Tag: structure-activity relationship

Modified FELL tetrapeptides showed that strong PDE4B inhibition in vitro did not reliably predict anti-inflammatory effects in rats.

Chemists have created twenty pyrrole-based hydrazide-hydrazone antioxidants, with a tryptophan-derived lead compound outperforming Trolox in radical-scavenging assays and showing potential ...

A new conceptual analysis argues that property cliffs, abrupt physicochemical property changes triggered by small structural modifications, exist across acidity, ...

Trypanosoma cruzi, the single-celled parasite behind Chagas disease, has long frustrated drug developers... One of the more striking aspects of ...

A second-generation library of N,N′-disubstituted aliphatic diamines shows potent, selective activity against multiple Leishmania species, with compounds 12a, 12m, and ...

Chemists have used a mild silicon catalyst to rapidly build dihydropyrimidinethione compounds that inhibit the cholinesterase enzymes implicated in Alzheimer's ...

A new review argues that benzothiazole derivatives, acting through DHFR inhibition and heme detoxification, could yield next-generation antimalarials effective against ...

Chemists have synthesised a series of sulfonamide-linked 1,2,3-triazole hybrids via click chemistry, with a dichloro-substituted lead showing activity against bacteria, ...

New halogenated bis-coumarin compounds inhibit both acetylcholinesterase and monoamine oxidase-B at micromolar concentrations, offering a dual-target template for Alzheimer's drug ...

A new review maps how plant-derived flavonoids attack tuberculosis through multiple molecular mechanisms while outlining the structural features and delivery ...