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. Author manuscript; available in PMC: 2013 Apr 20.
Published in final edited form as: ACS Chem Biol. 2012 Feb 13;7(4):672–677. doi: 10.1021/cb200496y

Figure 1. The structure of SR1001 (N-(5-(N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2- yl)phenyl)sulfamoyl)-4-methylthiazol-2-yl)acetamide) and SR2211 (1,1,1,3,3,3-hexafluoro-2-(2-fluoro-4'-((4-(pyridin-4-ylmethyl)piperazin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)propan-2-ol).

Figure 1

SR2211 was derived from SR1001 after several rounds of SAR. The hexaflurophenyl group was retained while modifying the left-hand portion of the molecule. The sulfonamide residue in SR1001 reduced CNS penetration so efforts were made to replace this with more lipophilic groups.