103386-91-0Relevant articles and documents
Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides
Youssefyeh,Campbell,Klein,Airey,Darkes,Powers,Schnapper,Neuenschwander,Fitzpatrick,Pendley,Martin
, p. 895 - 903 (2007/10/02)
This report describes the development of novel benzamides which are orally active, highly potent, specific antagonists of 5-HT3 receptors. Described in this first report are the structure-activity relationships that led to novel structures with improved potency and selectivity. From this series of compounds, (S)-28 was identified and selected for further evaluation as a 5- HT3 receptor antagonist. Compared with 5-HT3 antagonists such as GR 38032F, BRL 43694, and metoclopramide, (S)-28 was most active in (a) inhibiting binding to 5-HT3 receptor binding sites in rat entorhinal cortex with an K(i) value of 0.19 nM and (b) blocking cisplatin-induced emesis in the ferret with an ED50 value determined to be 9 μg/kg po.
PHOTOLACTONIZATION : A NOVEL SYNTHETIC ENTRY TO MACROLIDES
Quinkert, Gerhard,Billhardt, Uta-Maria,Jakob, Harald,Fischer, Gerd,Glenneberg, Juergen,et al.
, p. 822 - 861 (2007/10/02)
o-Quinol acetates, hydroxyalkyalted at C(6), are easily accesible from simple phenols by Wessely acetoxylation (preferentially catalyzed by BF3).On UV irradiation ( in the presence of an appropriate tertiary amine), they are smoothly converted to macrocyclic lactones.Subtle conditions have been elaborated to lead to high overall yields, and the scope of the conversion of phenols to macrolides has been elucidated.
