2804. Dalfopristin

Nomenclature

CAS number: 112362-50-2
(26R,27S)-26-[[2-(Diethylamino)ethyl]sulfonyl]-26,27-dihydrovirginiamycin M1; 26-(2-diethylaminoethyl)sulfonylpristinamycin IIB; RP-54476.
C34H50N4O9S; mol wt 690.85.
C 59.11%, H 7.29%, N 8.11%, O 20.84%, S 4.64%.

Description and references

Semisynthetic polyunsaturated macrolactone type II streptogramin, q.v. Prepn: J.-C. Barriere et al., EP 191662; eidem, US 4668669 (1986, 1987 both to Rhone-Poulenc). In vitro activity: H. C. Neu et al., J. Antimicrob. Chemother. 30, Suppl. A, 83 (1992). HPLC determn in plasma: A. Le Liboux et al., J. Chromatogr. B 708, 161 (1998)

Chemical structure

Properties

White solid, mp ≈150°.

Derivative

Mixture with quinupristin.

Nomenclature

CAS number: 126602-89-9
RP-59500; Synercid (Rh^one-Poulenc).

Description and references

Semisynthetic streptogramin comprised of two synergistic components in a defined 70:30 percent w/w mixture of dalfopristin and quinupristin, q.v., mesylate salts. HPLC determn for quality control: B. Vasselle et al., J. Pharm. Biomed. Anal. 19, 641 (1999). In vitro activity in comparison with pristinamycin, q.v.: A. Lozniewski et al., Pathol. Biol. 48, 463 (2000). Clinical trial in vancomycin resistant Enterococcus faecium (VREF) infection: R. C. Moellering et al., J. Antimicrob. Chemother. 44, 251 (1999); in skin infections: R. L. Nichols et al., ibid. 263. Review: B. Pavan, Curr. Opin. Investig. Drugs 1, 173-180 (2000).

Therapeutic Category

Antibacterial.

Keywords

Antibacterial (Antibiotics)