Chroman-4-one and chromone based somatostatin beta-turn mimetics

• A scaffold approach has been used to develop somatostatin beta-turn mimetics based on chroman-4-one and chromone ring systems. Such derivatives could adopt conformations resembling type II or type II' beta-turns. Side chain equivalents of the crucial Trp8 and Lys9 in somatostatin were introduced in the 2- and 8-positions of the scaffolds using efficient reactions. Interestingly, this proof-of-concept study shows that 4 and 9 have K-i-values in the low mu M range when evaluated for their affinity for the sst2 and sst4 receptors. (C) 2016 Elsevier Masson SAS. All rights reserved.

Ämnesord

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)

MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)

Nyckelord

Chromone

Chroman-4-one

Peptidomimetics

Somatostatin

binding affinities

nonpeptide peptidomimetics

natural-products

analog

receptors

scaffolds

design

conformation

polypeptide

peptides

Pharmacology & Pharmacy

Publikations- och innehållstyp

ref (ämneskategori)

art (ämneskategori)