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. Author manuscript; available in PMC: 2018 Nov 22.
Published in final edited form as: ChemMedChem. 2017 Nov 7;12(22):1839–1847. doi: 10.1002/cmdc.201700429

Table 2.

Biological Activity of Ureidopropanamides Derived from Modification of Compound 2.

graphic file with name nihms957776u3.jpg
Ca+2 mobilization Ca+2 mobilization MTT
FPR2-HL60 FPR1-HL60 FPR2-HL60 FPR1-HL60
Compd. X Y EC50, μM (efficacy, %)[a] EC50, μM (efficacy, %)[a] IC50, μM (max. inhibition, %)[a] IC50, μM (max. inhibition, %)[a] EC50, μM[a]
(S)-2 4-Br H 0.004 ± 0.002 (115)[b] 0.3 ± 0.08 (135) [b] N.T.b N.T. N.T.
(2R)-42 4-OH H N.A.c N.A. N.A. N.A. >100
(2R)-43 3-OH H N.A. 12.5 ± 2.5 (90) N.A. N.A. >100
(2S)-44 4-OH H N.A. 11.0 ± 3.6 (65) N.A. N.A. >100
(2S)-45 3-OH H N.A. 0.55 ± 0.13 (90) N.A. 1.2 ± 0.4 (90) >100
(2R)-46 4-Br OH 0.35 ± 0.12 (140) 0.82 ± 0.37 (110) 25.3 ± 7.2 (100) 0.56 ± 0.17 (85) >100
(2S)-47 4-Br OH 0.78 ± 0.23 (90) 0.23 ± 0.05 (125) 2.1 ± 0.6 (100) 0.076 ± 0.014 (95) >100
[a]

data are the mean of three indipendent experiments; N.T.= not tested; N.A.= not active;

[b]

data taken from ref. [28].