TABLE 1.
Structure of compound A and other LCAT activators
| Compound | Chemical Name | EC50 | ECmax |
|---|---|---|---|
| mM | % | ||
| A | 3-((5-(ethylthio)-1,3,4-thiadiazol-2-yl)thio)pyrazine-2-carbonitrile | 0.794 | 161.3 |
| 5 | 3-((5-(methylthio)-1,3,4-thiadiazol-2-yl)thio)pyrazine-2-carbonitrile | 5.81 | 149.6 |
| 10 | 3-[5-(3-cyano-pyrazin-2-ylsulfanyl)-[1,3,4]thiadiazol-2-ylsulfanyl]-propionamide | 142a | 135.6b |
| 19 | ±-(3S,4R)-4-(3,5-difluorophenyl)-3-methoxy-1-(methylthio)azetidin-2-one | 1.69 | 167.3 |
| 20 | ±-(3S,4R)-4-(4-bromophenyl)-3-methoxy-1-(methylthio)azetidin-2-one | 1.02 | 165.4 |
EC50 and ECmax values are shown for compound A and derivatives (compounds 5 and 10) and for the β-lactam–based compounds 19 and 20.
a
Calculated at the highest dose.
b
Did not reach maximum.