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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

Table 1.

Nγ-Substituted pyrazolylthiazole analogs.

graphic file with name nihms-295551-f0010.jpg

R1 = C(CH3)3, C6H5

R2 = CH2CH=CH2, C6H4(4-Br), CH2C6H5, (CH2)2OH

X = OEt, NHC6H4(4-OMe), NHCH2C6H5, NH(CH2)2OH, N(CH2CH2)2O, OH

Compd R1 R2 X
9a C(CH3)3 CH2CH=CH2 OEt
9b C(CH3)3 C6H4(4-Br) OEt
9c C(CH3)3 CH2C6H5 OEt
9d C(CH3)3 CH2CH2OH OEt
9e C6H5 CH2CH=CH2 OEt
9f C6H5 C6H4(4-Br) OEt
9g C6H5 CH2C6H5 OEt
9h C6H5 CH2CH2OH OEt
11a C(CH3)3 CH2CH=CH2 NHC6H4(4-OMe)
11b C(CH3)3 CH2CH=CH2 NHCH2C6H5
11c C(CH3)3 CH2CH=CH2 N(CH2CH2)2O
11d C(CH3)3 C6H4(4-Br) NHC6H4(4-OMe)
11e C(CH3)3 C6H4(4-Br) NHCH2C6H5
11f C(CH3)3 C6H4(4-Br) N(CH2CH2)2O
11g C(CH3)3 CH2C6H5 NHC6H4(4-OMe)
11h C(CH3)3 CH2C6H5 NHCH2C6H5
11i C(CH3)3 CH2C6H5 N(CH2CH2)2O
11j C(CH3)3 CH2CH2OH NHC6H4(4-OMe)
11k C(CH3)3 CH2CH2OH NHCH2C6H5
11l C(CH3)3 CH2CH2OH N(CH2CH2)2O
11m C6H5 CH2CH=CH2 NH(CH2)OH
11n C6H5 C6H4(4-Br) NH(CH2)OH
11o C6H5 CH2C6H5 NH(CH2)OH
11p C6H5 CH2CH2OH NH(CH2)OH
11q C6H5 CH2CH=CH2 NHC6H4(4-OMe)
11r C6H5 C6H4(4-Br) NHC6H4(4-OMe)
11s C6H5 CH2C6H5 NHC6H4(4-OMe)
11t C6H5 CH2CH2OH NHC6H4(4-OMe)
11u C6H5 CH2CH=CH2 N(CH2CH2)2O
11v C6H5 C6H4(4-Br) N(CH2CH2)2O
11w C6H5 CH2C6H5 N(CH2CH2)2O
11x C6H5 CH2CH2OH N(CH2CH2)2O
12a C(CH3)3 CH2CH=CH2 OH
12b C(CH3)3 C6H4(4-Br) OH
12c C(CH3)3 CH2C6H5 OH
12d C6H5 CH2CH=CH2 OH
12e C6H5 C6H4(4-Br) OH
12f C6H5 CH2C6H5 OH
12g C6H5 CH2CH2OH OH