作者:Gianfranco Balboni、Ilaria Lazzari、Claudio Trapella、Lucia Negri、Roberta Lattanzi、Elisa Giannini、Annalisa Nicotra、Pietro Melchiorri、Sergio Visentin、Chiara De Nuccio、Severo Salvadori
DOI:10.1021/jm800854e
日期:2008.12.11
basis of a Janssen's patent, we approached a new synthesis of some 1,3,5-triazin-4,6-diones as potential non peptidic prokineticin receptor antagonists, containing the following substitutions: (N(1) and N(5) link a 4-methoxybenzyl and a 4-ethylbenzyl, respectively; C(2) can link an amino-ethyl-guanidine (reference compound 1) or an ethylendiamine (2) or an amino-ethyl-amino-2-imidazoline (3). New compounds
根据Janssen的专利,我们研究了一些新的1,3,5-triazin-4,6-diones作为潜在的非肽促动力肽受体拮抗剂的合成方法,它包含以下取代基:(N(1)和N(5 )分别连接4-甲氧基苄基和4-乙基苄基; C(2)可以连接氨基-乙基胍(参考化合物1)或乙基乙二胺(2)或氨基-乙基-氨基-2-咪唑啉(3 )。评估了新化合物的PKR1和PKR2亲和力,并以抑制1 nM Bv8诱导的细胞内Ca2 +动员的方式评估了拮抗剂的性能。