Aim: We report the synthesis and biological evaluation of a small library 15 functionalized 3-styryl-2-pyrazolines pyrazoles, derived from curcuminoids, as trypanosomicidal agents. Methods & results: The compounds were prepared via cyclization reaction between corresponding curcuminoids appropriate hydrazines. All derivatives synthesized investigated for their activities. Compounds 4a 4e sh...

1-Cycloalkyl-2-propene-1-ones were synthesized by electrophilic addition of cycloalkanecarboxylic acid chlorides and its mono- dichloride-substituted derivatives to ethylene in the presence an AlCl3 catalyst at a temperature –10 ÷ –150C dichloroethane medium. The resulting vinyl ketones converted chlorination CCl4 –50C corresponding 1-cycloalkyl-2,3-dichloro-1-propanones, which form 1-R´-3-cycl...

In search of new selective CB2 ligands, the synthesis and preliminary biological evaluation of novel 1,4-dihydroindeno[1,2-c]pyrazole hybrids of the highly potent prototypicals 5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-N-fenchyl-1H-pyrazole-3-carboxamide 1 and 1-(2,4-dichlorophenyl)-6-methyl-N-(piperidin-1-yl)-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide 2 are detailed.We postulated that...

In the pharmaceutical industry, co-crystals are becoming increasingly valuable as crystalline solids that can offer altered/improved physical properties of an active pharmaceutical ingredient (API) without changing its chemical identity or biological activity. In order to identify new solid forms of diclofenac-an analgesic with extremely poor aqueous solubility for which few co-crystal structur...

The diphenyl-pyrazole compound anle138b is a known inhibitor of oligomeric aggregate formation in vitro and in vivo. Therefore, anle138b is considered a promising drug candidate to beneficially interfere with neurodegenerative processes causing devastating pathologies in humans. The atomistic details of the aggregation inhibition mechanism, however, are to date unknown since the ensemble of sma...