3686. Erythromycin Propionate

Nomenclature

CAS number: 134-36-1
Erythromycin 2′-propanoate; propionylerythromycin; monopropionylerythromycin; Propiocine (Hoechst).
C40H71NO14; mol wt 789.99.
C 60.81%, H 9.06%, N 1.77%, O 28.35%.

Description and references

Semi-synthetic macrolide antibiotic. Prepn: V. C. Stephens, US 2993833 (1961 to Lilly); V. C. Stephens, J. W. Conine, Antibiot. Annu. 1958-59, 346. Pharmacology and toxicology: C. Lee et al., ibid. 354. Clinical studies: R. S. Griffith, ibid. 364; D. M. Perry et al., ibid. 375. Clinical pharmacokinetics: M. Ducci et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 19, 494 (1981). HPLC determn in plasma: W. Xiao et al., J. Chromatogr. B 817, 153 (2005).

Derivative

Monohydrate.

Properties

Crystals from acetone + water, mp 122-126°. [α]D25 -81.6° (acetone). pKa: 6.9. Very slightly sol in water. Readily sol in methanol, ethanol, acetone, ethyl acetate, DMF. LD50 in mice, rats (g/kg): 2.87, >5.0 orally; >5.0, >5.0 s.c. (Lee).

Therapeutic Category

Antibacterial.

Keywords

Antibacterial (Antibiotics); Macrolides