81282-82-8Relevant 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.
KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 0491; 0492, (2016/09/26)
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
Sulfamic acid (H2NSO3H): A low-cost, mild, and efficient catalyst for the synthesis of substituted N-Phenylpyrazoles under solvent-free conditions
Shetty, Mohan R.,Samant, Shriniwas D.
experimental part, p. 1411 - 1418 (2012/04/17)
N-Phenylpyrazoles are synthesized by condensing phenylhydrazine and 1,3-diketones in the presence of a catalytic amount of sulfamic acid, a mild and an efficient solid acid catalyst, under solvent-free conditions. This condensation proceeds smoothly in shorter reaction time. Copyright Taylor & Francis Group, LLC.