A Pd-catalyzed highly regioselective 6-exo-dig cyclization/alkenylation reaction of ortho-ethynylanilides has been developed. This tandem cross-coupling protocol represents a simple, efficient, step- and atom-economic approach for the construction of scarcely known polyene-substituted benzo[d][1,3]oxazines in moderate to excellent yields with a broad substrate scope.

The structure of tetrafibricin, a novel and potent fibrinogen receptor antagonist isolated from the culture broth of Streptomyces neyagawaensis NR0577, was determined. Tetrafibricin has a unique structure containing primary amine, conjugated tetraenoic acid, and polyhydroxy functionalities that is biosynthetically related to the polyene macrolide antibiotics.

Strain JAU4234, identified as Streptomyces padanus, was isolated from soil collected in Jiangxi Province, China. It produced actinomycin X2, fungichromin, and a new polyene macrolide compound with antifungal activity, antifungalmycin 702. Antifungalmycin 702 had good general antifungal activity and may have potential future agricultural and/or clinical applications.

A new member of the polyene family, N-dimethylaminoacetyl-partricin A 2-dimethylaminoethylamide diaspartate (SPA), was investigated and was found to be more effective than amphotericin B (i) in vivo by enhancing mouse resistance to cryptococcal meningoencephalitis and (ii) in vitro by potentiating the anticryptococcal activity of murine microglial cells.

Even though it is highly toxic, Amphotericin B (AmB), an amphipathic polyene macrolide antibiotic, is used in the treatment of severe systemic fungal infections as a life-saving drug. To examine the influence of conformational factors on selective toxicity of these compounds, we have investigated the conformational properties of five AmB amide derivatives. It was found that the extended conform...

The constitution of vacidin A, a representative of the aromatic heptaene macrolide antibiotics was established on the basis of 13C and 1H-1H double quantum filtered correlated spectroscopy, rotating frame nuclear Overhauser effect spectroscopy, J-resolved 1H as well as 1H-13C correlation NMR spectra. Geometry of the polyene chromophore was determined as 22E,24E,26E,28Z,30Z,32E,34E.

Streptomyces sp. TP-A0871 produces the polyene macrolactam heronamide C. Here, we report its draft genome sequence to get insight into heronamide biosynthesis and genome-mining for novel secondary metabolites of polyketide and nonribosomal peptide classes. The genome encodes over nine orphan gene clusters for polyketide and/or nonribosomal peptide syntheses.

The in vitro activity of a new water-soluble polyene, SPA-S-843, was evaluated against 116 strains of Candida, Cryptococcus, and Saccharomyces spp. and compared with that of amphotericin B. SPA-S-843 demonstrated better inhibitory activity against all of the yeasts examined and better fungicidal activity against Candida albicans, Candida glabrata, Candida krusei, and Candida tropicalis than did...