Synthesis and biological activity of substance P C-terminal hexapeptide analogues: structure-activity studies

Citations Over TimeTop 18% of 1986 papers

Abstract

A series of analogues of the C-terminal hexapeptide of substance P, modified at the glutaminyl residue, was synthesized and their relative activities as spasmogens were determined in the guinea pig ileum and rat colon muscularis mucosae preparations in vitro. In general, when compared to SP6-11, the loss of the carboxamide group has little effect on activity in the colon and reduces activity on the ileum. The exception to this is the Orn6 analogue which retains activity on both preparations and is proposed as a useful tool for structure-activity studies. It is concluded that the hydrogen-bonding potential of the position 6 substituent may be an important determinant of biological activity.

Related Papers

• → Novel Synthesis, Cytotoxic Evaluation, and Structure−Activity Relationship Studies of a Series of α-Alkylidene-γ-lactones and Lactams(2005)107 cited
• → Synthesis, topoisomerase I inhibition and structure–activity relationship study of 2,4,6-trisubstituted pyridine derivatives(2004)95 cited
• → Molecular docking and structure–activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors(2010)22 cited
• → Ring-truncated deguelin derivatives as potent Hypoxia Inducible Factor-1α (HIF-1α) inhibitors(2015)28 cited
• → Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors containing a stereochemically unique peptide isostere(1993)24 cited