16202-15-6Relevant articles and documents
Analogs of sub-nanomolar hMC1R agonist LK-184 [Ph(CH2) 3CO-His-D-Phe-Arg-Trp-NH2]. An additional binding site within the human melanocortin receptor 1?
Koikov,Ebetino,Solinsky,Cross-Doersen,Knittel
, p. 3997 - 4000 (2004)
Twenty nine analogs of a superpotent MC1R agonist LK-184 (1) were tested at human melanocortin receptors (hMC1, hMC3, and hMC4Rs). All derivatives with the spacer between the N-terminus and the aromatic ring longer or shorter than C3 were much less potent at hMC1R than 1. Only LK-312 PhCO(CH 2)3CO-His-D-Phe-Arg-Trp-NH2 (3), partially mimicking the π-system of 1, had an EC50 of 0.05nM at hMC1R, which confirms the localization of the π-binding zone of the receptor. Truncation of 1 to Ph(CH2)3CO-His-D-Phe-Arg-NH2 gave a full MC1 agonist, LK-394 (30), with an EC50 of 5nM and a weak partial agonism at MC3/4Rs. This suggests the existence of an additional binding site within hMC1R next to that for the core sequence His-D-Phe-Arg-Trp-NH 2.
PYRROLOPYRROLE COMPOSITIONS AS PYRUVATE KINASE (PKR) ACTIVATORS
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Paragraph 00148-00149, (2018/10/19)
The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds of formula (I) useful as activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia.
High-performance liquid chromatography separation of enantiomers of mandelic acid and its analogs on a chiral stationary phase
Aneja, Ritu,Luthra, Pratibha Mehta,Ahuja, Satinder
experimental part, p. 479 - 485 (2010/08/20)
The enantiomers of mandelic acid and its analogs have been chromatographically separated on a chiral stationary phase (CSP) derived from 4-(3,5-dinitrobenzamido) tetrahydrophenanthrene. The rationale of separations of these compounds is discussed with respect to the method development for determining enantiomeric purity and possibility of obtaining enantiomerically pure materials by high-pressure liquid chromatography. The relationship of analyte structure to the extent of enantiomeric separation has been examined and separation factors (a) are presented for various groups of structurally related compounds. Chiral recognition models have been suggested to account for the observed separations. These models provide mechanistic insights into the chiral recognition process.
