220271-07-8Relevant academic research and scientific papers
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity
Dos Santos Fernandes, Guilherme Felipe,De Souza, Paula Carolina,Moreno-Viguri, Elsa,Santiva?ez-Veliz, Mery,Paucar, Rocio,Pérez-Silanes, Silvia,Chegaev, Konstantin,Guglielmo, Stefano,Lazzarato, Loretta,Fruttero, Roberta,Man Chin, Chung,Da Silva, Patricia Bento,Chorilli, Marlus,Solcia, Mariana Cristina,Ribeiro, Camila Maríngolo,Silva, Caio Sander Paiva,Marino, Leonardo Biancolino,Bosquesi, Priscila Longhin,Hunt, Debbie M.,De Carvalho, Luiz Pedro S.,De Souza Costa, Carlos Alberto,Cho, Sang Hyun,Wang, Yuehong,Franzblau, Scott Gary,Pavan, Fernando Rogério,Dos Santos, Jean Leandro
, p. 8647 - 8660 (2017/11/03)
Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is the infectious disease responsible for the highest number of deaths worldwide. Herein, 22 new N-oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antitubercular potential against Mtb. Compound 8 was found to be the most promising compound, with MIC90 values of 1.10 and 6.62 μM against active and nonreplicating Mtb, respectively. Additionally, we carried out in vivo experiments to confirm the safety and efficacy of compound 8; the compound was found to be orally bioavailable and highly effective, leading to a reduction of Mtb to undetectable levels in a mouse model of infection. Microarray-based initial studies on the mechanism of action suggest that compound 8 blocks translation. Altogether, these results indicate that benzofuroxan derivative 8 is a promising lead compound for the development of a novel chemical class of antitubercular drugs.
New 1,4-dihydropyridines conjugated to furoxanyl moieties, endowed with both nitric oxide-like and calcium channel antagonist vasodilator activities
Di Stilo, Antonella,Visentin, Sonja,Cena, Clara,Gasco, Andréa Marcello,Ermondi, Giuseppe,Gasco, Alberto
, p. 5393 - 5401 (2007/10/03)
A series of 4-phenyl-1,4-dihydropyridines substituted at the ortho and meta positions of the phenyl ring with NO-donating furoxan moieties and their non-NO-releasing furazan analogues were synthesized and pharmacologically characterized. The vasodilator a
