96-50-4Relevant articles and documents
-
Portnov et al.
, (1971)
-
Synthesis of 6-membered-ring fused thiazine-dicarboxylates and thiazole-pyrimidines via one-pot three-component reactions
Bode, Moira L.,Coyanis, Elena Mabel,Fernandes, Manuel A.,Fish, Muhammad Q.,Mohlala, Reagan L.
, (2021/09/18)
A facile and efficient one-pot three-component reaction method for the synthesis of thiazine-dicarboxylates is reported. Reaction of an isocyanide and dialkyl acetylenedicarboxylate with 2-amino-4H-1,3-thiazin-4-one derivatives containing both an acidic proton and an internal nucleophile gave the products in good yields of 76–85%. The reactivity of dialkyl acetylenedicarboxylates was further tested in the synthesis of thiazole-pyrimidines where a two-component reaction of 2-aminothiazole with dialkyl acetylenedicarboxylates was successfully converted to a more efficient three-component reaction of a thiourea, α-haloketone and dialkyl acetylenedicarboxylate (DMAD/DEtAD) to give thiazole-pyrimidines in good yields of 70–91%.
Hg2+ induced hydrolysis of thiazole amine based Schiff base: Colorimetric and fluorogenic chemodosimeter for Hg2+ ions in an aqueous medium
Tekuri, Venkatadri,Sahoo, Suban K.,Trivedi, Darshak R.
, p. 19 - 26 (2019/04/05)
Simple pyrene-based chemosensors 1 to 3, were synthesized from pyrene-1-carboxaldehyde and they were characterized using various spectroscopic techniques like UV–Vis, FT-IR, Mass, 1H NMR and 13C NMR. Among synthesized receptors, the receptor 1 shows high selectivity towards Hg2+ ions. Further, the high selectivity of receptor 1 towards Hg2+ ions in the presence of various other interfering metal ions like Ni2+, Zn2+, Mn2+, Co2+, Cu2+, Cr3+, Fe3+, Al3+, Ag+, Fe2+, Cd2+, Mg2+, Pb2+, Ca2+, Na+, K+ was confirmed by UV–Vis and fluorescence methods. The detection limit for Hg2+ ions was found to be 0.270 μM. The chemodosimetric irreversible hydrolysis of the receptor 1 in the presence of Hg2+ was studied by UV/Vis, fluorescence, FT-IR, LC-MS, 1H NMR and theoretical DFT study. Further, the real life applications of receptor 1 for the determination of Hg2+ ions were demonstrated by UV–Vis method.
Imidazole-thiazole coupled derivatives as novel lanosterol 14-α demethylase inhibitors: ionic liquid mediated synthesis, biological evaluation and molecular docking study
Nikalje, Anna Pratima G.,Tiwari, Shailee V.,Sarkate, Aniket P.,Karnik, Kshipra S.
, p. 592 - 606 (2017/11/06)
A novel series of imidazole-thiazole coupled derivatives (7a–7q) were synthesized using Green protocol and identified by different spectroscopic techniques. The synthesized derivatives (7a–7q) were evaluated for their in vitro antifungal activity against the six fungi strains. The compounds 7j and 7k exhibited the most promising antifungal activity. The compound 7k exhibited extremely high antifungal activity against C. albicans, C. glabrata, F. oxysporum, A. flavus, A. niger, and C. neoformans with MIC80 values of 0.2, 0.2, 20, 35, 40, and 5 μg/ml respectively. The mode of action of the most promising antifungal compounds 7j and 7k was established by ergosterol extraction and quantitation assay. From the ergosterol extraction and quantitation assay it was found that the compounds 7j and 7k act by inhibition of ergosterol biosynthesis in C. albicans. The molecular docking study revealed the high spontaneous binding ability of the tested compounds to the active site of lanosterol 14α-demethylase, which proves that the tested compounds inhibit the synthesis of lanosterol 14α-demethylase. The synthesized compounds were analyzed for ADMET properties to establish oral drug like behavior and shows satisfactory results. To establish the antifungal selectivity and safety, the most active compounds were further tested for cytotoxicity against human cancer cell lines HeLa and K-562 and were found to be non-cytotoxic in nature. The in vivo acute oral toxicity study was performed for the most active compounds and results indicate that the compounds are non-toxic in nature.
