357639-73-7Relevant academic research and scientific papers
Synthesis and biological evaluation of some novel 1-indanone thiazolylhydrazone derivatives as anti-Trypanosoma cruzi agents
Caputto, Maria E.,Moglioni, Albertina G.,Finkielsztein, Liliana M.,Ciccarelli, Alejandra,Lombardo, Elisa,Frank, Fernanda,Moltrasio, Graciela Y.,Vega, Daniel
, p. 155 - 163,9 (2020/07/31)
A series of novel 4-arylthiazolylhydrazones (TZHs) derived from 1-indanones were synthesized in good yields (66-92%) in a simple procedure using microwave irradiation and then characterized by spectroscopy studies. The compounds were evaluated for their in vitro anti-Trypanosoma cruzi activity against the epimastigote, trypomastigote and amastigote forms of the parasite. Most TZHs displayed excellent activity, and were more potent and selective than the reference drug Benznidazole, used in the current chemotherapy. Analysis of the free sterols from parasite incubated with the compounds showed that inhibition of ergosterol biosynthesis is a possible target for the action of these new TZHs. In particular, TZH 9 emerged as a promising antichagasic compound to be evaluated in animal models.
Efficient one-pot three-component synthesis of N-(4-arylthiazol-2-yl) hydrazones in water under ultrasound irradiation
Zhang, Dong-Nuan,Li, Ji-Tai,Song, Ya-Li,Liu, Hui-Min,Li, Hong-Ya
experimental part, p. 475 - 478 (2012/04/23)
A highly efficient and facile one-pot three-component synthesis of N-(4-arylthiazol-2-yl) hydrazones was carried out in excellent yield without any catalyst in water under ultrasound irradiation.
Selective inhibitory activity against MAO and molecular modeling studies of 2-thiazolylhydrazone derivatives
Chimenti, Franco,Maccioni, Elias,Secci, Daniela,Bolasco, Adriana,Chimenti, Paola,Granese, Arianna,Befani, Olivia,Turini, Paola,Alcaro, Stefano,Ortuso, Francesco,Cardia, Maria C.,Distinto, Simona
, p. 707 - 712 (2007/10/03)
A series of 2-thiazolylhydrazone derivatives have been investigated for the ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO) selectively. All of the compounds showed high activity against both the MAO-A and the MAO-B isoforms with pKi values ranging between 5.92 and 8.14 for the MAO-A and between 4.69 and 9.09 for the MAO-B isoforms. Both the MAO-A and the MAO-B isoforms, deposited in the Protein Data Bank as model 2BXR and 1GOS, respectively, were considered in a computational study performed with docking techniques on the most active and MAO-B-selective inhibitor, 18.
Synthesis and anti-microbial activity of isothiosemicarbazones and cyclic analogues.
Maccioni,Cardia,Bonsignore,Plumitallo,Pellerano,De Logu
, p. 809 - 817 (2007/10/03)
It is known that some derivatives of both thiourea and thiosemicarbazide exhibit potent anti-microbial activity. In order to investigate the effects on the biological properties of structural modifications of such structures, we have synthesised and studi
