Chemical and Pharmaceutical Bulletin p. 1374 - 1382 (1998)
Update date:2022-08-02
Topics:
Okada, Yoshio
Tsukatani, Masaki
Taguchi, Hiroaki
Yokoi, Toshio
Bryant, Sharon D.
Lazarus, Lawrence H.
An amino group was introduced to the 3 or 6 position of a pyrazinone ring by cyclization of dipeptidyl chloromethyl ketones. Boc-Tyr-OH was coupled with the amino function, followed by removal of the Boc group to give pyrazinone ring-containing tyrosine derivatives. Of the various tyrosine derivatives prepared, 5-methyl-6-β-phenethyl-3-tyrosylaminobutyl-2(1H)- pyrazinone exhibited strong binding to the μ-opioid receptor with a K(i) value of 55.8 nM and to the δ-opioid receptor with a K(i) value of 2165 nM and with a K(i)μ/K(i)δ value of 0.026.
View MoreNanjing Norris Pharm Technology Co., Ltd.
Contact:+86-13901585132
Address:2 Qiande Road, Jiangning sciencepark Hi-Tech Zone, Nanjing, P.R.China
website:http://www.sjc.com.tw
Contact:(886) 2-2396-6223
Address:14Fl., No. 99. Sec. 2, Jen Ai Road
Contact:021-36356756
Address:Room601,Building No.14,280 Yangcheng Road,Shanghai
PharmaResources(Kaiyuan)CO,.Ltd
Contact:+86-21-50720028
Address:No.3, Beihuan Road, Economic Development District, Kaiyuan City, Tieling City, Liaoning Province, China 112300
website:http://www.win-winchemical.com
Contact:0086-577-64498589
Address:6F, No. 396 Xingping Road, Longwan Industrial Zone, Wenzhou City, Zhejiang, 325000 P.R.China
Doi:10.1021/jo00864a025
(1976)Doi:10.1039/a803819h
(1998)Doi:10.1039/DT9790000654
()Doi:10.1021/jo01298a026
(1980)Doi:10.1021/ja00812a047
(1974)Doi:10.1021/ol0341750
(2003)
