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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 1.

Biological Activity of Ureidopropanamides Derived from Modification of Compounds (R)- and (S)-4.

graphic file with name nihms957776u2.jpg
Ca+2 mobilization Ca+2 mobilization MTT
FPR2-HL60 FPR1-HL60 FPR2-HL60 FPR1-HL60
Compd. X Y Z EC50, μM (efficacy,%)[a] EC50, μM (efficacy, %)[a] IC50, μM (max. inhibition, %)[a] IC50, μM (max. inhibition, %)[a] EC50, μM[a]
(R)-4 OCH3 CN 4-Cl-3-F 0.63 ± 0.2 (100)[b] 1.8 ± 0.3 (60) [b] N.T.[c] N.T. N.T.
(S)-4 OCH3 CN 4-Cl-3-F 0.45 ± 0.1 (115) [b] 3.4 ± 0.9 (60) [b] N.T. N.T. N.T.
(R)-24 OH CN H N.A. [d] N.A. N.A. N.A. >100
(S)-24 OH CN H N.A. N.A. N.A. 16.4 ± 3.4 (55) >100
(R)-25 OCH3 OH H 0.41 ± 0.16 (90) 5.1 ± 1.3 (55) 24.8 ± 2.4 (75) N.A. >100
(S)-25 OCH3 OH H 2.9 ± 0.8 (130) 1.5 ± 0.3 (95) 9.8 ± 2.1 (95) N.A. >100
(R)-26 OCH3 CN 3-OH 2.6 ± 0.14 (65) N.A. 2.1 ± 0.4 (60) N.A. 44.4
(S)-26 OCH3 CN 3-OH 0.18 ± 0.09 (115) 1.4 ± 0.4 (100) 0.98 ± 0.13 (85) N.A. >100
(R)-27 OCH3 CN 4-OH 7.0 ± 2.0 (70) N.A. 29.5 ± 2.6 (50) N.A. >100
(S)-27 OCH3 CN 4-OH 1.6 ± 0.5 (75) 1.3 ± 0.4 (120) 3.7 ± 1.3 (85) N.A. 21.8
[a]

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

[b]

data taken from ref. [33];