58791-84-7Relevant academic research and scientific papers
Synthesis and activity of novel tetrazole compounds and their pyrazole-4-carbonitrile precursors against Leishmania spp
Faria, Jéssica V.,Dos Santos, Maurício S.,Bernardino, Alice M.R.,Becker, Klaus M.,Machado, Gérzia M.C.,Rodrigues, Raquel F.,Canto-Cavalheiro, Marilene M.,Leon, Leonor L.
, p. 6310 - 6312 (2013)
A new series of 5-(1-aryl-3-methyl-1H-pyrazol-4-yl)-1H-tetrazole derivatives (4a-m) and their precursor 1-aryl-3-methyl-1H-pyrazole-4- carbonitriles (3a-m) were synthesized and evaluated as antileishmanials against Leishmania braziliensis and Leishmania amazonensis promastigotes in vitro. In parallel, the cytotoxicity of these compounds was evaluated on the RAW 264.7 cell line. The results showed that among the assayed compounds the substituted 3-chlorophenyl (4a) (IC50/24 h = 15 ± 0.14 μM) and 3,4-dichlorophenyl tetrazoles (4d) (IC50/24 h = 26 ± 0.09 μM) were the most potent against L. braziliensis promastigotes, as compared the reference drug pentamidine, which presented IC50 = 13 ± 0.04 μM. In addition, 4a and 4d derivatives were less cytotoxic than pentamidine. However, these tetrazole derivatives (4) and pyrazole-4- carbonitriles precursors (3) differ against each of the tested species and were more effective against L.braziliensis than on L. amazonensis.
Pyrazolyl-tetrazoles and imidazolyl-pyrazoles as potential anticoagulants and their integrated multiplex analysis virtual screening
Louren?o, André L.P.G.,Vegi, Percilene F.,Faria, Jéssica V.,Pinto, Gustavo S.P.,Dos Santos, Maurício S.,Sathler, Plínio C.,Saito, Max S.,Santana, Marcos,Dutra, Tatiana P.P.,Rodrigues, Carlos R.,Monteiro, Robson Q.,Bernardino, Alice M.R.,Castro, Helena C.
, p. 33 - 47 (2018/12/13)
This article reports a novel virtual screening algorithm seeking the rational identification of novel lead anticoagulants. Seven 5-(3-methyl-1-aryl-1H-pyrazol-4-yl)-1H-tetrazoles and seven novel 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-3-methyl-1H-pyrazole
