Synthesis and antifungal and antibacterial bioactivity of cyclic diamines containing boronate esters

Synthesis, characterization and antifungal testing of 3,4-dihydropyrimidin-2(1H)-(thio)ones containing boronic acids and boronate esters

“…Although related N 2 B heterocycles are potent antifungal agents [31], none of the boron containing dihydropyrimidinones showed any appreciable activity against Aspergillus niger, Aspergillus flavus, Candida albicans and Saccharomyces cerevisiae using Amphotericin B as a control.…”

ortho‐(Aminomethyl)phenylboronic acids—synthesis, structure and sugar receptor activity

“…[4] These and many other applications have been recently reviewed by Cuthbertson. [5] From the medicinal chemistry point of view, the phenylboronic acid derivatives are used in anticancer therapy as boron neutron capture therapy (BNCT) [6] or as chemotherapeutic agents, [7] antibiotics, [8] enzyme inhibitors [9] or for the treatment of tumors. [10] Their unique feature of forming reversible covalent complexes with sugars [11] has been applied in the design of new saccharide sensors, [12] particularly focused on the measure of the blood glucose level of diabetic patients.…”

Synthesis, structure, and antifungal activity of dihydropyridones containing boronate esters

“…As part of our ongoing investigation into making novel boron compounds [12], and considering the wealth of bioactivities found in aminoboronic acid derivatives, we decided to examine the synthesis of boron-containing 2,3-dihydro-4-pyridones using the aza Diels-Alder reaction with Danishefsky's diene. Previous studies have shown that compounds containing boronic acids can be extremely difficult to characterize in terms of elemental composition, owing to the ease with which they partially dehydrate to the corresponding trimeric and oligomeric anhydrides [13].…”