5445-15-8Relevant academic research and scientific papers
Thiosemicarbazones as Aedes aegypti larvicidal
Da Silva, Jo?o Bosco P.,Navarro, Daniela Maria Do A.F.,Da Silva, Aluizio G.,Santos, Geanne K.N.,Dutra, Kamilla A.,Moreira, Diogo Rodrigo,Ramos, Mozart N.,Espíndola, José Wanderlan P.,De Oliveira, Ana Daura T.,Brondani, Dalci José,Leite, Ana Cristina L.,Hernandes, Marcelo Zaldini,Pereira, Valéria R.A.,Da Rocha, Lucas F.,De Castro, Maria Carolina A.B.,De Oliveira, Beatriz C.,Lan, Que,Merz, Kenneth M.
, p. 162 - 175 (2015)
Abstract A set of aryl- and phenoxymethyl-(thio)semicarbazones were synthetized, characterized and biologically evaluated against the larvae of Aedes aegypti (A. egypti), the vector responsible for diseases like Dengue and Yellow Fever. (Q)SAR studies were useful for predicting the activities of the compounds not included to create the QSAR model as well as to predict the features of a new compound with improved activity. Docking studies corroborated experimental evidence of AeSCP-2 as a potential target able to explain the larvicidal properties of its compounds. The trend observed between the in silico Docking scores and the in vitro pLC50 (equals -log LC50, at molar concentration) data indicated that the highest larvicidal compounds, or the compounds with the highest values for pLC50, are usually those with the higher docking scores (i.e., greater in silico affinity for the AeSCP-2 target). Determination of cytotoxicity for these compounds in mammal cells demonstrated that the top larvicide compounds are non-toxic.
Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
Rahim, Fazal,Javed, Muhammad Tariq,Ullah, Hayat,Wadood, Abdul,Taha, Muhammad,Ashraf, Muhammad,Qurat-Ul-Ain,Khan, Muhammad Anas,Khan, Fahad,Mirza, Salma,Khan, Khalid M.
, p. 106 - 116 (2015/09/02)
A series of thirty (30) thiazole analogs were prepared, characterized by 1H NMR, 13C NMR and EI-MS and evaluated for Acetylcholinesterase and butyrylcholinesterase inhibitory potential. All analogs exhibited varied butyrylcholinester
Efficient synthesis of new tetradentate ligands with potential applications for 64Cu PET-imaging
Bodio, Ewen,Julienne, Karine,Gouin, Sébastien G.,Faivre-Chauvet, Alain,Deniaud, David
experimental part, p. 924 - 927 (2011/03/20)
We wish to report the synthesis of new tetradentate ligands in less than 3 h in good to excellent yields from a commercially available compound using microwave-assisted technology. First tests of complexation showed a high ability of these ligands to chel
