7441-53-4Relevant academic research and scientific papers
Hydroxy phenyl hydrazides and their role as corrosion impeding agent: A detail experimental and theoretical study
Singh, Ashish Kumar,Chugh, Bhawna,Singh, Manjeet,Thakur, Sanjeeve,Pani, Balaram,Guo, Lei,Kaya, Savas,Serdaroglu, Goncagul
, (2021/02/27)
This study presents synthesis of environmentally benign corrosion inhibitors, hydroxy acetophenone derivative namely, N′-(1-(2-hydroxyphenyl) ethylidene) acetohydrazide (ATOH), N′-(1-(2-hydroxyphenyl) ethylidene) benzohydrazide (BZOH), 2-(1-(2-hydroxyphen
In vitro evaluation of new 4-thiazolidinones on invasion and growth of Toxoplasma gondii
Molina, Diego A.,Ramos, Gerardo A.,Zamora-Vélez, Alejandro,Gallego-López, Gina M.,Rocha-Roa, Cristian,Gómez-Marin, Jorge Enrique,Cortes, Edwar
, p. 129 - 139 (2021/06/15)
Treatments for toxoplasmosis such as pyrimethamine have shown numerous side effects. It has been reported that the likelihood of relapse associated with pyrimethamine-based therapy in patients with HIV and toxoplasmic encephalitis (TE) can have significant implications, even for patients who often develop new lesions in areas of the brain previously free of infection. This led us to research for new agents against Toxoplasma gondii. Recent findings have shown the potent biological activity of 4-thiazolidinones. We proposed to design and synthesize a new series of 2-hydrazono-4-thiazolidinones derivatives to evaluate the in vitro growth inhibition effect on T. gondii. The growth rates of T. gondii tachyzoites in Human Foreskin Fibroblast (HFF) cell culture were identified by two in vitro methodologies. The first one was by fluorescence in which green fluorescent RH parasites and cherry-red fluorescent ME49 parasites were used. The second one was a colorimetric methodology using β-Gal parasites of the RH strain constitutively expressing the enzyme beta-galactosidase. The 4-thiazolidinone derivatives 1B, 2B and 3B showed growth inhibition at the same level of Pyrimethamine. These compounds showed IC50 values of 1B (0.468–0.952 μM), 2B (0.204–0.349 μM) and 3B (0.661–1.015 μM) against T. gondii. As a measure of cytotoxicity the compounds showed a TD50 values of: 1B (60 μM), 2B (206 μM) and 3B (125 μM). The in vitro assays and molecular modeling results suggest that these compounds could act as possible inhibitors of the Calcium-Dependent Protein Kinase 1 of T. gondii. Further, our results support the fact that of combining appropriate detection technologies, combinatorial chemistry and computational biology is a good strategy for efficient drug discovery. These compounds merit in vivo analysis for anti-parasitic drug detection.
Design, synthesis, bioactivity, and DFT calculation of 2-thiazolyl-hydrazone derivatives as influenza neuraminidase inhibitors
Cui, Man-Ying,Nie, Jian-Xia,Yan, Zhong-Zhong,Xiao, Meng-Wu,Lin, Ding,Ye, Jiao,Hu, Ai-Xi
, p. 938 - 947 (2019/05/15)
Three series of thiazolylhydrazone derivatives were designed, synthesized, and evaluated for their neuraminidase (NA) inhibitory activity against influenza virus H1N1 in vitro. Compounds 1 and 2 were synthesized via the one-pot reaction and compound 3 was
Novel thiazole clubbed triazole derivatives as antimicrobial, antimalarial, and cytotoxic agents
Bansal, Kushal K.,Sharma, Diksha,Sharma, Archana,Rajak, Harish,Sharma, Prabodh C.
, p. 305 - 312 (2018/09/14)
Thiazole is one of the most potential heterocyclic moieties in bioorganic chemistry and is major tool in drug design and discovery. The present work describes the synthesis of a series of N-{(1-(4-(4bromophenyl) thiazol-2-yl)-3-substitutedphenyl-1H-pyrazo
(4-alkyl-5-acyl-2-thiazole) hydrazone derivatives and medical application thereof
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Paragraph 0035-0036; 0037; 0040-0041, (2018/09/28)
The invention relates to (4-alkyl-5-acyl-2-thiazole) hydrazone derivatives shown as a formula I and pharmaceutically acceptable salts thereof, a medicinal composition and the application thereof to preparation of an influenza virus neuraminidase inhibitor
Synthesis, structural characterization and electrochemical studies of nickel(II), copper(II) and cobalt(III) complexes of some ONS donor ligands derived from thiosemicarbazide and S-alkyl/aryl dithiocarbazates
Ali, Mohammad Akbar,Tan, Ai Ling,Mirza, Aminul Huq,Santos, Jose H.,Abdullah, Aimi Hanisah Bte Hj
, p. 651 - 659 (2013/01/15)
Four tridentate ONS ligands, namely 2-hydroxyacetophenonethiosemicarbazone (H2L1), the 2-hydroxyacetophenone Schiff base of S-methyldithiocarbazate (H2L2), the 2-hydroxy-5-nitrobenzaldehyde Schiff base of S-methyldithiocarbazate (H2L3), and the 2-hydroxy-5- nitrobenzaldehyde Schiff base of S-benzyldithiocarbazate (H2L4), and their complexes of general formula [Ni(HL1)], [ML] (M = NiII or CuII; L = L1, L2, L3 and L4), [Co(HL)(L); L = L1, L2, L3 and L4] and [ML(B)] (M = NiII or CuII; L = L2 and L 4; B = py, PPh3) have been prepared and characterized by physico-chemical techniques. Spectroscopic evidence indicates that the Schiff bases behave as ONS tridentate chelating agents. X-ray crystallographic structure determination of [NiL2(PPh3)] and [CuL 4(py)] indicates that these complexes have an approximately square-planar structure with the Schiff bases acting as dinegatively charged ONS tridentate ligands coordinating via the phenoxide oxygen, azomethine nitrogen and thiolate sulfur atoms. The electrochemical properties of the complexes have been studied by cyclic voltammetry. Springer Science+Business Media B.V. 2012.
Mixed-ligand thiosemicarbazone complexes of nickel: Synthesis, structure and catalytic activity
Datta, Sayanti,Seth, Dipravath Kumar,Butcher, Ray J.,Bhattacharya, Samaresh
experimental part, p. 120 - 128 (2011/12/16)
Reaction of thiosemicarbazones of salicylaldehyde, 2-hydroxyacetophenone and 2-hydroxynaphthaldehyde with Ni(ClO4)2·6H 2O, using 2,2′-bipyridine as coligand, afforded three dinuclear complexes (1a, 1b and 1c). Similar reac
M-STAGE KINESIN INHIBITOR
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Page/Page column 74, (2010/11/08)
A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, -C(=W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents -C(=Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
THIADIAZOLINE DERIVATIVE
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Page 49, (2010/02/08)
(wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents -C(-W)R6 or the like; R3 represents a hydrogen atom, -C(=WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
