The sustainable development of our future represents an unorthodox challenge in sciences and technologies.The exploration of unconventional chemical reactivities that could potentially result in more sustainable chemi...The sustainable development of our future represents an unorthodox challenge in sciences and technologies.The exploration of unconventional chemical reactivities that could potentially result in more sustainable chemical productions with efficient utilization of resource and inherent prevention of waste will provide the foundation for the synthetic chemistry of our future.As part of this endeavor,we have explored metal-mediated reactions in water to minimize protection-deprotection and the use of organic solvents,catalytic nucleophilic additions via C-H reactions to avoid generation and use of stoichiometric organic halides and metal in water,and Cross-Dehydrogenative-Coupling(CDC) reactions to minimize overall transformation steps.展开更多
A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial ...A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution technique.The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and Fluconazole.The combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive A.flavus.In addition,the interaction of compound 5l with calf thymus DNA demonstrated that this compound could effectively intercalate into DNA to form a compound 5l-DNA complex that might block DNA replication and thereby exert good antimicrobial activity.展开更多
基金the Canada Research Chair (Tier I) foundationthe E. B. Eddy Endowment Fund+1 种基金the CFI, NSERC, FQRNTthe NSF and the NSF-EPA Joint Program for a Sustainable Environment for partial support of our research over the years
文摘The sustainable development of our future represents an unorthodox challenge in sciences and technologies.The exploration of unconventional chemical reactivities that could potentially result in more sustainable chemical productions with efficient utilization of resource and inherent prevention of waste will provide the foundation for the synthetic chemistry of our future.As part of this endeavor,we have explored metal-mediated reactions in water to minimize protection-deprotection and the use of organic solvents,catalytic nucleophilic additions via C-H reactions to avoid generation and use of stoichiometric organic halides and metal in water,and Cross-Dehydrogenative-Coupling(CDC) reactions to minimize overall transformation steps.
基金supported by the National Natural Science Foundation of China (21172181,21372186)the Research Fellowship for International Young Scientists from the International (Regional) Cooperation and Exchange Program (81250110554,81350110338,81350110523)+1 种基金the key program from Natural Science Foundation of Chongqing (CSTC2012- jjB10026)the Specialized Research Fund for the Doctoral Program of Higher Education of China (20110182110007)
文摘A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS spectra.All the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution technique.The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and Fluconazole.The combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive A.flavus.In addition,the interaction of compound 5l with calf thymus DNA demonstrated that this compound could effectively intercalate into DNA to form a compound 5l-DNA complex that might block DNA replication and thereby exert good antimicrobial activity.
