Table 1.

NPBWR1 antagonist activity of compounds 7a–7al (IC₅₀ μM)

Compound	R1	R2	IC50
7a	Cyclopentyl	H	3.70
7b	Phenyl	H	0.78
7c	2-Methylphenyl	H	0.37
7d	3-Methylphenyl	H	1.40
7e	4-Methylphenyl	H	1.70
7f	2-Trifluoromethylphenyl	H	0.37
7g	3-Trifluoromethylphenyl	H	1.80
7h	4-Trifluoromethylphenyl	H	1.00
7i	2,6-Dimethylphenyl	H	0.24
7j	3,5-Dimethylphenyl	H	0.41
7k	3,4-Dimethylphenyl	H	0.61
7l	4-Methoxyphenyl	H	3.80
7m	4-Phenylphenyl	H	9.40
7n	4-Isopropylphenyl	H	10.0
7o	4-Chlorophenyl	H	0.59
7p	2-Ethylphenyl	H	0.26
7q	2-Isopropylphenyl	H	0.64
7r	2-Methoxyphenyl	H	0.67
7s	2-(Methoxycarbonyl)phenyl	H	1.20
7t	2-Cyanophenyl	H	1.40
7u	(1,1′-Biphenyl)-2-yl	H	0.54
7v	2-(Pyrazol-1-yl)phenyl	H	0.22
7w	Anthracen-9-yl	H	0.32
7x	Naphtalen-2-yl	H	1.50
7y	Naphtalen-1-yl	H	0.14
7z	Naphthalen-1-ylmethyl	H	4.20
7aa	4-Fluoronaphtalen-1-yl	H	0.36
7ab	2-Methylnaphtalen-1-yl	H	0.22
7ac	2-Methoxynaphtalen-1-yl	H	0.35
7ad	4-Bromonaphtalen-1-yl	H	2.00
7ae	4-Methylnaphtalen-1-yl	H	0.37
7af	Quinolin-5-yl	H	3.40
7ag	Naphtalen-1-yl	CO2Et	0.45
7ah	Naphtalen-1-yl	CH2OH	2.50
7ai	Naphtalen-1-yl	CH2OAc	11.60
7aj	Naphtalen-1-yl	Me	1.90
7ak	Naphtalen-1-yl	Phenyl	18.00
7al	Phenyl	COPh	0.58

^aData are reported as mean of n = 3 determinations.