19283-13-7Relevant articles and documents
Simple and efficient synthesis of N-alkyl and N-aryl succinimides in hot water
Bozdo?an, Burcu,Er?at?r, Mehmet,Demirkol, Onur,Akba?lar, Dilek,Giray, E. Sultan
, p. 217 - 223 (2017/01/22)
A new, simple synthesis of succinimides is described. The reactions were carried out under the ultimate green conditions excluding both catalyst and organic solvent by applying simple stirring at 100 °C. A wide variety of N-susbstituted succinimides have been prepared in high yields by using succinic acid and primary amines in hot water. Yield of N-alkyl substituted succinimides were found to be higher than those of N-aryl substituted succinimides.
Binaltorphimine-Related Bivalent Ligands and Their κ Opioid Receptor Antagonist Selectivity
Portoghese, P. S.,Nagase, H.,Lipkowski, A. W.,Larson, D. L.,Takemori, A. E.
, p. 836 - 841 (2007/10/02)
In an effort to develop selective antagonists for κ opioid receptors, bivalent ligands that contain opioid antagonist pharmacophores derived from naltrexone or other morphinans were synthesized and tested on the guinea pig ileum (GPI) and mouse vas deferens (MVD) preparations.The minimum requirements for κ selectivity are at least one free phenolic OH group and one N-cyclopropyl or N-allyl substituent.Several compounds (3, 8, 10) with κ selectivity as good as or better than norbinaltorphimine (nor-BNI, 2) were discovered.The structure-activity relationship revealed that the pyrrole ring functions strictly as a spacer and does not contribute to κ selectivity.The pharmacologic data suggest that only one antagonist pharmacophore may be required for κ selectivity and that the other morphinan portion of the molecule confers selectivity by interacting with a unique subsite proximal to the antagonist pharmacophore recognition locus.
