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. Author manuscript; available in PMC: 2018 Oct 11.
Published in final edited form as: Chem Rev. 2017 Sep 27;117(19):12415–12474. doi: 10.1021/acs.chemrev.7b00283

Table 9.

Biological Evaluation of AIP Analogs and Amide Derivatives Thereofa

AgrC
Sequence I II III* IV
331 AIP-III IN(CDFLL) 5.05 5.63 ag 8.53
342 AIP-III Amide IN(XDFLL) >1000 >1000 75.2 299
335 D4A IN(CAFLL) 0.485 0.429 0.0506 0.0349
343 D4A Amide IN(XAFLL) 1.2 2.19 0.055 0.192
340 tD2A Ac(CAFLL) 0.257 0.9 0.329 0.0957
344 tD2A Amide Ac(XAFLL) 1.5 13.9 0.216 0.189

graphic file with name nihms949912u8.jpg

a

IC50 in nM, X = L-diaminopropionic acid, ag = agonist, t = truncated.

*

For the sake of comparison, x-fold improvement against AgrC-III is measured against the amide.