Synthesis and antifungal activity of ASP9726, a novel echinocandin with potent Aspergillus hyphal growth inhibition.

The synthesis and antifungal activity of ASP9726, a novel echinocandin with potent Aspergillus hyphal growth inhibition and significantly improved MIC against Candida parapsilosis and echinocandin resistant-Candida is described.

4-(1-benzoylindol-3-yl)butyric acids and FK143: novel nonsteroidal inhibitors of steroid 5 alpha-reductase (II).

A novel series of indolebutyric acids with varying benzoyl substituents were synthesized to develop nonsteroidal inhibitors of steroid 5 alpha-reductase. We previously reported the discovery of a novel nonsteroidal 5 alpha-reductase inhibitor, FR119680, which had an IC50 value of 5.0 nM against the rat prostatic enzyme.

Total synthesis of WS9326A, a potent tachykinin antagonist from Streptomyces violaceoniger.

Total synthesis of the cyclic peptide lactone WS9326A, a potent tachykinin antagonist isolated from Streptomyces violaceoniger strain 9326, has been achieved via Cbz-Thr(Boc-allo-Thr-Asn-Ser(Bzl)-(E)delta MeTyr-Leu-D-Phe-OTce, which was cyclized (Phe and allo-Thr) using an active ester method with N-hydroxysuccinimide. Finally the unique N-acyl group, the 2-(1(Z)-pentenyl)cinnamoyl moiety, was introduced onto the amino group in the Thr unit. The key step of the synthesis involves the preparation of the E-isomer of the dehydro-N-methyltyrosine (delta MeTyr) unit.

WF11605, an antagonist of leukotriene B4 produced by a fungus. II. Structure determination.

The structure of WF11605, a novel tetracyclic triterpene glucoside, was determined to be 1. The plane structure of deacetyl-WF11605 aglycone was elucidated as 2 through the concerted application of a series of 2D NMR techniques. The relative configurations were established by X-ray crystallographic analysis of bis(p-bromobenzoyl) derivative 3 and absolute stereochemistry by CD exciton chirality method.