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Synthesis, antibacterial and free radical scavenging activity of some newer N-((10-nitro-1H-indolo [1, 2-c]quinazolin-12-yl)methylene)benzenamines

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| Nov 18, 2020

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European Pharmaceutical Journal

Volume 67 (2020): Issue 1 (January 2020)

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Article Category: Original Paper

Published Online: Nov 18, 2020

Page range: 7 - 16

Received: Feb 20, 2019

Accepted: Dec 11, 2019

DOI: https://doi.org/10.2478/afpuc-2020-0002

Keywords
free radical scavenger, antibacterial, DPPH, indoloquinazoline, IC

© 2019 Dixit A. et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

*Ar:–Phenyl, 2-Chlorophenyl, 3-Chlorophenyl, 4-Chlorophenyl, 2-Nitrophenyl, 3-Nitrophenyl, 4-Nitrophenyl, 4-Fluorophenyl, 4-Bromophenyl, 2-Chloro-4-nitrophenyl, 4-Chloro-2-nitrophenyl

DPPH free radical scavenging activity of compounds 4b1–4b11

Compounds	% Inhibition at μg/ml^*					IC50 value (μmol/L)
Compounds	10	20	30	40	50	IC50 value (μmol/L)
Ascorbic acid	45.8 ± 1.21	54.01 ± 1.09	61.60 ±0.98	66.89 ± 1.23	78.01 ± 2.31	87.67
4b1	17.26 ± 4.36	20.98 ± 0.43	26.20 ± 0.69	36.84 ± 2.86	41.26 ± 1.50	189.43
4b2	4.01 ± 2.43	14.75 ± 0.79	24.29 ± 1.71	35.24 ± 0.89	37.94 ± 1.67	150.70
4b3	14.75 ± 0.42	19.67 ± 0.91	27.60 ± 0.46	32.92 ± 0.75	36.64 ± 0.45	178.80
4b4	7.42 ± 0.75	15.66 ± 0.30	20.88 ± 0.62	30.82 ± 0.45	35.13 ± 0.75	174.22
4b5	16.06 ± 0.45	21.68 ± 0.30	28.01 ± 0.30	34.93 ± 1.08	45.98 ± 0.75	141.77
4b6	4.31 ± 0.75	13.65 ± 0.62	23.18 ± 1.50	26.70 ± 0.75	32.92 ± 0.62	176.32
4b7	50.19 ± 1.05	54.71 ± 0.45	65.45 ± 0.75	73.49 ± 0.90	76.70± 0.75	25.18
4b8	50.59 ± 1.17	53.61 ± 0.79	57.02 ± 0.62	60.94 ± 0.45	67.66 ± 0.75	28.09
4b9	12.74 ± 1.83	20.57 ± 0.96	28.41 ± 0.75	32.92 ± 0.92	36.04 ± 0.74	158.38
4b10	27.40 ± 0.21	30.41 ± 0.60	33.12 ± 0.79	35.63 ± 0.62	38.75 ± 0.45	203.73
4b11	44.67 ± 0.96	50.00 ± 0.62	56.62 ± 0.82	59.83 ± 0.45	67.46 ± 0.60	44.22

Zone of inhibition values for derivatives (4b1–4b11) at 100 μg/ml and 150 μg/ml

Compounds	Zone of inhibition (mm)
	B. subtilis		E. coli
	100 μg/ml	150 μg/ml	100 μg/ml	150 μg/ml
4b1	2	7	3	5
4b2	2	8	4	9
4b3	4	8	6	10
4b4	5	10	4	9
4b5	3	7	4	9
4b6	6	10	7	10
4b7	6	12	7	12
4b8	5	10	7	13
4b9	13	18	12	17
4b10	12	15	13	17
4b11	6	14	8	14
Ciprofloxacin (25 μg/ml)	20		18

H2O2 free radical scavenging activity of compounds 4b1–4b11

Compounds	% Inhibition at μg/ml^*					IC50 value (μmol/L)
Compounds	10	20	30	40	50	IC50 value (μmol/L)
Ascorbic acid	44.35 ± 1.21	55.32 ± 1.34	62.09 ± 1.51	66.72 ± 1.10	77.02 ± 1.33	88.23
4b1	4.02 ± 0.57	10.18 ± 0.75	18.11 ± 0.75	24.52 ± 0.37	32.32 ± 0.57	224.22
4b2	1.88 ± 0.37	7.67 ± 1.32	16.98 ± 0.37	20.37 ± 0.75	26.03 ± 0.75	220.12
4b3	9.68 ± 0.57	20.25 ± 0.57	24.02 ± 1.32	28.80 ± 0.57	34.08 ± 0.94	191.10
4b4	2.26 ± 0.37	8.55 ± 0.94	15.34 ± 0.78	20.00 ± 0.75	28.17 ± 0.94	213.82
4b5	1.25 ± 0.57	7.92 ± 1.13	12.20 ± 1.15	19.24 ± 0.37	23.52 ± 0.78	234.89
4b6	4.90 ± 0.99	10.06 ± 0.57	19.37 ± 0.57	23.64 ± 0.94	28.17 ± 0.57	205.62
4b7	44.90 ± 0.37	54.08 ± 0.57	60.37 ± 0.37	65.15 ± 0.94	76.10 ± 0.94	39.46
4b8	43.52 ± 0.57	54.00 ± 1.15	59.11 ± 0.57	66.03 ± 0.75	72.83 ± 1.13	44.47
4b9	8.30 ± 0.75	13.96 ± 0.37	20.12 ± 0.57	28.80 ± 0.57	30.81 ± 0.57	178.53
4b10	4.90 ± 0.75	8.30 ± 0.37	13.20 ± 0.37	20.75 ± 0.37	24.90 ± 0.75	219.88
4b11	47.04 ± 0.57	53.58 ± 1.13	57.10 ± 0.57	63.39 ± 0.75	74.08 ± 0.57	35.61

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