Two new binuclear O-bridged copper(II) carboxylates with chemical formulas [Cu 2 (3-ClC 6 H 4 CH 2 COO) 4 (phen) 2 ] (1) and [Cu 2 (3-ClC 6 H 4 CH 2 COO) 4 (bipy) 2 ] (2) where phen = 1,10-phenanthroline and bipy = 2,2'-bipyridine have been synthesized and characterized by FT-IR, UV-Visible spectroscopy, CHN analysis and single crystal XRD. The results revealed distorted square pyramidal geometry around each copper atom of 1 and 2. The DNA interaction studies showed strong binding with K b = 5.07 × 10 3 and 4.62 × 10 3 M -1 for 1 and 2, respectively. Both complexes showed strong enzyme inhibition, i.e., 70% and 90% for α-glucosidase with IC 50 = 34.6 and 30.1 μM for 1 and 2, respectively, where acarbose was employed as control. However, both the complexes were found inactive against α-amylase. Using galantamine hydrobromide as control, 1 showed moderate inhibition activity (47%) with IC 50 = 179.4 μM for acetylcholine esterase whereas 2 showed strong inhibition activity (76%) with IC 50 = 95.8 μM for butyrylcholine esterase. The data reflects active anti-diabetic and anti-Alzheimer's nature of the synthesized complexes.
This research reports
the synthesis of new benzimidazole-derived
N
-acylhydrazones
(NAH), their characterization using various
spectroscopic methods, and in vitro evaluation as potent carbonic
anhydrase-II inhibitors. Among the target compounds (
9–29
), few showed higher inhibition than the standard acetazolamide (IC
50
: 18.6 ± 0.43 μM), for example, compound
9
(IC
50
: 13.3 ± 1.25 μM),
10
(IC
50
: 17.2 ± 1.24 μM),
12
(IC
50
: 14.6 ± 0.62 μM), and
15
(IC
50
: 14.5 ± 1.05 μM). Molecular docking was performed
on the most active compounds, which revealed their binding interactions
with the active site of the enzyme, thus supporting the experimental
findings.
A novel series of multifunctional benzimidazoles has been reported as potent inhibitors of α-glucosidase. The procedure relies on the synthesis of 5-amino-1H-benzo[d]imidazole-2-thiol 5 via the multistep reaction through 2-nitroaniline 1, benzene-1,2-diamine 2, 1H-benzo[d]imidazole-2-thiol 3, and 5-nitro-1H-benzo[d]imidazole-2-thiol 4. Further treatment of 5 with aromatic aldehydes 6a−m provided access to the target 5-(arylideneamino)-1H-benzo[d]imidazole-2-thiols 7a−m.The results of the bioactivity assessment revealed all the compounds as excellent inhibitors of the enzyme (IC 50 range: 0.64 ± 0.05 μM to 343.10 ± 1.62 μM) than acarbose (873.34 ± 1.21). Among them, 7i was the most active inhibitor (IC 50 : 0.64 ± 0.05 μM) followed by 7d
The phytochemical screening of the crude methanolic stem extracts of
Cassia javanica
plant showed the presence of different classes of organic compounds like alkaloids, tannins, flavonoids, saponins, phlobatanins, steroids, anthraquinone and cardiac glycoside. The starching frequencies of these functional groups were determined from FT-IR spectroscopic data. The crude and their fractions were examined for antibacterial potential against
Klebsiella pneumoniae
and
Proteus mirabilis
. The antibacterial assay showed maximum zone of inhibition for ethyl acetate fraction, i.e. 20 mm against
Proteus mirabilis
and 18 mm against
Klebsiella pneumoniae
in the comparison with Levofloxacin used as standard (40 mm). Meanwhile for methanolic crude extract, the inhibition zone was recorded 14 mm against
Klebsiella pneumoniae
and 22 mm against
Proteus mirabilis
. The minimum inhibitory concentrations and minimum bactericidal concentrations were recorded as 187.5 µg ml
−1
against
Proteus mirabilis
and 93.75 µg ml
−1
against
Klebsiella pneumoniae.
The scavenging free radical assay was noted as 69.61% at the concentration of 100 ppm.
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