Frejat, Firas Obaid Arhema;Cao, Yaquan;Zhai, Hongjin;Abdel-Aziz, Salah A.;Gomaa, Hesham A. M.;Youssif, Bahaa G. M.;Wu, Chunli published 《Novel 1,2,4-oxadiazole/pyrrolidine hybrids as DNA gyrase and topoisomerase IV inhibitors with potential antibacterial activity》. The research results were published in《Arabian Journal of Chemistry》 in 2022.Product Details of 100-54-9 The article conveys some information:
DNA gyrase is a promising target for antibacterial agents. Several classes of small-mol. inhibitors have been discovered in recent decades, but none of these have reached the market. We have designed a small library of 1,2,4-oxadiazole/pyrrolidine hybrids with mid nanomolar inhibitory and potent antibacterial activities against DNA gyrase and topoisomerase IV. Compounds 9, 15, 16, 19, and 21 inhibited Escherichia coli DNA gyrase to a similar extent as the reference compound, novobiocin, with inhibitory values ranging from 120 nM to 270 nM. Compound 16 was one of the most potent compounds in the series, with an IC50 value of 120 nM against E. coli gyrase, which is lower than the IC50 value of novobiocin (170 nM). Compound 16 had the highest inhibitory activity, with min. inhibitory concentrations (MIC) of 24 and 62 ng/mL against Staphylococcus aureus and E. coli, resp., which compared favorably with ciprofloxacin (30 and 60 ng/mL, resp.). Compounds 9, 15, 19, and 21 were similar to novobiocin in terms of their activity against E. coli and S. aureus topoisomerase IV, while compound 16 was more potent than novobiocin. To complete the study, the researchers used 3-Cyanopyridine (cas: 100-54-9) .
3-Cyanopyridine(cas: 100-54-9) is an antimicrobial agent that can be used in the treatment of infectious diseases.Product Details of 100-54-9 It has been shown to be effective against a variety of bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and Streptococcus pneumoniae.