Peripherally acting enkephalin analogs. 2. Polar tri-and tetrapeptides

…, LA Lowe, G Mills, PY Sang, DSA Simpkin…

Index: Hardy, George W.; Lowe, Lawrence A.; Mills, Gail; Sang, Pang Yih; Simpkin, Dean S. A.; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 1108 - 1118

Full Text: HTML

Citation Number: 22

Abstract

The design, synthesis, and biological activity of a series of DArgZ-enkephalin-derived tetrapeptide amides and tripeptide aralkylamides are reported. These polar analogues were designed to be excluded from the central nervous system with their action thus limited to peripheral opioid receptors. The effects of the nature of the aromatic ring, aryl ring substitution, and aralkylamine chain length on activity were investigated; in a number of ...

Related Articles:

Potential antitumor agents. 36. Quantitative relationships between experimental antitumor activity, toxicity, and structure for the general class of 9-anilinoacridine …

[Denny, William A.; Cain, Bruce F.; Atwell, Graham J.; Hansch, Corwin; Panthananickal, Augustine; Leo, A. Journal of Medicinal Chemistry, 1982 , vol. 25, # 3 p. 276 - 300]

Synthesis and pharmacological studies of N-substituted 6-[(2-aminoethyl) amino]-1, 3-dimethyl-2, 4 (1H, 3H)-pyrimidinediones, novel class III antiarrhythmic agents

[Katakami; Yokoyama; Miyamoto; Mori; Kawauchi; Nobori; San-nohe; Kaiho; Kamiya Journal of Medicinal Chemistry, 1992 , vol. 35, # 18 p. 3325 - 3330]

Synthesis and pharmacological studies of N-substituted 6-[(2-aminoethyl) amino]-1, 3-dimethyl-2, 4 (1H, 3H)-pyrimidinediones, novel class III antiarrhythmic agents

[Katakami; Yokoyama; Miyamoto; Mori; Kawauchi; Nobori; San-nohe; Kaiho; Kamiya Journal of Medicinal Chemistry, 1992 , vol. 35, # 18 p. 3325 - 3330]

A new type of ketolides bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether synthesis and structure–activity relationships

[Nomura, Takashi; Iwaki, Tsutomu; Yasukata, Tatsuro; Nishi, Koichi; Narukawa, Yukitoshi; Uotani, Koichi; Hori, Toshihiko; Miwa, Hideaki Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 24 p. 6615 - 6628]

A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists

[Dannhardt, Gerd; Gruchalla, Markus V.; Kohl, Beate K.; Parsons Archiv der Pharmazie, 2000 , vol. 333, # 8 p. 267 - 274]

More Articles...