Hydrazones and their derivatives are very important compounds in medicinal chemistry due
to their reported biological activity for the treatment of several diseases, like Alzheimer’s, cancer, inflammation,
and leishmaniasis. However, most of the investigations on hydrazones available in literature
today are directed to the synthesis of these molecules with little discussion available on their biological
activities. With the purpose of bringing lights into this issue, we performed a revision of the literature
and wrote this review based on some of the most current research reports of hydrazones and derivatives,
making it clear that the synthesis of these molecules can lead to new drug prototypes. Our
goal is to encourage more studies focused on the synthesis and evaluation of new hydrazones, as a contribution
to the development of potential new drugs for the treatment of various diseases.
3-Arylidenechroman-4-ones
and 2-arylidene-1-tetralones are hydrogenated
to cis-benzylic alcohols in dr’s and er’s
up to 99:1 via a CC and CO one-pot reduction in the
presence of 2–5 mol % Noyori–Ikariya-type RuII chiral complexes and HCO2Na as a hydrogen source under
asymmetric transfer hydrogenation–dynamic kinetic resolution
(ATH-DKR) conditions. The oxidation of theses substrates resulted
in the enantioselective synthesis of the natural homoisoflavanone
dihydrobonducellin and its carba-analogues.
Six quinoline-piperonal hybrids were synthesized and evaluated as potential drugs against Alzheimer’s disease (AD). Theoretical analysis of the pharmacokinetic and toxicological properties of the compounds suggest that they present good oral bio-availability and are also capable of penetrating the blood–brain barrier, qualifying as leads for new drugs against AD. Evaluation of their inhibitory capacity against acetyl- and butyrilcholinesterases (AChE and BChE) through Ellmann’s test showed that three compounds present promising results with one of them being capable of inhibiting both enzymes. Further docking studies of the six compounds synthesized helped to elucidate the main interactions that may be responsible for the inhibitory activities observed.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.