219540-76-8Relevant academic research and scientific papers
Design and synthesis of a novel series of orally active, selective somatostatin receptor 2 agonists for the treatment of type 2 diabetes
Banno, Yoshihiro,Sasaki, Shigekazu,Kamata, Makoto,Kunitomo, Jun,Miyamoto, Yasufumi,Abe, Hidenori,Taya, Naohiro,Oi, Satoru,Watanabe, Masanori,Urushibara, Tomoko,Hazama, Masatoshi,Niwa, Shin-ichi,Miyamoto, Saku,Horinouchi, Akira,Kuroshima, Ken-ichi,Amano, Nobuyuki,Matsumoto, Shin-ichi,Matsunaga, Shinichiro
, p. 5995 - 6006 (2017/10/10)
The discovery of a novel series of β-methyltryptophan (β MeTrp) derivatives as selective and orally active non-peptide somatostatin receptor 2 (SSTR2) agonists for the treatment of Type 2 diabetes is described. In our previous research, Compound A, β-MeTr
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter
Efange, Simon M. N.,Khare, Anil B.,Von Hohenberg, Krystyna,MacH, Robert H.,Parsons, Stanley M.,Tu, Zhude
scheme or table, p. 2825 - 2835 (2010/08/05)
To identify selective high-affinity inhibitors of the vesicular acetylcholine transporter (VAChT), we have interposed a carbonyl group between the phenyl and piperidyl groups of the prototypical VAChT ligand vesamicol and its more potent analogues benzovesamicol and 5-aminobenzovesamicol. Of 33 compounds synthesized and tested, 6 display very high affinity for VAChT (K i, 0.25-0.66 nM) and greater than 500-fold selectivity for VAChT over σ1 and σ2 receptors. Twelve compounds have high affinity (Ki, 1.0-10 nM) and good selectivity for VAChT. Furthermore, 3 halogenated compounds, namely, trans-3-[4-(4-fluorobenzoyl) piperidinyl]-2-hydroxy-1,2,3,4-tetrahydronaphthalene (28b) (Ki = 2.7 nM, VAChT/sigma selectivity index = 70), trans-3-[4-(5-iodothienylcarbonyl) piperidinyl]-2-hydroxy-1,2,3,4-tetrahydronaphthalene (28h) (Ki = 0.66 nM, VAChT/sigma selectivity index = 294), and 5-amino-3-[4-(p-fluorobenzoyl) piperidinyl]-2-hydroxy-1,2,3,4,-tetrahydronaphthalene (30b) (Ki = 2.40 nM, VAChT/sigma selectivity index = 410) display moderate to high selectivity for VAChT. These three compounds can be synthesized with the corresponding radioisotopes so as to serve as PET/SPECT probes for imaging the VAChT in vivo.
Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors
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Page/Page column 56, (2010/11/28)
The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specificat
