On November 19, 1998, Liu, Shenquan; Tang, Cheng; Ho, Bin; Ankersen, Michael; Stidsen, Carsten E.; Crider, A. Michael published an article.Synthetic Route of 199522-66-2 The title of the article was Nonpeptide Somatostatin Agonists with sst4 Selectivity: Synthesis and Structure-Activity Relationships of Thioureas. And the article contained the following:
Utilizing NNC 26-9100 as a structural lead, a variety of nonpeptide derivatives of somatostatin were synthesized and evaluated for sst2 and sst4 receptor binding affinity. A novel thiourea scaffold was utilized to attach (1) a heteroaromatic nucleus to mimic the Trp8 residue, (2) a nonheteroarom. nucleus to mimic Phe7, and (3) a primary amine or other basic group to mimic the Lys9 residue of somatostatin. Displacement studies were carried out using membranes from cell lines expressing ssts [BHK cells (sst4) and HEK 293 cells (sst2)] utilizing [125I]Tyr11-SRIF as the radioligand. Several thioureas and an urea derivative exhibited Ki values of less than 100 nM. Two thioureas and the urea derivative are believed to be the most potent nonpeptide sst4 agonists known with Ki of 6, 16, and 14 nM, resp. Since the thiourea and the urea derivatives exhibit high sst4 selectivity, these novel nonpeptide derivatives may be useful tools for studying the sst4 receptor. Studies are currently in progress to evaluate the therapeutic potential of NNC 26-9100 in the treatment of glaucoma. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Synthetic Route of 199522-66-2
The Article related to thiourea preparation structure somatostatin agonist, nnc26910 derivative somatostatin sst4 receptor agonist, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 199522-66-2