Preparation of 9-deoxo-4"-deoxy-6,9-epoxyerythromycin lactams "motilactides": potent and orally active prokinetic agents.
A series of new, highly potent and orally active "motilactides", 9-deoxo-4"-deoxy-6,9-epoxyerythromycin lactams was designed, synthesized, and evaluated for their gastrointestinal motor stimulating activity. These compounds were acid stable and showed good oral efficacy.
Faghih
R
R
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064, USA.
Nellans
H N
HN
Lartey
P A
PA
Petersen
A
A
Marsh
K
K
Bennani
Y L
YL
Plattner
J J
JJ
D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001682:Biological Availability; D004285:Dogs; D004852:Epoxy Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007202:Indicators and Reagents; D015394:Molecular Structure; D016065:Myoelectric Complex, Migrating / Q000187:drug effects* / Q000502:physiology; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011964:Receptors, Gastrointestinal Hormone / Q000819:agonists; D018013:Receptors, Neuropeptide / Q000819:agonists; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D004852:Epoxy Compounds; D007202:Indicators and Reagents; D011355:Prodrugs; D011964:Receptors, Gastrointestinal Hormone; D018013:Receptors, Neuropeptide; C050802:motilin receptor; D004917:Erythromycin