Skip to main content
. Author manuscript; available in PMC: 2024 Jan 5.
Published in final edited form as: J Med Chem. 2023 Aug 21;66(17):11831–11842. doi: 10.1021/acs.jmedchem.3c00406

Table 1.

The sequences and minimum inhibitory concentrations and fold changes for Api-137, the C-terminal leucine carboxylic acid modified derivatives (* = decarboxy; ** = primary alcohol), and the Arg17 modifications.

Peptide Sequence Unnatural Amino Acid MIC (μM) Fold change
Api-137 gu-ONNRPVYIPRPRPPHPRL-OH none 0.16–0.3 1
1 gu-ONNRPVYIPRPRPPHPrL-OH r = homoarginine 2.5 16
2 gu-ONNRPVYIPRPRPPHPrL-OH r = citrulline 20 128
3 gu-ONNRPVYIPRPRPPHPRL-OH R = mono-methyl arginine 0.3 1
4 gu-ONNRPVYIPRPRPPHPRl-* l = decarboxy leucine >40 >800
5 gu-ONNRPVYIPRPRPPHPRl-** l = l-leucinol 5 32
6 gu-ONNRPVYIPRPRPPHPRl-** l = d-leucinol 10–20 62–128
7 gu-ONNRPVYIPRPRPPHPRf-** f = l-phenylalaninol 5 32
8 gu-ONNRPVYIPRPRPPHPRf-** f = d-phenylalaninol 40 800