227624-29-5Relevant articles and documents
Unconventional Secondary Structure Mimics: Ladder-Rungs
Arancillo, Maritess,Burgess, Kevin,Lin, Chen-Ming,Whisenant, Jonathan
supporting information, p. 9398 - 9402 (2020/05/05)
Secondary structures tend to be recognizable because they have repeating structural motifs, but mimicry of these does not have to follow such well-defined patterns. Bioinformatics studies to match side-chain orientations of a novel hydantoin triazole chemotype (1) to protein-protein interfaces revealed it tends to align well across parallel and antiparallel sheets, like rungs on a ladder. One set of these overlays was observed for the protein-protein interaction uPA?uPAR. Consequently, chemotype 1 was made with appropriate side-chains to mimic uPA at this interface. Biophysical assays indicate these compounds did in fact bind uPAR, and elicit cellular responses that affected invasion, migration, and wound healing.
One-pot synthesis of Weinreb amides employing 3,3-dichloro-1,2-diphenylcyclopropene (CPI-Cl) as a chlorinating agent
Shekharappa,Roopesh Kumar,Sureshbabu, Vommina V.
, p. 790 - 798 (2019/03/26)
The synthesis of Nα-protected amino alkyl Weinreb amides starting from the corresponding α-amino acids as well as carboxylic acids has been delineated through the in situ generation of acid chlorides using CPI-Cl as a chlorinating agent. The protocol is simple; the reaction conditions employed were mild, and compatible with all the three commonly used urethane protecting groups namely, Boc, Cbz and Fmoc groups. The resulting Weinreb amides are obtained in good yields as optically pure products.
Substituted melanocortin receptor-specific piperazine compounds
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Page/Page column 31-34; 51, (2010/05/13)
A substituted piperazine compound having the structure I: or the structure IX: or an enantomeric, stereoisomeric or diastereomeric form of the foregoing, and pharmaceutically acceptable salts thereof, where J, L, Q, W, A, R6, R7, z and y are as defined in the specification, and the carbon atoms marked with an asterisk can have any stereochemical configuration, which compounds bind to one or more melanocortin receptors and may be employed in pharmaceutical preparations for treatment of one or more melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.
