17637-11-5Relevant 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.
Single-hole hollow nanospheres from enantioselective self-assembly of chiral AIE carboxylic acid and amine
Li, Dong-Mi,Zheng, Yan-Song
body text, p. 1100 - 1108 (2011/04/12)
Phenylacrylonitrile tartaric acids have been found to enantioselectively self-assemble with an enantiomer of a chiral amine to form either nanofibers or nanospheres that exhibit aggregation-induced emission (AIE). The nanofibers exhibited stronger emission intensity and longer wavelengths of absorption and emission than the nanospheres because of increased π-π conjugation, an effect previously unseen in AIE. When the solvent consists of a mixture of water and THF rather than water and ethanol, the resultant nanospheres have holes. The holes are the result of the dissolution of defects and a decrease in the bending energy. This is in contrast to hole formation from solvents flowing out of the nanospheres, as previously seen. Through control of the water/THF ratio, the size of the holes in the nanospheres can be tuned. Nanospheres with a single hole displayed both higher uptake capacity and larger release speed of the drug naproxen than closed nanospheres. The ability to adjust fluorescent properties of AIE molecules through the preparation of organic single-hole hollow nanospheres has also been investigated along with the implications of the AIE mechanism.
ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE
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Page/Page column 441-442, (2008/06/13)
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