193747-23-8Relevant academic research and scientific papers
Synthesis and biological evaluation of [α-(1,5-disubstituted 1H-pyrazol-4-yl)benzyl]azoles, analogues of bifonazole
Menozzi, Giulia,Mosti, Luisa,Bruno, Olga,Lo Presti, Eleonora,Musiu, Chiara,Longu, Silvia,La Colla, Paolo,Filippelli, Walter,Falcone, Giuseppe,Piucci, Brunella
, p. 416 - 422 (2007/10/03)
A series of pyrazole analogues of bifonazole, an antifungal drug used in clinical practice, 2a-h and 4a-h were synthesized and tested in vitro against Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus, with no significant results. Imidazoles 2a-h were also tested in vivo for antiarrhythmic and antihypertensive activities; two of these compounds showed moderate activity against ventricular fibrillation caused by aconitine in rats. The above compounds were prepared by reaction of phenyl-[5 substituted 1-phenyl (or 1-methyl)-1H-pyrazol-4-yl]methanols with N,N'-carbonyldiimidazole (2a-h) or of the respective chloro derivatives with 1H-1,2,4-triazole (4a-h).
ω-Dialkylaminoalkyl Ethers of Phenyl-(5-substituted 1-phenyl-1H-pyrazol-4-yl)methanols with Analgesic and Anti-inflammatory Activity
Menozzi, Giulia,Mosti, Luisa,Fossa, Paola,Mattioli, Francesca,Ghia, Marco
, p. 963 - 968 (2007/10/03)
A series of carbinols 3a-f was prepared starting from methanols 1a-f via oxidation with pyridinium chlorochromate to aldehydes 2a-f, followed by a Grignard reaction of the latter. Reaction of 3a-f with ω-chloroalkyldialkylamine hydrochlorides afforded a series of aminoether derivatives 4g-t. Compounds 4i,m-p,s showed a good analgesic activity in the acetic acid writhing test in mice. Moreover, compounds 4h,l,s exhibited a moderate anti-inflammatory activity in the carrageenan-induced edema assay in rats.
