https://zenodo.org/record/1003263/files/Cushnie%20et%20al%20%282011%29%20post-peer%20reviewed%20version.pdf

Recent advances in understanding the antibacterial properties of flavonoids

Imidazole ring is an important five-membered aromatic heterocycle widely present in natural products and synthetic molecules. The unique structural feature of imidazole ring with desirable electron-rich characteristic is beneficial for imidazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of imidazole-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous imidazole-based compounds as clinical drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potency, which have shown the enormous development value. This work systematically gives a comprehensive review in current developments of imidazole-based compounds in the whole range of medicinal chemistry as anticancer, antifungal, antibacterial, antitubercular, anti-inflammatory, antineuropathic, antihypertensive, antihistaminic, antiparasitic, antiobesity, antiviral, and other medicinal agents, together with their potential applications in diagnostics and pathology. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic imidazole-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes.

Comprehensive Review in Current Developments of Imidazole‐Based Medicinal Chemistry

Recent developments in biological activities of chalcones: a mini review.

Objective: Some natural products consisting of the alkaloids yohimbine and vincamine (indole-type), scopolamine and atropine (tropane-type), colchicine (tropolone-type), allantoin (imidazolidine-type), trigonelline (pyridine-type) as well as octopamine, synephrine, and capsaicin (exocyclic amine-type); the flavonoid derivatives quercetin, apigenin, genistein, naringin, silymarin, and silibinin; and the phenolic acids namely gallic acid, caffeic acid, chlorogenic acid, and quinic acid, were tested for their in vitro antiviral, antibacterial, and antifungal activities and cytotoxicity.Materials and methods: Antiviral activity of the compounds was tested against DNA virus herpes simplex type 1 and RNA virus parainfluenza (type-3). Cytotoxicity of the compounds was determined using Madin-Darby bovine kidney and Vero cell lines, and their cytopathogenic effects were expressed as maximum non-toxic concentration. Antibacterial activity was assayed against following bacteria and their isolated strains: Escherichi...

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Cytotoxicity, antiviral and antimicrobial activities of alkaloids, flavonoids, and phenolic acids

Plants as sources of new antimicrobials and resistance-modifying agents

A review of anti-infective and anti-inflammatory chalcones.

Synthesis, physicochemical properties and antimicrobial evaluation of new (E)-chalcones.

Syntheses of 11 new N-bromoalkyl substituted bromides of (E)-4-azachalcone and N-o-(m- and p-) halobenzyl substituted halides of (E)-3'-hydroxy-4-azachalcone of antimicrobial activity are reported. Compounds 3d, 3e, 6b, 6c, and 6e reveal good antimicrobial activity against Staphylococcus aureus and Enterococcus faecalis as well as moderate activity against Escherichia coli and Klebsiella pneumoniae.

Synthesis and antimicrobial properties of N-substituted derivatives of (E)-4-azachalcones.

The synthesis of 24 new 2-alkylthio and 2-(E)-N-thioalkyl-4-azachalkonyl substituted derivatives of uracil and their antimicrobial activity are reported. In particularly compounds 6o and 6p showed a good antibacterial activity against Staphylococcus aureus and Streptococcus faecalis.

Synthesis and antimicrobial properties of S-substituted derivatives of 2-thiouracil.

Twelve new N-substituted (E)-azachalconium bromides were synthesized and tested for antimicrobial and antifungal activities. Compounds 5c, 5d and 5h-5l showed very good antimicrobial activity against Staphylococcus aureus, Enterococcusfaecalis as well as Bacillus subtilis and 5h-5j showed moderate activity against Escherichia coli. In particular, (E)-N-dodecyl-4-azachalconium bromide (5i) and (E)-N-tetradecyl-4-azachalconium bromide (5j) showed the most intensive activity against all tested microorganisms.

Zdzisława Nowakowska

Papers

A review of anti-infective and anti-inflammatory chalcones.

Synthesis, physicochemical properties and antimicrobial evaluation of new (E)-chalcones.

Synthesis and antimicrobial properties of N-substituted derivatives of (E)-4-azachalcones.

Synthesis and antimicrobial properties of S-substituted derivatives of 2-thiouracil.

Antimicrobial activity of some N-alkyl substituted of (E)-4-azachalconium and (E)-3′-hydroxy-4-azachalconium bromides