N-acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRβ
We have identified a novel liver X receptor (LXR) agonist (2) that activates the LXRβ subtype with selectivity over LXRα. LXRβ selectivity was confirmed using macrophages derived from LXR mutant mice. Despite its selectivity and modest potency, the compou
Direct microwave synthesis of N,N′-diacylhydrazines and boc-protected hydrazides by in situ carbonylations under air
Palladium-catalyzed hydrazidocarbonylations of aryl iodides and bromides were performed by controlled microwave irradiation, employing Mo(CO)6 as a convenient CO source. A fluorous phosphine ligand was succesfully used to recycle the catalytic
Herrero, Maria Antonia,Wannberg, Johan,Larhed, Mats
p. 2335 - 2338
(2007/10/03)
A New Class of Nonhormonal Pregnancy-Terminating Agents. Synthesis and Contragestational Activity of 3,5-Diaryl-s-triazoles
A series of 3,5-diaryl-s-triazoles were synthesized and evaluated as postimplantation contragestational agents.The introduction of various substituents (e.g., an o-alkyl chain on one phenyl and a m-alkoxy group on the other) was found to increase the potency.Several compounds with very high pregnancy-terminating activity in both hamsters and rats were obtained.One of these, 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-s-triazole, DL 111 (36), was selected for detailed evaluation in various animal species.A synthetic scheme for the preparation of these compounds and preliminary structure-activity relationships are presented.