European Journal of Medicinal Chemistry p. e426 - e437 (2016)
Update date:2022-08-04
Topics:
Negi, Beena
Kumar, Deepak
Kumbukgolla, Widuranga
Jayaweera, Sampath
Ponnan, Prija
Singh, Ramandeep
Agarwal, Sakshi
Rawat, Diwan S.
MRSA causes 60-70% of Staphylococcus aureus infection in hospitals and it has developed resistance against the currently available drugs. Interestingly, a series of 35 metronidazole-triazole hybrids on screening against MRSA were found to be active. Compound 22 was found to be effective at 4 μg/mL concentration against nine strains of MRSA. The inhibitory activity was further enhanced upto 1 μg/mL when this compound was used in combination with oxacillin in 1:1 ratio. All the compounds were found to be non-toxic in THP-1 cell line upto a concentration of 50 μM. The time-kill kinetics studies suggested bacteriostatic nature of the compounds. In silico studies show that these compounds interact with Thr600, Ser598, Asn464, His583 and Tyr446 in the active site of PBP2a crystal structure from MRSA.
View Moreshanghai tuomiao chemicial co.,ltd.
website:https://www.tuomiaochem.com/
Contact:021 - 59853336
Address:shanghai
JiangXi Keyuan Biopharma Co., LTD.
Contact:+86-563-6833666
Address:Guangde Fine Chemical Zone, Anhui Province, China
Contact:+86-0592 5353131
Address:No.56 Guani Road Software Park 2,Siming District
Rizhao Lanxing Chemical Indusrial Co.,Ltd
Contact:86-633-2616708
Address:NO.15 West road Shenglan, Lanshan district, Rizhao City
Contact:13357117572
Address:No.149 Shiji dadao Road.
Doi:10.1021/ja01526a052
(1959)Doi:10.1021/ja00465a072
(1977)Doi:10.1016/S0040-4039(01)83817-X
(1977)Doi:10.1016/j.bmc.2013.01.008
(2013)Doi:10.1021/ja00466a048
(1977)Doi:10.1246/bcsj.50.2986
(1977)