - 1175 (2004)
A series of 3-mercapto-propionic acid derivatives that function as reversible inhibitors of carboxypeptidase U have been prepared. We present a successful design strategy using cyclic, low basicity guanidine mimetics resulting in potent, selective and bioavailable inhibitors of carboxypeptidase U (TAFIa).
Partially Saturated Bicyclic Heteroaromatics as an sp3-Enriched Fragment Collection
Twigg, David G.,Kondo, Noriyasu,Mitchell, Sophie L.,Galloway, Warren R. J. D.,Sore, Hannah F.,Madin, Andrew,Spring, David R.
supporting information, p. 12479 - 12483 (2016/10/13)
Fragment-based lead generation has proven to be an effective means of identifying high-quality lead compounds for drug discovery programs. However, the fragment screening sets often used are principally comprised of sp2-rich aromatic compounds, which limits the structural (and hence biological) diversity of the library. Herein, we describe strategies for the synthesis of a series of partially saturated bicyclic heteroaromatic scaffolds with enhanced sp3character. Subsequent derivatization led to a fragment collection featuring regio- and stereo-controlled introduction of substituents on the saturated ring system, often with formation of new stereocenters.
PIPERIDINE DERIVATIVES USEFUL AS OREXIN ANTAGONISTS
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Page/Page column 32, (2010/07/09)
This invention relates to imidazopyridylmethylene substituted piperidine derivatives orexin antagonists and their use as pharmaceuticals.
