Disease relevance of Erythromyclamine

• Effect of medium pH on the activity of dirithromycin and erythromycylamine in Bactec broth against Mycobacterium avium complex [1].
• To overcome erythromycin A resistance within Gram-positive cocci and bacteria, novel compounds have been semi-synthesised, such as ketolides and C-4'' carbamate erythromycylamine derivatives [2].

High impact information on Erythromyclamine

• Under these particular conditions, inhibition of ribosomal protein synthesis by dirithromycin was < 10% of the value measured for erythromycylamine [3].
• An enriched sample of epidirithromycin (95% purity) was synthesized by condensing erythromycylamine and 2-(2-methoxyethoxy)acetaldehyde in diethyl ether as the reaction solvent, and the product was fully characterized by nuclear magnetic resonance spectroscopy and high-pressure liquid chromatographic (HPLC) analysis [3].
• The formation of a cytochrome P-450 type I binding spectrum and a metabolic intermediate complex by troleandomycin, erythromycin, dirithromycin, and erythromycylamine was also assessed in microsomes prepared from human livers [4].
• Synthesis and structure-activity relationships of new 9-N-alkyl derivatives of 9(S)-erythromycylamine [5].
• A series of new 9-N-alkyl derivatives of 9(S)-erythromycylamine has been synthesized by reductive alkylation of erythromycylamine with aliphatic aldehydes and sodium cyanoborohydride [5].

Biological context of Erythromyclamine

• Dirithromycin is rapidly converted by non-enzymatic hydrolysis during absorption to erythromycylamine, which is microbiologically active [6].
• Structure-activity relationships among 9-N-alkyl derivatives of erythromycylamine and their effect on the oxidative burst of human neutrophils in vitro [7].

Anatomical context of Erythromyclamine

• Here we have extended the analysis of structure-activity relationships by studying the effects of five 9-N-alkyl derivatives of erythromycylamine on oxidant production by human neutrophils in vitro [7].

Associations of Erythromyclamine with other chemical compounds

• Dirithromycin and erythromycylamine were low affinity inhibitors of CYP3A (inhibitory binding affinities of 493 mumol/L and 701 mumol/L, respectively); conversely, terfenadine was a moderate affinity inhibitor (inhibitory binding affinity of 28 mumol/L) [8].
• Both erythromycin and puromycin affect fluorescence from fluorescent derivatives of aminoacyl-tRNAs, while both puromycin and aminoacyl-tRNAs affect fluorescence of fluorescent derivatives of erythromycylamine [9].

Gene context of Erythromyclamine

• The authors compared the abilities of dirithromycin (a new macrolide antibiotic agent), its major metabolite erythromycylamine, and the known CYP3A substrate terfenadine to inhibit CYP3A in vitro [8].

References