69822-20-4Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis
Bouhedja, Mourad,Peres, Basile,Fhayli, Wassim,Ghandour, Zeinab,Boumendjel, Ahcène,Faury, Gilles,Khelili, Smail
, p. 774 - 796 (2018)
Two new series of ring-opened analogues of cromakalim bearing sulfonylurea moieties (series A: with N-unmethylated sulfonylureas, series B: with N-methylated sulfonylureas) were synthesized and tested as relaxants of vascular and respiratory smooth muscle
Design and synthesis of novel meta-linked phenylglycine macrocyclic FVIIa inhibitors
Richter, Jeremy M.,Cheney, Daniel L.,Bates, J. Alex,Wei, Anzhi,Luettgen, Joseph M.,Rendina, Alan R.,Harper, Timothy M.,Narayanan, Rangaraj,Wong, Pancras C.,Seiffert, Dietmar,Wexler, Ruth R.,Priestley, E. Scott
supporting information, p. 67 - 72 (2017/12/12)
Two novel series of meta-linked phenylglycine-based macrocyclic FVIIa inhibitors have been designed to improve the rodent metabolic stability and PK observed with the precursor para-linked phenylglycine macrocycles. Through iterative structure-based design and optimization, the TF/ FVIIa Ki was improved to subnanomolar levels with good clotting activity, metabolic stability, and permeability.
Stereoselective C-glycosidation of d-fucose derivatives directed by the protective groups
Cortezano-Arellano, Omar,Meléndez-Becerra, Camilo A.,Cortés, Fernando,Sartillo-Piscil, Fernando,Cordero-Vargas, Alejandro
supporting information, p. 51 - 59 (2014/06/23)
Stereoselectivity in the C-glycosidation of lactones derived from d-fucose by following Kishi's method, which involves the addition of a nucleophile onto a carbohydrate-derived lactone and subsequent reduction of the lactol, was found to be reliant on the nature of the C2 and C3 protective groups. Lactones bearing TBDMS protecting groups selectively afford 1,3-trans products (α anomer), in which the stereoselective outcome is in apparent concordance with Woerpel's model. On the other hand, their benzylated congeners produce the 1,3-cis products (β anomer) as the major diastereoisomers. The latter results suggest an abnormal behavior during the stereoselective nucleophilic substitution at the anomeric position of the benzylated lactones.
MACROCYCLIC FACTOR VIIA INHIBITORS
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Paragraph 00138, (2015/01/09)
The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.
