2104-05-4Relevant academic research and scientific papers
Synthesis of novel azabicyclo derivatives containing a thiazole moiety and their biological activity against pine-wood nematodes
Li, Hui,Lu, Aoyun,Zhang, Yanqiu,Peng, Yanqing,Song, Gonghua
, p. 371 - 375 (2020/01/02)
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.
Synthesis of 4- and 5-arylthiazolinethiones as inhibitors of indoleamine 2,3-dioxygenase
Balti, Monaem,Plas, Aurélie,Meinguet, Céline,Haufroid, Marie,Thémans, Quentin,Efrit, Mohamed Lotfi,Wouters, Johan,Lanners, Steve
supporting information, p. 3607 - 3610 (2017/07/07)
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.
2-[3H-THIAZOL-2-YLIDINEMETHYL]PYRIDINES AND RELATED COMPOUNDS AND THEIR USE
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Page/Page column 42, (2009/10/06)
The present invention pertains to certain 2-[3H-thiazol-2-ylidinemethyl]pyridine compounds and analogs thereof, which, inter alia, inhibit cell proliferation, treat cancer, etc., and more specifically to compounds of the following formula, wherein RA1, RA2, RA3, RA4, RB1, RB2, RNA, RNB, and X? are as defined herein: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative conditions such as cancer, etc.
A facile synthesis of thiazole-2(3H)-thiones through [hydroxy(tosyloxy) iodo]benzene
Aggarwal, Ranjana,Pundeer, Rashmi,Kumar, Vinod,Chaudhri, Vishwas,Singh, Shiv P.,Prakash, Om
, p. 2659 - 2664 (2007/10/03)
A one-pot facile synthesis of thiazole-2(3H)-thiones (4) has been achieved by hypervalent iodine oxidation of ketones (1) using [hydroxy (tosyloxy)iodo]benzene, followed by the treatment of the reaction mixture with dithiocarbamate salts (3) The intermediate α-tosyloxy-ketones (2) have also been isolated and converted to the target compounds.
AN UNUSUAL OBSERVATION IN THE SYNTHESIS OF THIOZOLES
Ahluwalia, V. K.,Arora, K. K.,Kaur, Gurvinder,Mehta, Bhupinder
, p. 333 - 340 (2007/10/02)
Dibromoacetyl benzene derivatives on condensation with thiourea give 2-amino-4-arylthiazoles instead of the expected 2-amino-4-aryl-5-bromothiazoles.Attempts have been made to find the reaction pathway.
