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(E)-2-(benzo[d]thiazol-2-yl)-3-heteroarylacrylonitriles are described as a new class of selective inhibitors of acetylcholinesterase (AChE). The most potent compound in the series exhibited good AChE inhibitory activity (IC₅₀ = 64 µM). Compound 7f was found to be more selective than galanthamine in inhibiting AChE and it showed a moderate selectivity index.(More)
The solvent-free reaction between 5-amino-1H-pyrazoles and-triketones (2-acetyldimedone and 2-acetylindandione) leads to the formation of new fused pyrazolo[1,5-a]pyrimidines in good yields. A possible mechanistic route is postulated on the basis of the isolation of the cyclization intermediate. The structures and regiospecificity of the reaction were(More)
The commercially available Amberlyst ®-15 in the presence of AcOH was conveniently used to catalyze the in-tramolecular cyclization of a series of 2´-amino[1,3]dioxolochalcones to the corresponding dihydroquinolin-8-ones. This procedure is compatible with different functional groups and may be used as an alternative strategy for the synthesis of this(More)
New hetaryl- and alkylidenerhodanine derivatives 3a-d, 3e, and 4a-d were prepared from heterocyclic aldehydes 1a-d or acetaldehyde 1e. The treatment of several rhodanine derivatives 3a-d and 3e with piperidine or morpholine in THF under reflux, afforded (Z)-5-(hetarylmethylidene)-2-(piperidin-1-yl)thiazol-4(5H)-ones and 2-morpholinothiazol-4(5H)-ones 5a-d,(More)
A new series of NH-pyrazoline derivatives 6 was synthesized by cyclocondensation reaction of novel [(7-chloroquinolin-4-yl)oxy]chalcones 5 with hydrazine hydrate. The treatment of pyrazolines 6 with acetic anhydride or formic acid yielded the N-acetyl- or N-formylpyrazoline derivatives 7-8, respectively. These novel 2-pyrazoline derivatives 6-8 were(More)
The title compound, C(14)H(11)NS, crystallizes with Z' = 0.75 in the space group C2/m. Two independent molecules are present, one of which lies with all the non-H atoms on a mirror plane, while the other is fourfold disordered across a site of 2/m symmetry. The ordered molecules are stacked such that they enclose continuous channels running along twofold(More)
Twenty-four new hybrid analogues (15-38) containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S. National Cancer Institute (NCI). Compounds 25, 30, 31, 36, and 37 showed significant cytostatic activity, with the most outstanding(More)
In both 3-tert-butyl-7,7-dimethyl-1-phenyl-5,6,7,8-tetrahydroimidazo[3,4-b]quinolin-5-one, C22H25N3O, (I), and 2,8,8-trimethyl-5-phenyl-6,7,8,9-tetrahydroimidazo[2,3-a]quinolin-6-one, C19H19N3O, (II), the heterobicyclic portions of the molecules are planar, with naphthalene-type delocalization in (II), while the carbocyclic ring in each compound adopts an(More)