New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compar...

A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman's method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showe...

In the crystal structure of the title compound, C(28)H(37)N(4)O(2)S(+)·Cl(-) [systematic name: 4-(1,2-benzothia-zol-3-yl)-1-({2-[(3,5-dioxo-4-aza-tricyclo-[5.2.1.0(2,6)]decan-4-yl)meth-yl]cyclo-hex-yl}meth-yl)piperazin-1-ium chloride], the anions and cations are linked by N-H⋯Cl hydrogen bonds. The crystal structure is further stabilized by C-H⋯π and C-H⋯O inter-actions.

IN THE CRYSTAL STRUCTURE OF THE TITLE COMPOUND [SYSTEMATIC NAME: 1-ethyl-6-fluoro-4-oxo-7-(piperazin-4-ium-1-yl)-1,4-dihydro-quinoline-3-carboxyl-ate sesquihydrate], C(16)H(18)FN(3)O(3)·1.42H(2)O, N-H⋯O and O-H⋯O hydrogen bonds assemble the mol-ecules in a two-dimensional layered corrugated sheet structure parallel to the b axis. The water mol-ecules are disordered [occupancies 0.741 (11) and 0...

Development of chemotherapeutic resistance is a major cause of pharmacologic failure in cancer treatment. One mechanism of resistance in tumor cells is the overexpression of glutathione S-transferases (GSTs) that serve two distinct roles in the development of drug resistance via the formation of glutathione conjugates with drugs for their cellular efflux, and the inhibition of the mitogen-activ...

Purpose: Arylpiperazines have been recognized as the largest and most diverse class of compounds exerting actions on the central nervous system with strong affinity for serotonin and dopamine receptors. We here report the synthesis of some novel arylpiperazines and their evaluation for possible antipsychotic properties. Methods: The target compounds 2-[4-(aryl substituted) piperazin-1-yl]-N-phe...