Synthesis, Molecular Modeling, and Biological Evaluation of Novel Tetrahydro-β-Carboline Hydantoin and Tetrahydro-β-Carboline Thiohydantoin Derivatives as Phosphodiesterase 5 Inhibitors

Table 1

Inhibitory effect of the synthesized compounds on PDE5.

Cpd #	%PDE5 inhibition at 10 μM	PDE5 inhibition IC50 μM	Cpd #	%PDE5 inhibition at 10 μM	PDE5 inhibition IC50 μM
1	77	2.5	11	46	ND
2	63	ND	12	87	0.55
3	55	ND	13	63	ND
4	75	6.4	14	60	ND
5	87	0.36	15	35	ND
6	88	0.72	16	63	ND
7	54	ND	17	29	ND
8	97	0.36	18	23	ND
9	83	2.4	19	87	0.56
10	68	ND	20	58	ND
Tadalafil	99	0.004