. 2013 Sep 4;4(10):932–936. doi: 10.1021/ml400151c

Table 1. Modification of the Triazole Ring Substituent in trans-Racemate^a.

graphic file with name ml-2013-00151c_0005.jpg

compd	R	SSI (IC₅₀ nM)	CSI (IC₅₀ nM)	logD_6.4	PAMPA (pH 7.4)	in vivo CSI (3 mg/kg %)
4	Me	36	290	–0.4	<2	30
5	iPr	11	91	0.37	4.7	15
6	CH₂F	6.0	77			48
7	CF₃	3.2	130	0.83	10	71

SSI: squalene synthase inhibitory activity. CSI: cholesterol synthesis inhibitory activity in rat hepatic cells. PAMPA: cell permeability score at pH 7.4. In vivo CSI: hepatic cholesterol inhibition (%) in rats at 1 h after 3 mg/kg single dose oral administration. No data = not tested.

Table 1. Modification of the Triazole Ring Substituent in trans-Racematea.

Table 1. Modification of the Triazole Ring Substituent in trans-Racemate^a.