- Synthesis of novel azabicyclo derivatives containing a thiazole moiety and their biological activity against pine-wood nematodes
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To explore a new skeleton with nematicidal activity, a series of novel azabicyclo derivatives containing a thiazole moiety were designed, synthesized and evaluated for their nematicidal activities. The bioassay results against pine-wood nematodes (Bursaphelenchus xylophilus) showed that most of the title compounds displayed nematicidal activity at a concentration of 40 mg/L. Especially, the title compounds2-((8-methyl-8-azabicyclo[3.2.1]octan-3-yl)oxy)-4-(4-chlorophenyl)thiazole (7e), 2-((8-methyl-8-azabicyclo[3.2.1]octan-3-yl)thio)-4-phenylthiazole (10a) and 2-((8-methyl-8-azabicyclo [3.2.1]octan-3-yl)thio)-4-(4-chlorophenyl)thiazole (10e) exhibited more than 90% mortality against Bursaphelenchus xylophilus.
- Li, Hui,Lu, Aoyun,Zhang, Yanqiu,Peng, Yanqing,Song, Gonghua
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p. 371 - 375
(2020/01/02)
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- Synthesis of 4- and 5-arylthiazolinethiones as inhibitors of indoleamine 2,3-dioxygenase
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Docking studies of 4-phenylthiazolinethione on human IDO1 suggest complexation of the heme iron by the exocyclic sulfur atom further reinforced by hydrophobic interactions of the phenyl ring within pocket A of the enzyme. On this basis, chemical modifications were proposed to increase inhibition activity. Synthetic routes had to be adapted and optimized to yield the desired substituted 4- and 5-arylthiazolinethiones. Their biological evaluation shows that 5-aryl regioisomers are systematically less potent than the corresponding 4-aryl analogs. Substitution on the phenyl ring does not significantly increase inhibition potency, except for 4-Br and 4-Cl derivatives.
- Balti, Monaem,Plas, Aurélie,Meinguet, Céline,Haufroid, Marie,Thémans, Quentin,Efrit, Mohamed Lotfi,Wouters, Johan,Lanners, Steve
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supporting information
p. 3607 - 3610
(2017/07/07)
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- An approach to the synthesis of 4-aryl and 5-aryl substituted thiazole-2(3: H)-thiones employing flow processing
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A method for the preparation of 4-aryl and 5-aryl substituted thiazole-2(3H)-thiones is described. Flow processing is employed as a tool, and supported acids and bases used to facilitate both the synthetic strategy and product isolation. The methodology is applicable to a range of substrates.
- Balti, Monaem,Miller, Shelli A.,Efrit, Mohamed Lotfi,Leadbeater, Nicholas E.
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p. 72165 - 72169
(2016/08/09)
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- Synthesis 4-(4'-methylphenyl)-2-mercaptothiazole structure with NMR, vibrational, Mass Spectroscopy and DFT studies
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4-(4'-methylphenyl)-2-mercaptothiazole (MPMT) was synthesized from a compound of thiocarbamate family using condensation reaction. The spectroscopic properties of this structure were studied using 1H-NMR, 13C-NMR, FT-IR, Mass Spectroscopy, and elemental analysis methods. Subsequently, its thermodynamic parameters were examined by performing density functional theory (DFT) calculation at B3LYP, B3PW91, and mPW1PW91 levels of theory and 6-311G (d, p) basis set. After studying the values of total energy, entropy, vibrational frequencies, ZPVE, HOMO and LUMO dependant parameters such as Chemical potential, Chemical hardness, Electrophilicity, and maximum amount of electronic charge transfer were also considered. However, chemical shift value of different nuclei were theoretically determined. The results indicated high conformity between the theoretical and experimental values. Finally, the electrostatic potential values of this structure were studied. The results showed variation in the value of this parameter at different part of the structure.
- Soleymani, Reza,Dijvejin, Reihaneh Dehghanian,Hesar, Asiye Fallahigozal Abad,Sobhanie, Ebtesam
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p. 1291 - 1304
(2013/02/25)
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- Synthesis new and novel aryl thiazole derivatives compounds
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Six new compounds of Thiazoles family was synthesis from condensation reaction of some compounds from pyrazolines. NMR, IR and elemental analysis was used for identification of these compounds. Position of aliphatic and aromatic hydrogens in pyrazolone and thiazole cycles had established proceeding of identification. Most of obtained compounds like aciform crystals, their color is white and yellow. Reaction time and yield of these compounds had shown better results as compared with other thiazole derivations.
- Akbarzadeh, Abolfath,Soleymani, Reza,Taheri, Milad,Ali, Maryam Karimi-Cheshmeh
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experimental part
p. 153 - 164
(2012/09/07)
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- Hypervalent iodine in synthesis. 48. A one-pot convenient procedure for the synthesis of 2-mercaptothiazoles by cyclocondensation of ketones with [hydroxy(tosyloxy)iodo]-benzene and ammonium dithiocarbamate
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α-Tosyloxylation of ketones with [hydroxy(tosyloxy)iodo]-benzene (HTIB), followed by treatment with ammonium dithiocarbamate, provides a one-pot convenient procedure for the synthesis of 2-mercaptothiazoles with good yields.
- Zhang,Chen
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p. 415 - 420
(2007/10/03)
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- Hypervalent iodine in synthesis; 60: A novel method for the synthesis of 2-mercaptothiazoles by cyclocondensation of alkynyl(phenyl)iodonium salts and ammonium dithiocarbamate
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A novel method for the synthesis of 2-mercaptothiazoles is achieved by cyclocondensation of alkynyl(phenyl)iodonium salts with ammonium dithiocarbamate. A reaction mechanism is proposed.
- Zhang,Chen
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p. 358 - 360
(2007/10/03)
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