143577-46-2Relevant articles and documents
Discovery of N-Substituted 3-Amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic Acids as Highly Potent Third-Generation Inhibitors of Human Arginase i and II
Van Zandt, Michael C.,Jagdmann, G. Erik,Whitehouse, Darren L.,Ji, Minkoo,Savoy, Jennifer,Potapova, Olga,Cousido-Siah, Alexandra,Mitschler, Andre,Howard, Eduardo I.,Pyle, Anna Marie,Podjarny, Alberto D.
, p. 8164 - 8177 (2019/10/02)
Recent efforts to identify new highly potent arginase inhibitors have resulted in the discovery of a novel family of (3R,4S)-3-amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid analogues with up to a 1000-fold increase in potency relative to the current standards, 2-amino-6-boronohexanoic acid (ABH) and N-hydroxy-nor-l-arginine (nor-NOHA). The lead candidate, with an N-2-amino-3-phenylpropyl substituent (NED-3238), example 43, inhibits arginase I and II with IC50 values of 1.3 and 8.1 nM, respectively. Herein, we report the design, synthesis, and structure-activity relationships for this novel series of inhibitors, along with X-ray crystallographic data for selected examples bound to human arginase II.
7-Azaindole derivatives as potential partial nicotinic agonists
Stoit, Axel R.,den Hartog, Arnold P.,Mons, Harry,van Schaik, Sjoerd,Barkhuijsen, Nynke,Stroomer, Cees,Coolen, Hein K.A.C.,Reinders, Jan Hendrik,Adolfs, Tiny J.P.,van der Neut, Martina,Keizer, Hiskias,Kruse, Chris G.
, p. 188 - 193 (2008/12/23)
We have investigated a series of 7-azaindoles as potential partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor affinity and functional activity. Compound (+)-51 exhibited the most potent nAChR binding (Ki = 10 nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation.
Process for preparing cyclic amines and intermediate products thereof
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, (2008/06/13)
A process for preparing a cyclic amine of Formula I STR1 in which R1 is phenyl, optionally substituted by 1 to 3 lower alkoxy groups; R2, R3 and R4 are independently hydrogen or lower alkyl; and n is 1 or 2, comprises (1) converting an aminoalcohol of Formula III STR2 to a dioxooxathiazolidine of Formula II STR3 in which R2, R3, R4 and n are as defined above; and (2) reacting the dioxooxathiazolidine of Formula II with an organometallic nucleophile, R1 M*, wherein R1 is as defined above, and hydrolyzing the resulting sulfamate salt.