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. Author manuscript; available in PMC: 2018 Oct 11.
Published in final edited form as: Chem Rev. 2017 Sep 27;117(19):12415–12474. doi: 10.1021/acs.chemrev.7b00283

Table 3.

Biological Evaluation of Extended-Reach Azithromycin Analogsa

Linker Indole IC50 MIC50
119 C3H8 graphic file with name nihms949912t1.jpg 0.54 0.78
120 C3H8 graphic file with name nihms949912t2.jpg 0.88 0.78
121 C3H8 graphic file with name nihms949912t3.jpg 0.227 1.56
122 C3H8 graphic file with name nihms949912t4.jpg 0.128 1.56
123 C3H8 graphic file with name nihms949912t5.jpg 0.49 0.78
124 C3H8 graphic file with name nihms949912t6.jpg 0.147 1.56
125 C6H4 graphic file with name nihms949912t7.jpg 0.12 3.13
126 C6H4 graphic file with name nihms949912t8.jpg 0.197 1.56
azithromycin (36) 0.292 0.78
a

IC50 values in μM and tested against cell-free E. coli ribosomes; MIC50 values in μg/mL against a susceptible strain of S. aureus; green denotes an increased activity; orange, decreased; yellow, equipotent.