Category: imidazoles-derivativesIn 2017 ,《Polysubstituted 2-aminoimidazoles as anti-biofilm and antiproliferative agents: Discovery of potent lead》 appeared in European Journal of Medicinal Chemistry. The author of the article were Gill, Rupinder Kaur; Kumar, Virender; Robijns, Stijn C. A.; Steenackers, Hans P. L.; Van der Eycken, Erik V.; Bariwal, Jitender. The article conveys some information:
Most of the human bacterial infections are associated with the biofilm formation and the natural tolerance of biofilms to antibiotics challenges treatment. Because of their low immunity, cancer patients are especially susceptible to bacterial infections. Compounds with anti-biofilm activity could therefore become a useful adjunct to chemotherapy, in particular if they also show antiproliferative activities. Taking this into consideration and as a result of continuous interest in 2-aminoimidazole derivatives, a series of novel polysubstituted 2-aminoimidazoles, e.g. I, was designed and synthesized. The compounds were evaluated against a panel of three bacterial strains for their biofilm and planktonic growth inhibitory activity and most of them show promising results. Furthermore, the synthesized compounds were evaluated against various cancer cell lines and almost all the compounds were found to possess potent antiproliferative activity. The substitution pattern at the C-4 position and the aryl carboxamide ring at the N-1 position have major effects on the biofilm inhibitory and antiproliferative activity. Especially, the introduction of a p-Me group at the carboxamide ring remarkably enhances both the anti-biofilm and antiproliferative activity. Two potent compounds were further studied for their antiproliferative activity and a flow cytometer-based cell cycle experiment was performed, which revealed their capability to induce G2/M phase cell cycle arrest. Based on these results, these two new compounds having potential to target both cancer proliferation and microbial biofilms might be used in single drug monotherapy. The experimental process involved the reaction of 1H-Imidazol-2-amine(cas: 7720-39-0Category: imidazoles-derivatives)
1H-Imidazol-2-amine(cas: 7720-39-0) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Category: imidazoles-derivatives
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem