Structure of a new macrolide antibiotic, X-14952B.

The Journal of Antibiotics
1985.0

Abstract

Recently, new macrolide antibiotics possessing various biological activities have been isolated from fermentation broths of streptomycetes. In the course of our search for antimicrobial substances from microorganisms, a new antibacterial antibiotic, X-14952B (1) was isolated from the fermentation broth of a Streptomyces sp. We report the structure elucidation of 1 by means of 1H and 13C NMR spectroscopic analyses. Antibiotic 1 has a molecular formula C42H69NO12 deduced from FAB-MS, elemental analysis and 13C NMR. The 13C NMR spectrum demonstrated that 1 is structurally similar to irumamycin (2), with the presence of 3-O-carbamoyl-2-deoxy-β-D-rhamnoside indicated by anomeric and carbamoyl carbons, and the aglycone moiety coinciding with 2. However, 1 lacks the epoxy carbons of 2 but has additional oxygen-bonded and methine carbons, indicating a different alkyl side chain. The structure of the C12 alkyl side chain of 1 was deduced from 2D-NMR analysis and a retroaldol reaction which yielded 3-hexanone. Combined evidence supports structure 1 for X-14952B as a 20-membered macrolide lactone attached to a neutral sugar and a C12 alkyl sidechain. Notably, the slight structural difference in the side-chains of 1 and irumamycin (2) results in 1 being primarily an antibacterial agent and 2 an antifungal agent, similar to structure-activity effects seen in other macrolides like concanamycins, virustomycin A, bafilomycin and L-681,110A.

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