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Synthesis of new analogs of echinocandin B by enzymatic deacylation and chemical reacylation of the echinocandin B peptide: synthesis of the antifungal agent cilofungin (LY121019).

par Debono, M;Abbott, B J;Fukuda, D S;Barnhart, M;Willard-Gallo, Karen ;Molloy, R M;Michel, K H;Turner, J R;Butler, T F;Hunt, A H
Référence Journal of antibiotics, 42, 3, page (389-397)
Publication Publié, 1989-03

Article révisé par les pairs

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Résumé :

The antifungal antibiotic, echinocandin B (ECB), was modified by a sequential procedure in which the initial step involved enzymatic removal of the native N-linoleoyl group from the N-terminus using an Actinoplanes utahensis culture. The resulting product, ECB nucleus, was reacylated using active esters or acid halides of various substituted acids to give a series of ECB analogs. These analogs possessed anti-Candida activity both in vitro and in vivo (mice). Other studies have shown that one of these, cilofungin, the 4-n-octyloxybenzoyl-ECB analog (LY121019), has excellent anti-Candida activity, low toxicity and is superior to other available antifungal antibiotics.