Polymer blends along with 1-(4-methylphenyl)-3-(4-N,N, dimethyl amino phenyl)-2-propen-1-one (MPDMAPP) NLO-chromophore-doped composite films were prepared by solvent casting method using DMF. The optical properties were studied using UV-visible, refractive index, steady state fluorescence, and fluorescence microscopic imaging techniques. The UV-vis absorption spectra showed three absorption bands and were assigned to localized n ? p*, n ? p* inter band, and p ? p* transition of charge transfer groups. The observed changes in the absorption peak, edges, and intensity with dopant concentration are understood based on charge transfer complex (CTC) formation. The refractive indices of the composite films varied from 1.4937-1.5398 for red and 1.5165-1.5516 for green light respectively. The steady state fluorescence data showed both emission peak wavelengths and intensity changes with MPDMAPP doping level in blend. The fluorescence anisotropy (r) variations in the composite films indicate the suppressed molecular motion of MPDMAPP in the solid composite film. The fluorescence microscopic image of these composite films showed that the films are photochromatic in nature. These modified properties are thought to be due to the charge transfer upon excitation from the donor to the acceptor connected through benzene ring and CTC formation. POLYM. ENG. SCI.,
A new
class of compounds formed by the linkage of −C(O)–NH–
with pyridine and thiazole moieties was designed, synthesized, and
characterized by various spectral approaches. The newly characterized
compounds were evaluated for their antimicrobial as well as anti-inflammatory
properties. The
in vitro
anti-inflammatory activity
of these compounds was evaluated by denaturation of the bovine serum
albumin method and showed inhibition in the range of IC
50
values—46.29–100.60 μg/mL. Among all the tested
compounds, compound
5l
has the highest IC
50
value and compound
5g
has the least IC
50
value. On the other hand, antimicrobial results revealed that compound
5j
showed the lowest MIC values and compound
5a
has the highest MIC values. Furthermore, molecular docking of the
active compounds demonstrated a better docking score and interacted
well with the target protein. Physicochemical parameters of the titled
compounds were found suitable in the reference range only. The
in silico
molecular docking study revealed their COX-inhibitory
action. Compound
5j
emerged as a significant bioactive
molecule among the synthesized analogues.
The current study
evaluates antidiabetic, anticoagulant, and antiplatelet
activity of novel benzimidazole-containing quinolinyl oxadiazoles.
These derivatives are synthesized and characterized using spectroscopy
(FT-IR, 1H NMR, and mass spectroscopy) and single-crystal
X-ray diffraction methods. The inhibitory effects of these compounds
were evaluated by the α-glucosidase inhibitory assay and shows
the activity in the range of IC50 = 0.66 ± 0.05 to
3.79 ± 0.46 μg/mL. In addition, molecular docking studies
revealed that benzimidazole-containing quinolinyl oxadiazoles can
correctly dock into the target receptor protein of the human intestinal α-glucosidase, while their bioavailability/drug-likeness
was predicted to be acceptable but requires further optimization.
On the other hand, compound 8a and 8d showed
anticoagulant activity as they enhanced the clotting time from control
180–410 and 180–390 s, respectively, in platelet rich
plasma and 230–460 and 230–545 s in platelet poor plasma.
Furthermore, only 8a showed antiplatelet activity by
inhibiting epinephrine-induced platelet aggregation, and the observed
aggregation inhibition was found to be 93.4%. Compounds 8a–f show nontoxic properties because of the non-hydrolyzing properties
in the RBC cells. In addition, 8a and 8d show anti-edema and anti-hemorrhagic properties in the experimental
mice. These findings reveal that benzimidazole-containing quinolinyl
oxadiazoles act as α-glucosidase inhibitors to develop novel
therapeutics for treating type-II diabetes mellitus and can act as
lead molecules in drug discovery as potential antidiabetic and antithrombotic
agents.
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