1131-17-5Relevant articles and documents
Design, synthesis and anticandidal evaluation of indazole and pyrazole derivatives
Rodríguez-Villar, Karen,Hernández-Campos, Alicia,Yépez-Mulia, Lilián,Sainz-Espu?es, Teresita Del Rosario,Soria-Arteche, Olivia,Palacios-Espinosa, Juan Francisco,Cortés-Benítez, Francisco,Leyte-Lugo, Martha,Varela-Petrissans, Bárbara,Quintana-Salazar, Edgar A.,Pérez-Villanueva, Jaime
, p. 1 - 19 (2021/03/16)
Candidiasis, caused by yeasts of the genus Candida, is the second cause of superficial and mucosal infections and the fourth cause of bloodstream infections. Although some antifungal drugs to treat candidiasis are available, resistant strains to current therapies are emerging. Therefore, the search for new candicidal compounds is certainly a priority. In this regard, a series of indazole and pyrazole derivatives were designed in this work, employing bioisosteric replacement, homologa-tion, and molecular simplification as new anticandidal agents. Compounds were synthesized and evaluated against C. albicans, C. glabrata, and C. tropicalis strains. The series of 3-phenyl-1H-indazole moiety (10a–i) demonstrated to have the best broad anticandidal activity. Particularly, compound 10g, with N,N-diethylcarboxamide substituent, was the most active against C. albicans and both miconazole susceptible and resistant C. glabrata species. Therefore, the 3-phenyl-1H-indazole scaf-fold represents an opportunity for the development of new anticandidal agents with a new chemo-type.
Preparation method of 5-piperazinyl-3-methyl-1-phenylpyrazole
-
Paragraph 0033; 0034; 0035; 0036, (2018/06/15)
The invention discloses a preparation method of a Teneligliptin key intermediate 5-piperazinyl-3-methyl-1-phenylpyrazole, and belongs to the technical field of pharmaceutical manufacturing. Accordingto the preparation method disclosed by the invention, 3-
PYRAZOLE DERIVATIVES AND THEIR USES THEREOF
-
Page/Page column 15; 16, (2014/09/29)
The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein U, R1, R2, R3 and Q are as defined herein. The disclosure also provides a method for treating or preventing a method for the prevention, treatment and/or alleviation of one or more autoimmune or alloimmune disease, pharmaceutical compositions and combination comprising a therapeutically effective amount of a compound, as defined herein.