In this work, twelve analogues of piperidine alkaloids (-)-cassine and (-)-spectaline were synthesized, as well the racemic forms these natural products. The compounds evaluated for their inhibition electric eel acetylcholinesterase (AChEee) human butyrylcholinesterase (BChEhu) by on-flow mass-spectrometry-based dual-enzyme assay, mechanisms most potent also determined. Our results showed a pre...

Abstract Background The heterocyclic compounds particularly pyridine displayed clinical and biological implementation. Pyridine scaffolds have been detected in most relevant drug molecules that included provided a great possibility for treatment. Main text Pyridine-containing increasing importance medicinal application as antiviral, anticholinesterase activities, antimalarial, antimicrobial, an...

Background: 2, 4-dichlorophenoxyacetic acid, (2, 4-D) is a selective herbicide available as the acids, esters and several salts which vary in their chemical properties, environmental behaviour, and to a lesser extent toxicity. The salt and ester forms are derivatives of the parent acid. It is widely used as a weed killer. The 2, 4-D dimethylamine is one of the salts of this group. Case Presenta...

Three series (series A-C) of coumarin analogues with phenylpiperazine functions as substitution were designed and synthesized for studying their potential for treating Alzheimer's (AD) disease. Their anticholinesterase activities were assayed according to Ellmann's method against freshly prepared acetylcholinesterase (AChE) from Electrophorus electricus using donepezil as the reference compound...

Verbascum species, the largest genus of the family Scrophulariaceae, have been used in traditional medicines for centuries in almost all parts of the world. In this paper, the usage, biological activities (antioxidant, anticholinesterase, antiinflammatory, antinociceptive, wound healing, cytotoxic, anticancer, antitumor, immunomodulatory, antimicrobial, antimalarial, anthelmintic, antiviral, an...

We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase (hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain...

In the current study, a number of alkaloids including retamine, cytisine, and sparteine (quinolizidine-type), yohimbine and vincamine (indole-type), scopolamine and atropine (tropane-type), colchicine (tropolone-type), allantoin (imidazolidine-type), trigonelline (pyridine-type) as well as octopamine, synephrine, and capsaicin (exocyclic amine-type) were tested in vitro for their inhibitory act...

encephalography: Basic Principles, Clinical Applications and Related Fields, 2nd edition. Edited by Niedermeyer E, Lopes da Silva F. Baltimore, Urban and Schwarzenberg, 1987, pp 79–83 8. Bruder N, Velly L, Rey M: A low voltage EEG signal may give low bispectral index values (letter). Anesth Analg 2004; 98:873 9. McGonigal A, Bartolomei F, Régis J, Guye M, Gavaret M, Trébuchon-Da Fonseca A, Dufo...

Anatoxin-a(s) is a guanidinemethyl phosphate ester isolated from the freshwater cyanobacterium (bluegreen algae) Anabaena flos-aquae strain NRC 525–17. Previous work has shown anatoxin-a(s) to be a potent irreversible inhibitor of electric eel acetylcholinesterase (AChE, EC 3.1.1.7). Anatoxin-a(s) has been shown to be an active site-directed inhibitor of AChE, which is resistant to reactivation...