据报道,通过调节1-,5-和6-位侧链的大小,发现了基于3-氨基甲酰基-2-吡啶酮衍生物的新型CB2配体。该模板周围的结构-活性关系导致鉴定出S-777469为选择性CB2受体激动剂,该化合物在1.0 mg / kg po和10 mg / kg po下表现出对化合物48/80诱导的刮擦的显着抑制作用(55 %和61%)。
据报道,通过调节1-,5-和6-位侧链的大小,发现了基于3-氨基甲酰基-2-吡啶酮衍生物的新型CB2配体。该模板周围的结构-活性关系导致鉴定出S-777469为选择性CB2受体激动剂,该化合物在1.0 mg / kg po和10 mg / kg po下表现出对化合物48/80诱导的刮擦的显着抑制作用(55 %和61%)。
Zinc(II)-Catalyzed Synthesis of Propargylamines by Coupling Aldimines and Ketimines with Alkynes
作者:Syeda Aaliya Shehzadi、Aamer Saeed、Filip Lemière、Bert U. W. Maes、Kourosch Abbaspour Tehrani
DOI:10.1002/ejoc.201701567
日期:2018.1.10
Imines derived from unactivated aldehydes or ketones and primary amines or α‐amino acid esters have been shown to undergo a ZnII‐catalyzed reaction with a variety of terminal alkynes to give secondary propargylamines that have tri‐ and tetrasubstituted α‐carbon atoms (from aldimines and ketimines, respectively).
catalyst was developed to produce biomass-derived 5-methylpyrrolidone under room temperature and atmospheric hydrogen. The suitable mesoporous structure created high dispersion of Pt species and accelerated the reaction processes. The isomerization of imine to enamine on the catalyst made this conversion easy undermildconditions.
SYNTHESIS AND PHYSIOLOGICAL ACTIVITIES OF NEW ACYCLIC AMINOPHOSPHONATES
作者:J. S. Wieczorek、R. Gancarz、K. Bielecki、E. Grzyś、J. Sarapuk
DOI:10.1080/10426500008076535
日期:2000.1.1
The dependence of biological activity of 37 newly synthesized acyclic aminomethanephosphonic acid derivatives on their structure was studied. It was found that the phytotoxicity of the compounds studied depended on their hydrophobic parameters, and in a smaller extent on the electronic parameters of the substituents on nitrogen and phosphorus atoms. No phytotoxicity dependence on the steric parameters of compounds was found. Tested organism was Spirodela oligorrhiza and the parameter studied was the concentration of compounds causing 50 % growth inhibition (EC50) The test had preliminary character and permitted to eliminate the less promising compounds out of further studies.
Bianchetti,G. et al., Gazzetta Chimica Italiana, 1967, vol. 97, p. 289 - 303