5473. Lexipafant

Nomenclature

CAS number: 139133-26-9
N-Methyl-N-[[4-[(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)methyl]phenyl]sulfonyl]-l-leucine ethyl ester; N-methyl-N-[[α-(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)-p-tolyl]sulfonyl]-l-leucine ethyl ester; BB-882; Zacutex (Brit. Biotech).
C23H30N4O4S; mol wt 458.57.
C 60.24%, H 6.59%, N 12.22%, O 13.96%, S 6.99%.

Description and references

Platelet activating factor (PAF) antagonist. Prepn: M. Whittaker, A. Miller, WO 9203422; eidem, US 5200412 (1992, 1993 both to British Bio-Technology). Structure-activity report: M. Whittaker et al., J. Lipid Mediators Cell Signalling 10, 151 (1994). Pharmacology: F. M. Abu-Zidan et al., Pharmacol. Toxicol. 78, 23 (1996). Clinical evaluation in acute pancreatitis: A. N. Kingsnorth et al., Br. J. Surg. 82, 1414 (1995).

Chemical structure

Properties

White crystalline solid from ethyl acetate, mp 105°. [α]D20 6.7° (c = 2.0 in CDCl3).

Therapeutic Category

Anti-inflammatory.

Keywords

Anti-inflammatory (Nonsteroidal); Platelet Activating Factor Antagonist