Synthesis and Pharmacological Valorization of Derivatives of 4-Phenyl-1,5-Benzodiazepin-2-One

Table 3

Results of the sedative activity of the products 5a–d at doses of 100 and 200 mg/kg ( compared to controls).

		Witness	Reference (bromazepam 20 mg/kg)	5a (100 mg/kg)	5a (200 mg/Kg)	5b (100 mg/kg)	5b (200 mg/kg)	5c (100 mg/kg)	5c (200 mg/kg)	5d (100 mg/kg)	5d (200 mg/kg)
Traction test	Percentage of falls (%)	0	100	10	12	8	8	0	0	0	0
	Average fall time (s)	0	10.0 ± 0.9	8.52 ± 2.94	4.48 ± 0.87	25.33 ± 7.12	8.80 ± 2.22	0	0	0	0
	Average recovery time (s)	0.50 ± 0.10	0	2.63 ± 1.15	1.38 ± 0.39	4.93 ± 2.53	3.37 ± 2.15	9.02 ± 2.58	5.71 ± 0.21	17.34 ± 4.70	14.71 ± 3.75
Chimney test	Average time to climb the chimney (s)	3.40 ± 0.50	>120	12.14 ± 2.19	8.19 ± 3.50	23.78 ± 5.67	12.48 ± 3.04	38.80 ± 10.14	33.29 ± 5.67	87.40 ± 12.74	75.63 ± 5.19
Hole-board test	Number of holes explored over 5 min	7 ± 1	0 ± 0	0.88 ± 0.38	0.84 ± 0.43	1.28 ± 0.36	1.20 ± 0.41	1.72 ± 1.29	1.48 ± 0.86	2.00 ± 1.12	1.80 ± 1.05
Rota-Rod test	Time spent on stem (s)	120 ± 0	1.2 ± 0.90	16.50 ± 3.35	15.40 ± 9.83	23.2 ± 6.98	19.25 ± 6.60	35.50 ± 11.9	25.20 ± 8.98	64.08 ± 26.02	40.20 ± 18.70