Erythromycin A cyclic 11,12-carbonate

説明Davercin is a macrolide antibiotic that inhibits bacterial protein synthesis by targeting the 50S ribosomal subunit, blocking the progression of nascent polypeptide chains. It has broad-spectrum activity against various Gram-positive and Gram-negative bacteria (MICs = 0.02-50 μg/ml). Davercin is non-toxic to mice and rats (LD50s = 4.05 and 5.9 g/kg, respectively). Formulations containing davercin have been used to treat a variety of urogenital bacterial infections.

使用Davercin (erythromycin A cyclic 11,12-carbonate) is a first generation semi-synthetic erythromycin. Davercin is prepared by coupling the 11- and 12-OH groups to form a cyclic carbonate. This simple modification improves the stability and hydrophobicity of the macrocyclic structure. Davercin shows comparable or better in vitro potency, low host toxicity and improved pharmacokinetics compared with erythromycin.