Official websites use .gov
A
.gov website belongs to an official
government organization in the United States.
Secure .gov websites use HTTPS
A lock (
) or https:// means you've safely
connected to the .gov website. Share sensitive
information only on official, secure websites.
Additive SAR Simplified the Lead Optimization of the Spiroindolones
| Compound | R1 = F R2 = H 27 |
R1 = H R2 = F 28 |
R1 = F R2 = F 29 |
R1 = F R2 = Cl 30 (NITD609) |
||||
|---|---|---|---|---|---|---|---|---|
| NF54 EC50 (nM) | 3.4 | 3.5 | 0.2 | 0.9 | ||||
| Liver Microsomesa | CLint | t1/2 (min) | CLint | t1/2 (min) | CLint | t1/2 (min) | CLint | t1/2 (min) |
| Mouse | High | 4.2 | Low | 53 | Low | 49.1 | Low | 49 |
| Human | Med | 10 | Low | 53.3 | Low | 56.4 | Low | 76 |
intrinsic clearance in liver microsomes; where high clearance corresponds to low stability in the presence of liver enzymes.
