249647-26-5Relevant articles and documents
The Discovery and Structure-Activity Evaluation of (+)-Floyocidin B and Synthetic Analogs
Bauer, Armin,Becker, Jonathan,Hammann, Peter,Kleiner, Yolanda,Kurz, Michael,Marner, Michael,Mihajlovic, Sanja,Vilcinskas, Andreas,Zubeil, Florian,K?nig, Henrik F.,Kl?dtke, Jannike,P?verlein, Christoph,Sch?berle, Till F.,Schuler, S?ren M. M.
, (2021/11/18)
Tuberculosis represents one of the ten most common courses of death worldwide and the emergence of multidrug-resistant M. tuberculosis makes the discovery of novel anti-tuberculosis active structures an urgent priority. Here, we show that (+)-floyocidin B representing the first example of a novel dihydroisoquinoline class of fungus-derived natural products, displays promising antitubercular hit properties. (+)-Floyocidin B was identified by activity-guided extract screening and its structure was unambiguously determined by total synthesis. The absolute configuration was deduced from a key synthesis intermediate by single crystal X-ray diffraction analysis. A hit series was generated by the isolation of further natural congeners and the synthesis of analogs of (+)-floyocidin B. Extensive biological and physicochemical profiling of this series revealed first structure-activity relationships and set the basis for further optimization and development of this novel antitubercular scaffold.
ISOXAZOLINE DERIVATIVES AS ANTIPARASITIC AGENTS
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Paragraph 0762; 0763, (2013/03/26)
This invention recites isoxazoline substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in mammals and birds. R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.