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.
supporting information, (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.
SPIROCYCLIC ISOXAZOLINE DERIVATIVES AS ANTIPARASITIC AGENTS
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, (2013/03/26)
The invention recites spirocyclic isoxazoline derivatives of Formula (V.1), Formula (V.2), Formula (V.1.1), and Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, processes for making, and their use as a parasi
ISOXAZOLINE DERIVATIVES AS ANTIPARASITIC AGENTS
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, (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.
Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70
Vu, Chi B.,Corpuz, Evelyn G.,Merry, Taylor J.,Pradeepan, Selvaluxmi G.,Bartlett, Catherine,Bohacek, Regine S.,Botfield, Martyn C.,Eyermann, Charles J.,Lynch, Berkley A.,MacNeil, Ian A.,Ram, Mary K.,Van Schravendijk, Marie Rose,Violette, Shelia,Sawyer, Tomi K.
, p. 4088 - 4098 (2007/10/03)
A series of 1,2,4-oxadiazole analogues has been shown to be potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70, a potential therapeutic target for immune suppression. These compounds typically are 200- 400-fold more potent than the native,