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. 2020 Dec 22;13(1):6. doi: 10.3390/pharmaceutics13010006

Table 1.

Inhibitory activities of the new hybrid compounds against E. coli DNA gyrase and topoisomerase IV.

graphic file with name pharmaceutics-13-00006-i001.jpg
Cpd. R X IC50 [nM] 1
E. coli
DNA Gyrase Topoisomerase IV
3a H graphic file with name pharmaceutics-13-00006-i002.jpg 450 ± 180 1000 ± 150
3b OBn graphic file with name pharmaceutics-13-00006-i003.jpg 3300 ± 1500 >10,000
7a H graphic file with name pharmaceutics-13-00006-i004.jpg 92 ± 10 2500 ± 1300
7b H graphic file with name pharmaceutics-13-00006-i005.jpg 130 ± 10 3100 ± 0
11a 2 H graphic file with name pharmaceutics-13-00006-i006.jpg 130 ± 30 >10,000
11b 3 OBn graphic file with name pharmaceutics-13-00006-i007.jpg 14 ± 9 2500 ± 1100
1a 4 13 ± 0 500 ± 280
1b 5 <10 350 ± 50
CP 6 120 ± 20 5400 ± 2100
NB 7 170 ± 20 11,000 ± 2000

1 Concentration of compound (mean ±SD, in nM) that inhibits the enzyme activity by 50%; 2, 3 Compounds 11a and 11b were obtained as hydrochloride salts; 4, 5 1a and 1b, GyrB and ParE inhibitors; 6 CP, ciprofloxacin; 7 NB, novobiocin.