74693-61-1Relevant academic research and scientific papers
Synthesis, biological assessment and molecular modeling of new dihydroquinoline-3-carboxamides and dihydroquinoline-3-carbohydrazide derivatives as cholinesterase inhibitors, and Ca channel antagonists
Tomassoli, Isabelle,Ismaili, Lhassane,Pudlo, Marc,De Los Ríos, Cristóbal,Soriano, Elena,Colmena, Inés,Gandía, Luis,Rivas, Luis,Samadi, Abdelouahid,Marco-Contelles, José,Refouvelet, Bernard
experimental part, p. 1 - 10 (2011/02/27)
The synthesis, biological evaluation, and molecular modeling of new 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides(4), 4-hydroxy-2-oxo-1,2- dihydroquinoline-3-carbohydrazide (6), and some hexahydropyrimido[5,4-c] quinoline-2,5-diones (9) produced earlier by our laboratory, as AChE/BuChE inhibitors, is described. From these analyses compound 4c resulted equipotent regarding the inhibition of cholinesterases'; inhibitors 6k, 9a, 9b were selective for AChE, whereas product 4d proved selective for BuChE. Docking analysis has been carry out in order to identify the binding mode in the active site, and to explain the observed selectivities. Only compound 9a has been shown to decrease K+-induced calcium signals in bovine chromaffin cells.
4-hydroxy-2-quinolones 165*. 1-R-4-hydroxy-2-oxo-1,2-dihydro- quinoline-3-carbaldehydes and their thiosemicarbazones. Synthesis, structure, and biological properties
Ukrainets,Yangyang, Liu,Tkach,Gorokhova,Turov
scheme or table, p. 705 - 714 (2010/04/02)
Two variants are discussed of the synthesis of 1-R-4-hydroxy-2-oxo-1,2- dihydroquinoline-3-carboxylic acid β-N-tosylhydrazides which undergo a McFayden-Stevens reaction to give 1-R-4-hydroxy-2-oxo-1,2-dihydroquinoline-3- carbaldehydes in high yields. It was shown that the thiosemicarbazones prepared from them exist in the solid state exclusively in the syn-form while in solution a hydrazone ? enhydrazine tautomerism is observed. The results of a study of the antitubercular activity of the synthesized compounds are reported.
4-HYDROXYQUINOLONES-2. 5. SYNTHESIS AND PHYSICOCHEMICAL AND BIOLOGICAL PROPERTIES OF NEW PYRAZOLE DERIVATIVES
Ukrainets, I. V.,Bezuglyi, P. A.,Treskach, V. I.,Kornilov, M. Yu.,Turov, A. V.,et al.
, p. 912 - 916 (2007/10/02)
Hydrazinolysis of 1-R-3-carbethoxy-4-hydroxyquinolones-2 was used to synthesize the corresponding hydrazides; thermal cyclodehydration of the latter yielded 3-oxopyrazolo--5-R-quinolones-4.Findings relating to their analgesic and antiphlogistic activity are outlined.
