Synthesis of -Alkenylated Heterocycles via TP-Promoted Condensation with Ketones.

Herein, we describe a convenient protocol for the synthesis of -alkenylated heterocycles using abundant ketone electrophiles and TP as a water scavenger under microwave irradiation. The method can be applied to a diverse range of -heterocycles and ketones with good to excellent yields (up to 94%). This procedure is particularly attractive, as it is metal- and base-free, tolerates a variety of functional groups, and offers ease of product purification.

Discovery and Optimization of a Novel Macrocyclic Amidinourea Series Active as Acidic Mammalian Chitinase Inhibitors.

Our research group has been involved for a long time in the development of macrocyclic amidinoureas (MCAs) as antifungal agents. The mechanistic investigation drove us to perform an target fishing study, which allowed the identification of chitinases as one of their putative targets, with showing a submicromolar inhibition of chitinase. In this work, we investigated the possibility to further inhibit the corresponding human enzymes, acidic mammalian chitinase (AMCase) and chitotriosidase (CHIT1), involved in several chronic inflammatory lung diseases.

Focused library of phenyl-fused macrocyclic amidinoureas as antifungal agents.

The rise of antimicrobial-resistant phenotypes and the spread of the global pandemic of COVID-19 are worsening the outcomes of hospitalized patients for invasive fungal infections. Among them, candidiases are seriously worrying, especially since the currently available drug armamentarium is extremely limited. We recently reported a new class of macrocyclic amidinoureas bearing a guanidino tail as promising antifungal agents.