1768-59-8Relevant articles and documents
Synthesis, in vitro α-glucosidase inhibitory activity and molecular docking studies of new thiazole derivatives
Khan, Khalid Mohammed,Qurban, Saira,Salar, Uzma,Taha, Muhammad,Hussain, Shafqat,Perveen, Shahnaz,Hameed, Abdul,Ismail, Nor Hadiani,Riaz, Muhammad,Wadood, Abdul
, p. 245 - 258 (2016)
Current study based on the synthesis of new thiazole derivatives via “one pot” multicomponent reaction, evaluation of their in vitro α-glucosidase inhibitory activities, and in silico studies. All synthetic compounds were fully characterized by 1H NMR, 13C NMR and EIMS. CHN analysis was also performed. These newly synthesized compounds showed activities in the range of IC50?=?9.06?±?0.10–82.50?±?1.70?μM as compared to standard acarbose (IC50?=?38.25?±?0.12?μM). It is worth mentioning that most of the compounds such as 1 (IC50?=?23.60?±?0.39?μM), 2 (IC50?=?22.70?±?0.60?μM), 3 (IC50?=?22.40?±?0.32?μM), 4 (IC50?=?26.5?±?0.40?μM), 6 (IC50?=?34.60?±?0.60?μM), 7 (IC50?=?26.20?±?0.43?μM), 8 (IC50?=?14.06?±?0.18?μM), 9 (IC50?=?17.60?±?0.28?μM), 10 (IC50?=?27.16?±?0.41?μM), 11 (IC50?=?19.16?±?0.19?μM), 12 (IC50?=?9.06?±?0.10?μM), 13 (IC50?=?12.80?±?0.21?μM), 14 (IC50?=?11.94?±?0.18?μM), 15 (IC50?=?16.90?±?0.20?μM), 16 (IC50?=?12.60?±?0.14?μM), 17 (IC50?=?16.30?±?0.29?μM), and 18 (IC50?=?32.60?±?0.61?μM) exhibited potent inhibitory potential. Molecular docking study was performed in order to understand the molecular interactions between the molecule and enzyme. Newly identified α-glucosidase inhibitors except few were found to be completely non-toxic.
UV-visible and 1H-15N NMR spectroscopic studies of colorimetric thiosemicarbazide anion sensors
Farrugia, Kristina N.,Makuc, Damjan,Podborska, Agnieszka,Szacilowski, Konrad,Plavec, Janez,Magri, David C.
, p. 1662 - 1672 (2015/03/05)
Four model thiosemicarbazide anion chemosensors containing three N-H bonds, substituted with phenyl and/or 4-nitrophenyl units, were synthesised and studied for their anion binding abilities with hydroxide, fluoride, acetate, dihydrogen phosphate and chlo
Synthesis, phytotoxic, cytotoxic, acetylcholinesterase and butrylcholinesterase activities of N,N-diaryl unsymmetrically substituted thioureas
Begum, Saeedan,Choudhary, M. Iqbal,Khan, Khalid M.
experimental part, p. 1719 - 1730 (2010/05/18)
Fourteen N,N-diaryl unsymmetrically substituted thioureas were synthesised and their cytotoxic (in vitro), phytotoxic (in vitro), acetylcholinesterase and butrylcholinesterase activities were determined. Thiourea 16 exhibited high, and 1 and 3 showed significant phytotoxic activity. Thioureas 1, 3, 4, 6 and 10 showed significant activity and 2, 6 and 7 indicated moderate cytotoxic activities. Compound 12 exhibited butrylcholinesterase activity higher than a standard reference.