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Synthesis of Novel Benzimidazole Analogs for Neurodegenerative Diseases by Targeting Prolyl Oligopeptidase
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Abstract
A novel series of benzimidazole hydrazone‐Schiff bases have been prepared through multi‐step reaction process and structurally confirmed by
13
C‐,
1
H‐NMR and HR‐MS (ESI) spectroscopic techniques and evaluated against prolyl oligopeptidase (POP) inhibitory activity. In the series, eleven derivatives
20
,
14 15
,
19
,
10
,
9
,
11
,
4
,
5
,
18
, and
21
revealed excellent inhibition potential having IC
50
values from (IC
50
=1.44±0.08 μM) to (IC
50
=5.66±0.48 μM). However, six out of twenty compounds
12, 16, 13, 17, 22
, and
3
attributed significant activity while, three compounds were found good active in the range of IC
50
values 10.43±0.57 to 11.45±0.63 μM. The docking studies indicates that the hydrazone moiety show an imperative part in binding with one of the catalytic residues (Arg643) in the substrate binding region of POP enzyme. The excellent inhibitions of these compounds for POP enzyme may lead them to be a good candidates for drug against neurodegenerative diseases.
Title: Synthesis of Novel Benzimidazole Analogs for Neurodegenerative Diseases by Targeting Prolyl Oligopeptidase
Description:
Abstract
A novel series of benzimidazole hydrazone‐Schiff bases have been prepared through multi‐step reaction process and structurally confirmed by
13
C‐,
1
H‐NMR and HR‐MS (ESI) spectroscopic techniques and evaluated against prolyl oligopeptidase (POP) inhibitory activity.
In the series, eleven derivatives
20
,
14 15
,
19
,
10
,
9
,
11
,
4
,
5
,
18
, and
21
revealed excellent inhibition potential having IC
50
values from (IC
50
=1.
44±0.
08 μM) to (IC
50
=5.
66±0.
48 μM).
However, six out of twenty compounds
12, 16, 13, 17, 22
, and
3
attributed significant activity while, three compounds were found good active in the range of IC
50
values 10.
43±0.
57 to 11.
45±0.
63 μM.
The docking studies indicates that the hydrazone moiety show an imperative part in binding with one of the catalytic residues (Arg643) in the substrate binding region of POP enzyme.
The excellent inhibitions of these compounds for POP enzyme may lead them to be a good candidates for drug against neurodegenerative diseases.
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