Skip to main content
. 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 2.

Fusogenic potency and pharmacokinetic properties of 1 analogs bearing cyclohexane and triazol group substitutionsα

graphic file with name nihms-1645549-t0016.jpg
Cpd R1 R2 EC50 (nM) t1/2 HLM (min) t1/2 MLM (min) PAMPA-BBB Pe (nm/sec) Plasma t1/2 (hours)
2 graphic file with name nihms-1645549-t0017.jpg graphic file with name nihms-1645549-t0018.jpg 4.86 (4.05–5.82) 6 2 21.7 0.21
4 graphic file with name nihms-1645549-t0019.jpg graphic file with name nihms-1645549-t0020.jpg 76.02 (33.15-ND) 5 1 36.6 ND
5 graphic file with name nihms-1645549-t0021.jpg graphic file with name nihms-1645549-t0022.jpg 5.13 (2.64–9.11) 62 17 1.4 ND
6 graphic file with name nihms-1645549-t0023.jpg graphic file with name nihms-1645549-t0024.jpg 10.11 (3.49–28.47) >145 91 1 0.19
7 graphic file with name nihms-1645549-t0025.jpg graphic file with name nihms-1645549-t0026.jpg >1000 43 6 10.4 ND
8 graphic file with name nihms-1645549-t0027.jpg graphic file with name nihms-1645549-t0028.jpg 5.26 (3.12–8.37) 8 28 10.3 ND
9 graphic file with name nihms-1645549-t0029.jpg graphic file with name nihms-1645549-t0030.jpg 2.26 (1.01–4.65) >145 >145 0.03 0.38
α

EC50 values are mean with 95% confidence limits. Plasma t1/2 is in mice after IV bolus administration. ND means not determined.