Antiparasitic Activities of Acyl Hydrazones from Cinnamaldehydes and Structurally Related Fragrances.

New drugs for the treatment of protozoal parasite infections such as toxoplasmosis and leishmaniasis are required. Cinnamaldehyde and its derivatives appear to be promising antiparasitic drug candidates. Acyl hydrazones of cinnamaldehyde, 4-dimethylaminocinnamaldehyde, and of the synthetic fragrances silvial and florhydral were prepared and tested for activity against () and () parasites.

Superior Anticancer and Antifungal Activities of New Sulfanyl-Substituted Niclosamide Derivatives.

The approved anthelmintic salicylanilide drug niclosamide has shown promising anticancer and antimicrobial activities. In this study, new niclosamide derivatives with trifluoromethyl, trifluoromethylsulfanyl, and pentafluorosulfanyl substituents replacing the nitro group of niclosamide were prepared (including the ethanolamine salts of two promising salicylanilides) and tested for their anticancer activities against esophageal adenocarcinoma (EAC) cells. In addition, antifungal activity against a panel of strains, the most abundant causative agent of the neglected tropical disease eumycetoma, was evaluated.

A New Synthetic Curcuminoid Displays Antitumor Activities in Metastasized Melanoma.

Aim: The semisynthetic derivatives MePip-SF5 and isogarcinol, which are aligned with the natural products curcumin and garcinol, were tested for their antitumor effects in a preclinical model of pulmonary melanoma metastasis.

Methods And Results: MePip-SF5 was almost five times more effective in inhibiting B16F10 melanoma cell proliferation than its original substance of curcumin (IC MePip-SF5 2.8 vs.

Analogs of the Catechol Derivative Dynasore Inhibit HIV-1 Ribonuclease H, SARS-CoV-2 nsp14 Exoribonuclease, and Virus Replication.

Viral replication often depends on RNA maturation and degradation processes catalyzed by viral ribonucleases, which are therefore candidate targets for antiviral drugs. Here, we synthesized and studied the antiviral properties of a novel nitrocatechol compound () and other analogs that are structurally related to the catechol derivative dynasore. Interestingly, compound strongly inhibited two DEDD box viral ribonucleases, HIV-1 RNase H and SARS-CoV-2 nsp14 3'-to-5' exoribonuclease (ExoN).

Fluorinated and -Acryloyl-Modified 3,5-Di[()-benzylidene]piperidin-4-one Curcuminoids for the Treatment of Pancreatic Carcinoma.

Pancreatic carcinoma is a cancer disease with high mortality. Thus, new and efficient treatments for this disease are badly needed. Curcumin has previously shown promising effects in pancreatic cancer patients; however, this natural compound suffers from inadequate efficacy and bioavailability, preventing its clinical approval.