The role of immunologically released mediators, such as histamine, leukotrienes, and platelet-activating factor, is well-established for asthma and other allergic disorders. Developing therapeutic agents which would block mediator release from mast cells and other relevant cell types would provide a rational approach to asthma therapy. Using human basophil as a screen, a series of 4-aryl-2-(phenylamino)pyrimidines was found which inhibited mediator release. These compounds were prepared by condensing acetyl heterocycles with dimethylformamide dimethyl acetal to form enaminones which are cyclized with aryl guanidines to give pyrimidines. After examining a large number of analogs, N-[3-(1H-imidazol-1-yl)phenyl]-4-(2-pyridinyl)-2- pyrimidinamine (1-27) was chosen for toxicological evaluation.
Condensation of 17/3-estradiol 3-benzyl ether (I) with 1 a-bromo-A-trifluoroacetamido tri-O-acetylglucopyranoside (Xb) in the presence of cadmium carbonate gave the corresponding 17/3-estradiol 17-(a-and /3-)glycosides (lib, III). Selective deacylation and reacetylation followed by debenzylation afforded the 17/3-estradiol 17-(a-and /3-)A-acetyl-T Xhe isolation of -estradiol 3-glucuronide 17/3-acetylglucosaminide from rabbit urine by Layne and coworkers (1964) revealed a new conjugating pathway for steroids. In a subsequent series of papers, Layne and coworkers (Jirku and Layne, 1965; Layne el al., 1965;Collins et al., 1967Collins et al., , 1968) studied C-l7-glucosaminide formation by the action of an A-acetylglucosaminyl-transfer enzyme system and showed that the stereochemical configuration of the Hahydroxyl group was a necessary structural feature for estrogens containing a C-3-glucuronide.Recently, other double conjugates containing a A-acetylglucosaminide grouping have been isolated from human urine.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.