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. Author manuscript; available in PMC: 2017 Apr 13.
Published in final edited form as: Bioorg Med Chem Lett. 2008 Jun 12;18(14):4064–4067. doi: 10.1016/j.bmcl.2008.05.098

Table 2. NPS Antagonist Activity for Alternate 7-Substitution.

graphic file with name nihms62190u3.jpg
Compound R NPS Ile107 Ke NPS Asn107 Ke Asn/Ile
5a graphic file with name nihms62190t12.jpg 354 ± 51 353 ± 22 1.0
1m graphic file with name nihms62190t13.jpg 339 ± 76 460 ± 130 1.4
1n graphic file with name nihms62190t14.jpg 244 ± 42 267 ± 41 1.1
1o graphic file with name nihms62190t15.jpg 911 ± 130 4640 ± 1400 5.1
1p graphic file with name nihms62190t16.jpg 1110 ± 30 1100 ± 300 1.0
1q −CH3 > 4 mM > 4 mM --
1r graphic file with name nihms62190t17.jpg 3760 ± 470 2560 ± 70 0.7
1s graphic file with name nihms62190t18.jpg 280 ± 41 354 ± 96 1.3
a

All target compounds were fully characterized using NMR and Mass Spectrometry.