N-Benzoylthiourea-pyrrolidine carboxylic acid derivatives bearing an imidazole moiety: Synthesis, characterization, crystal structure, in vitro ChEs inhibition, and antituberculosis, antibacterial, antifungal studies

Imidazole‐hydrazone derivatives: Synthesis, characterization, X‐ray structures and evaluation of anticancer and carbonic anhydrase I–II inhibition properties

“…This ring is an essential building block developing new drug candidates because it is an essential part of structural scaffolds seen in contemporary medicinal chemistry. [9] The bioactivity of molecules with an imidazole ring has been found to include anticancer, [10] antioxidant, [11] antibacterial, [12] antiviral, [13] antitubercular [14] and antifungal [15] properties.…”

Identification of BACE-1 inhibitors through directed C(sp3)–H activation on 5-oxo-pyrrolidine-3-carboxylic acid derivatives

“…E-mail: andrea.trabocchi@unifi.it tion, [3 + 2] or [4 + 1] cycloaddition, 25 cascade reactions, or related transformations. 20,26 However, to the best of our knowledge, short and convenient synthesis of fully substituted 5-oxopyrrolidines, containing appendages in each available positions and bearing a carbonyl moiety in position 3 were not reported in the literature. In our previous synthetic efforts in the field of CNS drug discovery, [27][28][29] we reported the exploitation of the Castagnoli-Cushman reaction (CCR) to generate C-2 substituted morpholinone scaffolds as BACE-1 inhibitors.…”

Design, Synthesis and Bioactivity Evaluation of Novel 2-(pyrazol-4-yl)-1,3,4-oxadiazoles Containing an Imidazole Fragment as Antibacterial Agents

“…As a good pharmacodynamic group, imidazole can synergically enhance drug efficacy, improve in vitro and in vivo bioactivity, and reduce biotoxicity, and it also possesses excellent bioavailability, good tissue penetration and relatively low adverse reactions [ 1 , 2 , 3 ]. To date, imidazoles have become one of the most important skeletons in medicine and pesticide discovery, and many novel bioactive molecules have been reported based on this advantageous framework, such as antibacterial [ 4 , 5 ], antifungal [ 6 ], antiviral [ 7 ], anti-inflammatory [ 8 ], anticancer [ 9 ], antioxidant [ 10 ] and anti-Alzheimer’s disease [ 11 ]. Encouragingly, a number of imidazole core-containing medicines and pesticides have been successfully developed, especially in agricultural fields, and imidazole derivatives are widely applied as fungicides, herbicides and insecticides ( Figure 1 ).…”