In 2022,Elsebaie, Mohamed M.; El-Din, Hanzada T. Nour; Abutaleb, Nader S.; Abuelkhir, Abdelrahman A.; Liang, Hsin-Wen; Attia, Ahmed S.; Seleem, Mohamed N.; Mayhoub, Abdelrahman S. published an article in European Journal of Medicinal Chemistry. The title of the article was 《Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus》.Application In Synthesis of Pyridin-3-ylboronic acid The author mentioned the following in the article:
A set of structurally related diphenylurea derivatives I [R = Ph, furan-2-yl, cyclohexyl, iso-Bu, etc.] bearing aminoguanidine moiety was synthesized, and their antibacterial activity was assessed against a panel of multi-drug resistant Gram-pos. clin. isolates. Two compounds I [R = furan-2-yl, 4-methyl-pent-1-en-1-yl] were identified with better bacteriol. profile than the lead I [R = I]. The multi-step resistance development studies indicated that MRSA are less likely to develop resistance toward diphenylurea compounds I. Moreover, these compounds I demonstrated a prolonged post-antibiotic effect than that of vancomycin. Furthermore, compounds I [R = furan-2-yl, 4-methyl-pent-1-en-1-yl] were able to re-sensitize VRSA to vancomycin, resulting in 8- to more than 32-fold improvement in vancomycin MIC values against clin. VRSA isolates. Finally, when assessed in an in vivo skin infection mouse model, the efficacy of I [R = 4-methyl-pent-1-en-1-yl] was very comparable to that of the com. available fusidic acid ointment. Addnl., the diphenylurea I [R = 4-methyl-pent-1-en-1-yl] did not have a pronounced effect on the animal weights along the experiment indicating its safety and tolerability to mice. Taken together, these results indicate that the diphenylurea scaffold merits further investigation as a promising anti-staphylococcal treatment option. In the experimental materials used by the author, we found Pyridin-3-ylboronic acid(cas: 1692-25-7Application In Synthesis of Pyridin-3-ylboronic acid)
Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. Application In Synthesis of Pyridin-3-ylboronic acid