[(5-アミノ-1H-1,2,4-トリアゾール-3-イル)チオ]酢酸(3aS,4R,5S,6R,8R,9R,9aR,10R)-6-エチルデカヒドロ-5-ヒドロキシ-4,6,9,10-テトラメチル-1-オキソ-3a,9-プロパノ-3aH-シクロペンタシクロオクテン-8-イル

説明Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources). It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms. Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.

使用Azamulin is a semi-synthetic pleuromutilin prepared by sequential reaction of dihydropleuromutilin tosylate with 2-amino-1,2,4-triazole-5-thiol. While azamulin is a broad spectrum antibiotic in the pleuromutilin class, this aspect of its bioprofile has received little attention. In fact, the triazole substituent added to nominally improve the drugs bioavailability, imparted an unusual selectivity for the inhibition of specific cytochrome P450 mixed function oxidase sub-types, important for understanding the manner in which the body metabolises drugs or xenobiotics.

一般的な説明Azamulin isolated from fungus Pleurotus mutilis is a diterpene antibiotic. It is related to pleuromutilin being its synthetic azole derivative.