Potent macrocyclic antagonists to the motilin receptor presenting novel unnatural amino acids.
Novel, potent small molecule motilin receptor antagonists are described. These peptidomimetic macrocycles are composed of a tripeptide cyclized backbone-to-backbone with a nonpeptidic tether and bear new unnatural amino acids containing basic side chains.
Marsault
Eric
E
Tranzyme Pharma Inc. 3001, 12e av Nord, Sherbrooke, PQ, Canada J1H5N4. emarsault@tranzyme.com
Benakli
Kamel
K
Beaubien
Sylvie
S
Saint-Louis
Carl
C
Déziel
Robert
R
Fraser
Graeme
G
D000596:Amino Acids / Q000737:chemistry*; D003500:Cyclization; D047028:Macrocyclic Compounds / Q000494:pharmacology*; D011964:Receptors, Gastrointestinal Hormone / Q000037:antagonists & inhibitors* / Q000737:chemistry; D018013:Receptors, Neuropeptide / Q000037:antagonists & inhibitors* / Q000737:chemistry
D000596:Amino Acids; D047028:Macrocyclic Compounds; D011964:Receptors, Gastrointestinal Hormone; D018013:Receptors, Neuropeptide; C050802:motilin receptor