The inclusion of fluorine atoms or heterocyclic moiety into drug structures represents a recurrent motif in medicinal chemistry. The combination of these two features is constantly appearing in new molecular entities with various biological activities. This is demonstrated by the increasing number of newly synthesized fluorinated heterocyclic compounds among the Food and Drug Administration FDA-approved drugs. In this review, the biological activity, as well as the synthetic aspects, of 33 recently FDA-approved fluorinated heterocyclic drugs from 2016 to 2022 are highlighted.

One of the main causes of mortality in humans continues to be infectious diseases. Scientists are searching for new alternatives due to the fast increase in resistance of some harmful bacteria to the frontline antibiotics. To effectively treat pathogenic infections, it is crucial to design antibiotics that can prevent the development of pathogenic resistance. For this purpose, a set of 39 quaternary pyridinium and bis-pyridinium salts with different lengths of side alkyl or fluorinated chains, heterocyclic spacers, and counter ions were tested on diverse reference bacterial ATCC (American Type Culture Collection) strains, such as S. aureus and E. coli. Subsequently, 6 out of the 39 pyridinium salts showing relevant MIC (Minimum Inhibitory Concentration) values were tested on clinically isolated, resistant strains of S. aureus, S. epidermids, S. haemolyticus, K. pneumoniae, A. baumannii, and P. aeruginosa. Additional tests have been performed to assess if the minimum concentration detected through MIC assay may limit the growth of biofilms.

Diffuse large B‐cell lymphoma (DLBCL) is the most common subtype of non‐Hodgkin lymphoma, characterized by significant clinical and molecular heterogeneity. Here, we report the design and synthesis of a novel series of 2‐styrylquinoline‐4‐carboxamides via an efficient microwave‐assisted organic synthesis (MAOS) approach. This strategy enabled the rapid and high‐yielding isolation of derivatives 4a–z and 4aa–ah in three steps from commercially available isatin. Among the 34 compounds synthesized, 24 showed antiproliferative activity in vitro, with compound 4i displaying sub‐micromolar IC₅₀ values across multiple lymphoma cell lines, including SU‐DHL‐8 and TOLEDO. Mechanism of action studies demonstrated that 4i was able to induce G₂/M cell‐cycle arrest and DNA synthesis suppression, coupled with mitochondrial membrane depolarization and reactive oxygen species (ROS) accumulation, suggesting activation of the intrinsic apoptotic pathway. Importantly, active derivatives were nontoxic to healthy peripheral blood mononuclear cells (PBMCs), indicating a favorable therapeutic window. These results validate the quinoline scaffold as a promising chemotype, highlighting the utility of MAOS for the sustainable synthesis of bioactive heterocycles.

The constitutive low aromaticity of easily accessible 5-trifluoromethyl-1,2,4-oxadiazoles is explored to enable editing modification to the corresponding unprecedented gem -disubstituted 1,2,4-oxadiazolines.

We report on the synthesis and characterization of four novel Ru(II) polypyridyl complexes incorporating bipyridine or phenanthroline ancillary ligands. Substituted 1,2,4-oxadiazoles are introduced here for the first time as chelating...