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Effect of compound 26 (100 mg kg −1 d −1 ) and At (10 mg kg −1 d −1 ) on hepatic HMG-CoA reductase activity of HFD-fed hyperlipidemic rats. Values are expressed as the mean ± S.D. of six animals per group. *P < 0.05; ***P < 0.001 vs. ND + vehicle and ## P < 0.01 vs. HFD + vehicle groups.
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In this study, a series of coumarin-indole hybrids have been synthesized and evaluated for their lipid lowering activity. Preliminary biological screening of the synthesized compounds was undertaken in an in vitro model of the HMG-CoA reductase enzyme, and the activity was confirmed in Triton WR-1339 induced hyperlipidemic rats. Among the hybrids,...
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... HMG-CoA reductase activity was measured by the HMG CoA-mevalonate ratio in order to determine whether the decrease in cholesterol levels was due to the suppression of HMG-CoA reductase activity. As expected, feeding of HFD significantly increased the activity of HMG-CoA reductase (Fig. 4) in HFD-fed hyperlipidemic rats. However, treatment with compound 26 and atorvastatin significantly reduced the enzymatic activity in HFD-fed hyperlipidemic rats (Fig. ...
Context 2
... the decrease in cholesterol levels was due to the suppression of HMG-CoA reductase activity. As expected, feeding of HFD significantly increased the activity of HMG-CoA reductase (Fig. 4) in HFD-fed hyperlipidemic rats. However, treatment with compound 26 and atorvastatin significantly reduced the enzymatic activity in HFD-fed hyperlipidemic rats (Fig. ...
Citations
... Also, a series of coumarin-indole hybrids have been synthesized and evaluated in an in vitro model of the HMG-CoA reductase enzyme. Among the hybrids, compound 73 ( Figure 22) proved to be the best, as it significantly reduced the serum and hepatic lipid profiles in an HFD-fed hyperlipidemic rat model, being the mechanism of action associated with the regulation of HMG-CoA reductase activity in the liver [159]. P-glycoprotein is an important protein of the cell membrane that pumps many foreign substances out of cells. ...
3-Phenylcoumarins are a family of heterocyclic molecules that are widely used in both organic and medicinal chemistry. In this overview, research on this scaffold, since 2010, is included and discussed, focusing on aspects related to its natural origin, synthetic procedures and pharmacological applications. This review paper is based on the most relevant literature related to the role of 3-phenylcoumarins in the design of new drug candidates. The references presented in this review have been collected from multiple electronic databases, including SciFinder, Pubmed and Mendeley.
Indole is a heterocyclic compound formed by the fusion of a benzene ring and pyrrole ring, which has rich biological activity. Many indole-containing compounds have been sold on the market due to their excellent pharmacological activity. For example, vincristine and reserpine have been widely used in clinical practice. The diverse structures and biological activities of natural products provide abundant resources for the development of new drugs. Therefore, this review classifies natural products by structure, and summarizes the research progress of indole-containing natural product derivatives, their biological activities, structure-activity relationship and research mechanism which has been studied in the past 13 years, so as to provide a basis for the development of new drug development.
A convenient palladium-catalyzed domino cyclization reaction for the construction of bis(benzofuranyl)methane scaffolds bearing an all-carbon quaternary center has been described. In the cascade process, one C(sp²)−O bond, two C(sp²)−C(sp³) bonds as well as two benzofuran rings are formed in a single synthetic sequence. The approach shows wide scope of substrates and good functional-group tolerance. Moreover, this methodology is successfully extended to the synthesis of benzofuranyl methyl chromane derivatives.
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A highly efficient synthesis of unsymmetrical 3,3’-diindolylmethanes bearing various substituents has been developed by palladium-catalyzed cascade Heck/cyclization reaction. In this transformation, precursors allenamides and o-ethynylanilines were utilized to generate in situ indole skeletons. Modification of the methylene unit of diindolylmethane was achieved by treatment with oxidant and silyl nucleophiles. The methodology allows formation of one C−N bond, two C−C bonds and two new rings in one-pot.
We have described the synthesis of novel triazole incorporated diindolylmethanes (DIMs) using molecular hybridization approach and their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) both in active and dormant state. Among all the synthesized conjugates, the compounds 6b, 6f, 6l, 6n, 6q, 6r and 6s displayed good antitubercular activity against both active and dormant Mtb H37Ra strain. The compound 6l exhibited good antitubercular activity against Mtb H37Ra dormant with IC50 value 1 μg/mL and IC90 (MIC) value 3 μg/mL. The compounds 6b, 6l and 6r displayed good antitubercular activity against Mtb H37Ra active with IC50 values 2.19, 1.52 and 0.22 µg/mL respectively. The compounds 6b, 6h, 6l, and 6s displayed more than 70% inhibition towards B. subtilus strain against Gram-positive bacteria at 3µg/mL. The molecular docking study shows the binding modes of the titled compounds in active site of DprE1 enzyme and was helped to launch a structural basis for the inhibition of Mycobacteria.
