88368-72-3Relevant academic research and scientific papers
Design, synthesis, trypanocidal activity, and studies on human albumin interaction of novel s-alkyl-1,2,4-triazoles
Franklim, Tatiany N.,Freire-De-Lima, Leonardo,Chaves, Otávio A.,LaRocque-De-Freitas, Isabel F.,da Silva-Trindade, Joana D.,Netto-Ferreira, José C.,Freire-De-Lima, Célio G.,Decoté-Ricardo, Debora,Previato, José O.,Mendon?a-Previato, Lucia,De Lima, Marco E.F.
, p. 1378 - 1394 (2019/08/26)
Chagas disease is a neglected tropical disease caused by the hemoflagellated parasite Trypanosoma cruzi (Kinetoplastida). The only available drug to treat chagasic patients in Brazil, the nitroheterocycle benznidazole, is effective solely during the acute phase of the infection. There is accordingly a need to develop new therapeutic tools for the treatment of Chagas disease. This work reports the synthesis, trypanocidal evaluation and human serum albumin (HSA) interactions of a novel series of 1,2,4-triazoles. The new derivatives were synthesized via microwave irradiation in good yields. Most compounds showed toxic effects against T. cruzi with low toxicity to host cells. Three S-alkylated-triazoles showed the best activity profile against amastigotes, with half maximal inhibitory concentration (IC50) values of 3.95 ± 1.41, 4.15 ± 0.92 and 3.61 ± 0.65 μmol L-1, respectively. The interaction between HSA and 3-[(1E,3E)-4-(1,3-benzodioxol-5-yl)buta-1,3-dien-1-yl]-5-(butylthio)-4-cyclohexyl-4,5-dihydro-1H-1,2,4-triazole was investigated using multiple spectroscopic techniques and molecular docking, revealing that serum albumin is a potential endogenous carrier to this compound in the human bloodstream.
Substituted imidazo [1,5-a] [1,2,4] triazolo [4,3-d] [1,4] benzodiazepine derivatives
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, (2008/06/13)
The present invention is a compound of formula The compound and derivatives or pharmaceutically acceptable salts thereof of the invention have a good affinity and selectivity to the GABA A α5 receptor and are useful for the treatment of diseases related t
Synthesis and analgesic activity of novel N-acylarylhydrazones and isosters, derived from natural safrole
Lima, Patricia C.,Lima, Lidia M.,Da Silva, Kelli Cristine M.,Leda, Paulo Henrique O.,De Miranda, Ana Luisa P.,Fraga, Carlos A. M.,Barreiro, Eliezer J.
, p. 187 - 203 (2007/10/03)
A new series of antinociceptive compounds belonging to the N- acylarylhydrazone (NAH) class were synthesized from natural safrole (7). The most analgesic derivative represented by 10f, [(4'-N,N- dimethylaminobenzylidene-3-(3',4'-methylenedioxyphenyl)propionylhydrazine], was more potent than dipyrone and indomethacin, used as standards. The NAH compounds described herein were structurally planned by molecular hybridization and classical bioisosterism strategies on previously reported analgesic NAH in order to identify the pharmacophoric contribution of the N- acylarylhydrazone moiety and investigate the structure-activity relationship (SAR) in these series. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
