As the number of individuals affected with Alzheimer's disease (AD) increases and the availability of drugs for AD treatment remains limited, the need to develop effective therapeutics for AD becomes more and more pressing. Strategies currently pursued include inhibiting acetylcholinesterase (AChE) and targeting amyloid-β (Aβ) peptides and metal-Aβ complexes. This work presents the design, synt...

Chalcones considered as the precursor of flavonoids and isoflavonoids abundantly found in plants, and have also been shown to display a diverse array of pharmacological activities. This review is complementary to earlier reviews and covers more recent report of antimicrobial activity of chalcones as well as its important role as an intermediate for the synthesis of different synthetic molecules...

A series of 25 new chalcones were synthesized by Claisen-Schmidt condensation, well characterized by spectroscopic data, and evaluated for their antibacterial and antifungal activities by serial tube dilution method. Among the compounds tested, A3 and A6 containing 2,4-dichlorophenyl and 2,4-difluorophenyl moiety, respectively, were found to be the most potent in the series against both bacteri...

Chalcones (6a-f) have been prepared by the condensation of ketone (5) and different aromatic aldehydes. These chalcones (6a-f) on treatment with guanidine hydrochloride and phenyl hydrazine hydrochloride in presence of alkali give aminopyrimidines (7a-f) and phenylpyrazolines (8a-f) respectively. All the newly synthesised compounds have been characterised on the basis of IR, H NMR spectral data...

Studies have shown that natural and synthetic chalcones (1,3-diphenyl-2-propen-1-ones) possess monoamine oxidase (MAO) inhibition activities. Of particular importance to the present study is a report that a series of furanochalcones acts as MAO-B selective inhibitors. Since the effect of heterocyclic substitution, other than furan (and more recently thiophene, piperidine and quinoline) on the M...

BACKGROUND In metabolite profiling screens or analyses, where generic separation and analysis conditions are used in efforts to measure as many metabolites as possible, overlapping signals from very similar molecules often make it very difficult if not impossible to separate and identify specific molecules of specific classes. The aim of this study was to evaluate the utility of coupling ion mo...

The reaction of various 4'-hydroxychalcones (1a-e) with paraformaldehyde and dibenzylamine led to the formation of a novel series of 4'-hydroxy-3'-dibenzylaminomethyl chalcones (7a-e) instead of 4'-hydroxy-3',5'-bis-(dibenzylaminomethyl)chalcones 4. In order to rationalise the formation of monoadduct 7, energy minimized model structures of 4a and 7a were compared. The in vitro cytotoxic activit...

Nitric oxide (NO) plays an important role in many inflammatory responses and is also involved in carcinogenesis. In the present study, we investigated the inhibitory effect of extracts from Humulus lupulus L. on both the production of NO and the expression of inducible NO synthase (iNOS) in mouse macrophage RAW 264.7 cells. The production of NO was induced by a combination of lipopolysaccharide...

Background The Brazilian National Cancer Institute (INCA) estimated last year almost forty thousand new cancer cases of laryngeal carcinoma, melanoma, tracheal, bronchial and lung cancer. It is known that multidrug resistance and unspecific toxicity are the major challenges for commercial anticancer drugs [1]. In this regard, natural compounds and derivatives are considered as a source of novel...

A series of 1-phenyl-3-aryl-5-(4-(3-propanoloxy) phenyl)-1H-pyrazoles were synthesized from chalcones and studied for their in vitro antibacterial activity. Chalcones i.e.,1-aryl-3-(4hydroxyphenyl) prop-2-en-1-ones (1) on reaction with phenyl hydrazine in presence of acetic acid and few drops of HCl yielded the corresponding 1-phenyl-3-aryl-5-(4-hydroxyphenyl)-1H-pyrazoles (2) which on further ...