Preparation of 9-deoxo-4"-deoxy-6,9-epoxyerythromycin lactams "motilactides": potent and orally active prokinetic agents

Bioorg Med Chem Lett. 1998 Apr 7;8(7):805-10. doi: 10.1016/s0960-894x(98)00111-5.

Abstract

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.

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Biological Availability
  • Dogs
  • Epoxy Compounds / chemical synthesis*
  • Epoxy Compounds / chemistry
  • Epoxy Compounds / pharmacology
  • Erythromycin / analogs & derivatives*
  • Erythromycin / chemical synthesis*
  • Erythromycin / chemistry
  • Erythromycin / pharmacology
  • Indicators and Reagents
  • Molecular Structure
  • Myoelectric Complex, Migrating / drug effects*
  • Myoelectric Complex, Migrating / physiology
  • Prodrugs / chemical synthesis
  • Prodrugs / chemistry
  • Prodrugs / pharmacology
  • Receptors, Gastrointestinal Hormone / agonists
  • Receptors, Neuropeptide / agonists
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Epoxy Compounds
  • Indicators and Reagents
  • Prodrugs
  • Receptors, Gastrointestinal Hormone
  • Receptors, Neuropeptide
  • motilin receptor
  • Erythromycin