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. Author manuscript; available in PMC: 2011 Jun 7.
Published in final edited form as: J Med Chem. 2010 May 13;53(9):3772–3781. doi: 10.1021/jm100235h

Figure 1.

Figure 1

SAR around early bithiazole lead 1 led to s-cis-locked bithiazole 2, but these compounds have poor hydrophilicity. The structural features of these bithiazoles inspired the design of pyrazolylthiazole libraries based on differentially Nβ- and Nγ-substituted analogs 4 and 5, respectively.