- Synthesis of new thioureas derivatives and evaluation of their efficacy as proliferation inhibitors in mcf-7 breast cancer cells by using99m tc-mibi radiotracer
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Background & Objective: Anti-tumor activity of some thioureas derivatives is well documented in literature and received considerable attention. The present study aims to synthesize and characterize some novel thioureas and carbonylthioureas as anti-tumor
- Hormati, Ahmad,Shiran, Jafar Abbasi,Molazadeh, Mikaeil,Kaboudin, Babak,Ahmadpour, Sajjad
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p. 766 - 778
(2021/04/02)
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- Synthesis, characterization, and antibacterial activity of some thiazoles derived from allyl thioureas
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Synthesis of thiazoles was carried out from allyl thioureas using different cyclizing agents such as hydrogen chloride gas and bromine. Synthesized compounds were characterized by IR, 1H and 13C NMR, mass spectrometry, and elemental analysis. The synthesized thiazoles were evaluated for their antibacterial activity against Gram postitive (Lactobacillus bulgaris and Streptococcus mitis) and Gram negative (Yersinia) as well as antifungal activity against Aspergillus niger fungi.
- Khare,Sharma,Sharma
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p. 702 - 707
(2016/06/01)
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- Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors
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A series of 31 N,N-disubstituted 2-amino-5-halomethyl-2-thiazolines was designed, synthesized, and evaluated for inhibitory potential against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and carboxylesterase (CaE). The compounds did not inhibit AChE; the most active compounds inhibited BChE and CaE with IC50 values of 0.22-2.3 μM. Pyridine-containing compounds were more selective toward BChE; compounds with the para-OMe substituent in one of the two dibenzyl fragments were more selective toward CaE. Iodinated derivatives were more effective BChE inhibitors than brominated ones, while there was no influence of halogen type on CaE inhibition. Inhibition kinetics for the 9 most active compounds indicated non-competitive inhibition of CaE and varied mechanisms (competitive, non-competitive, or mixed-type) for inhibition of BChE. Docking simulations predicted key binding interactions of compounds with BChE and CaE and revealed that the best docked positions in BChE were at the bottom of the gorge in close proximity to the catalytic residues in the active site. In contrast, the best binding positions for CaE were clustered rather far from the active site at the top of the gorge. Thus, the docking results provided insight into differences in kinetic mechanisms and inhibitor activities of the tested compounds. A cytotoxicity test using the MTT assay showed that within solubility limits (30 μM), none of the tested compounds significantly affected viability of human fetal mesenchymal stem cells. The results indicate that a new series of N,N-disubstituted 2-aminothiazolines could serve as BChE and CaE inhibitors for potential medicinal applications.
- Makhaeva, Galina F.,Boltneva, Natalia P.,Lushchekina, Sofya V.,Serebryakova, Olga G.,Stupina, Tatyana S.,Terentiev, Alexey A.,Serkov, Igor V.,Proshin, Alexey N.,Bachurin, Sergey O.,Richardson, Rudy J.
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p. 1050 - 1062
(2016/02/19)
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- Synthesis and biological evaluation of arylthiourea derivatives with antitubercular activity
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Tuberculosis (TB) is a contagious disease caused by Mycobacterium tuberculosis (M. tuberculosis), and remains one of the most life-threatening plagues for public health in the world. The emergence of drug resistant strains of TB and co-infection with HIV has further complicated TB treatment. Here, the synthesis and characterizaton of a series of compounds were described, and these were followed by evaluating for their antibacterial activity against M. tuberculosis. Several novel arylthiourea derivatives exhibited excellent activity (lowest MIC=0.09 μg/ml) against M. tuberculosis including drug resistant strains of M. tuberculosis. The results suggest that these compounds are promising candidates for new anti-TB agent development.
- Luo, Rusong,Laitinen, Tuomo,Teng, Liyan,Nevalainen, Tapio,Lahtela-Kakkonen, Maija,Zheng, Baofu,Wang, Honghai,Poso, Antti,Zhang, Xuelian
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p. 640 - 650
(2013/08/23)
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- Heterocyclization of N-hetaryl-N′-(prop-2-en-1-yl)thioureas by the action of sulfuryl chloride
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Cyclization of N-hetaryl-N′-(prop-2-en-1-yl)thioureas by the action of sulfuryl chloride leads to the formation of the corresponding 2-hetarylimino-5-chloromethylthiazolidine hydrochlorides which are converted into the free bases by treatment with aqueous
- Zborovskii,Orysyk,Staninets,Rusanov,Chernega
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p. 1030 - 1034
(2008/03/13)
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- Influence of Substituents on the Synthesis of Thiazolidinones
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The influence of substituents (subunits) in the synthesis of thiazolidinones by the reaction of unsymmetrical thioureas with monochloroacetic acid in ethanol has been rationalised by the characterisation of the hydrolysis products of the resulting thiazolidinones.The formation of thiol from thiourea, which is the key intermediate in thiazolidinone synthesis, invariably involves the -NH- group adjacent to more electron withdrawing subunits.
- Sabu, M.,Garnaik, B. K.,Behera, Rajani K.
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p. 779 - 781
(2007/10/02)
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