1078132-25-8Relevant articles and documents
Synthesis of Spiropentadiene Pyrazolones by Rh(III)-Catalyzed Formal sp3 C-H Activation/Annulation
Zheng, Jiuan,Li, Panpan,Gu, Meng,Lin, Aijun,Yao, Hequan
supporting information, p. 2829 - 2832 (2017/06/07)
A Rh-catalyzed enol-directed formal sp3 C-H activation/annulation of α-arylidene pyrazolones with alkynes has been developed. This reaction provides a convenient route to synthesize spiropentadiene pyrazolones in good to excellent yields at room temperature, exhibiting good functional group tolerance, gram scalability, and high regioselectivity. Of note, the α-arylidene pyrazolone was introduced as a novel C3 synthon in C-H activation/annulation.
Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis
Castagnolo, Daniele,De Logu, Alessandro,Radi, Marco,Bechi, Beatrice,Manetti, Fabrizio,Magnani, Matteo,Supino, Sibilla,Meleddu, Rita,Chisu, Lorenza,Botta, Maurizio
, p. 8587 - 8591 (2008/12/23)
As a continuation of our previous work that turned toward the identification of antimycobacterial compounds with innovative structures, two series of pyrazole derivatives were synthesized by parallel solution-phase synthesis and were assayed as inhibitors of Mycobacterium tuberculosis (MTB), which is the causative agent of tuberculosis. One of these compounds showed high activity against MTB (MIC = 4 μg/mL). The newly synthesized pyrazoles were also computationally investigated to analyze their fit properties to the pharmacophoric model for antitubercular compounds previously built by us and to refine structure-activity relationship analysis.