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. Author manuscript; available in PMC: 2020 Dec 11.
Published in final edited form as: J Med Chem. 2020 Jun 18;63(13):7033–7051. doi: 10.1021/acs.jmedchem.0c00366

Table 3.

Fusogenic potency and pharmacokinetic properties of 8 analogs lacking the triazol ringα

Cpd Structure EC50 (nM) t1/2 HLM (min) t1/2 MLM (min) PAMPA-BBB Pe (nm/sec)
8 graphic file with name nihms-1645549-t0031.jpg 5.26 (3.12–8.37) 8 28 10.29
10 graphic file with name nihms-1645549-t0032.jpg 383.16 (105.66-ND) 13.3 1.9 160
11 graphic file with name nihms-1645549-t0033.jpg 9.95 (6.99–14.05) 40.1 24.2 15.7
12 graphic file with name nihms-1645549-t0034.jpg 40.84 (21.44–71.75) >145 >145 7.96
13 graphic file with name nihms-1645549-t0035.jpg 8.18 (6.55–10.15) >145 92.4 26.28
α

EC50 values are mean with 95% confidence limits.