1446908-08-2Relevant academic research and scientific papers
The hypnotic, anxiolytic, and antinociceptive profile of a novel μ-opioid agonist
Montes, Guilherme Carneiro,Da Silva, Bianca Nascimento Monteiro,Rezende, Bismarck,Sudo, Roberto Takashi,Ferreira, Vitor Francisco,De Carvalho Da Silva, Fernando,Da Cunha Pinto, Angelo,Da Silva, Bárbara Vasconcellos,Zapata-Sudo, Gisele
, (2017/06/08)
5'-4-Alkyl/aryl-1H-1,2,3-triazole derivatives PILAB 1-12 were synthesized and a pharmacological screening of these derivatives was performed to identify a possible effect on the Central Nervous System (CNS) and to explore the associated mechanisms of action. The mice received a peritoneal injection (100 μmol/kg) of each of the 12 PILAB derivatives 10 min prior to the injection of pentobarbital and the mean hypnosis times were recorded. The mean hypnosis time increased for the mice treated with PILAB 8, which was prevented when mice were administered CTOP, a μ-opioid antagonist. Locomotor and motor activities were not affected by PILAB 8. The anxiolytic effect of PILAB 8 was evaluated next in an elevated-plus maze apparatus. PILAB 8 and midazolam increased a percentage of entries and spent time in the open arms of the apparatus compared with the control group. Conversely, a decrease in the percentages of entries and time spent in the closed arms were observed. Pretreatment with naloxone, a non-specific opioid antagonist, prior to administration of PILAB 8 exhibited a reverted anxiolytic effect. PILAB 8 exhibited antinociceptive activity in the hot plate test, and reduced reactivity to formalin in the neurogenic and the inflammatory phases. These data suggest that PILAB 8 can activate μ-opioid receptors to provoke antinociceptive and anti-inflammatory effects in mice.
Ultrasound-assisted synthesis of isatin-type 5′-(4-alkyl/aryl-1H-1,2,3-triazoles) via 1,3-dipolar cycloaddition reactions
Silva, Bianca N. M.,Pinto, Angelo C.,Silva, Fernando C.,Ferreira, Vitor F.,Silva, Bárbara V.
, p. 2378 - 2382 (2016/12/07)
This short report describes the preparation of twelve isatin derivatives, 5′-(4-alkyl/aryl-1H- 1,2,3-triazoles), using 5-azido-spiro[1,3-dioxolane-2,3′-indol]-2′(1′H)-one in the presence of various alkynes under acidic conditions and ultrasound irradiatio
Synthesis of novel isatin-type 5'-(4-Alkyl/Aryl-1H-1,2,3-triazoles) via 1,3-dipolar cycloaddition reactions
Silva, Bianca N. M.,Silva, Ba?rbara V.,Silva, Fernando C.,Gonzaga, Daniel T. G.,Ferreira, Vitor F.,Pinto, Angelo C.
, p. 179 - 183 (2013/05/08)
Isatin and 1H-1,2,3-triazoles are two classes of compounds with great prominence in organic synthesis and medicinal chemistry as they are heterocycle nuclei with a high reactivity allowing to obtain several compounds with important biological properties. Herein, the synthesis of novel 5'-(4-alquil/aril-1H-1,2,3-triazole)-isatin via reaction of 1,3-dipolar cycloaddition catalyzed by acetic acid is reported.
