Synthesis and biological evaluation of coumarin derivatives as α-glucosidase inhibitors

Xu, Xuetao; Deng, Xu-Yang; Chen, Jie; Liang, Qi-Ming; Zhang, Kun; Li, Dongli; Wu, Panpan; Zheng, Xi; Zhou, Ran; Jiang, Zhengyun; Ma, Ai‐Jun; Chen, Wenhua; Wang, Shaohua

doi:10.1016/j.ejmech.2019.112013

Cited by 74 publications

(42 citation statements)

References 50 publications

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“…The two most potent compounds, 97a and 97b, showed that their α-glucosidase inhibition was reversible. Compound 97b fitted well into the active site of α-glucosidase forming a hydrogen bond with the LYS293 amino acid sequences [69]. Since compounds 97a-i were better inhibitors (Table 15) than 98a-i, it showed that conjugating cinnamic acid with 4-hydroxycoumarin was better than with 7-hydroxycoumarin.…”

Section: •-mentioning

confidence: 96%

“…All the compounds displayed LC 50 values higher than ivermectin. The cinnamic acid esters (67)(68)(69)(70), the type of alkyl group, the length of the chain and the degree of branching greatly affected their biological activity. The compounds with potent biological activity were compound 68, 71, 73 and 74.…”

Section: Cinnamic Acid Derivatives With Antiparasitic Activitymentioning

confidence: 99%

“…Xu et al evaluated the activity of coumarin derivatives (97a-i and 98a-i) ( Figure 26) as αglucosidase inhibitors with both the 97 series and the 98 series derivatives having the same substituents. Compounds 98a-i were less potent with 98b having the highest inhibition of 54.745 at 100 µM and IC50 of 94.52 µM, the rest had inhibition less than 50% and IC50 ˃100 µM [69]. Xu et al evaluated the activity of coumarin derivatives (97a-i and 98a-i) ( Figure 26) as α-glucosidase inhibitors with both the 97 series and the 98 series derivatives having the same substituents.…”

Section: •-mentioning

confidence: 99%

“…Xu et al evaluated the activity of coumarin derivatives ( 97a–i and 98a–i ) ( Figure 26 ) as α-glucosidase inhibitors with both the 97 series and the 98 series derivatives having the same substituents. Compounds 98a–i were less potent with 98b having the highest inhibition of 54.745 at 100 µM and IC 50 of 94.52 µM, the rest had inhibition less than 50% and IC 50 ˃100 µM [ 69 ].…”

Section: Cinnamic Derivatives With Antidiabetic Activitymentioning

confidence: 99%

Section: Cinnamic Derivatives With Antidiabetic Activitymentioning

confidence: 99%

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Cinnamic Acid Derivatives and Their Biological Efficacy

Ruwizhi

Aderibigbe

2020

IJMS

211

134

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The role played by cinnamic acid derivatives in treating cancer, bacterial infections, diabetes and neurological disorders, among many, has been reported. Cinnamic acid is obtained from cinnamon bark. Its structure is composed of a benzene ring, an alkene double bond and an acrylic acid functional group making it possible to modify the aforementioned functionalities with a variety of compounds resulting in bioactive agents with enhanced efficacy. The nature of the substituents incorporated into cinnamic acid has been found to play a huge role in either enhancing or decreasing the biological efficacy of the synthesized cinnamic acid derivatives. Some of the derivatives have been reported to be more effective when compared to the standard drugs used to treat chronic or infectious diseases in vitro, thus making them very promising therapeutic agents. Compound 20 displayed potent anti-TB activity, compound 27 exhibited significant antibacterial activity on S. aureus strain of bacteria and compounds with potent antimalarial activity are 35a, 35g, 35i, 36i, and 36b. Furthermore, compounds 43d, 44o, 55g–55p, 59e, 59g displayed potent anticancer activity and compounds 86f–h were active against both hAChE and hBuChE. This review will expound on the recent advances on cinnamic acid derivatives and their biological efficacy.

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Section: •-mentioning

confidence: 96%

Section: Cinnamic Acid Derivatives With Antiparasitic Activitymentioning

confidence: 99%

Section: •-mentioning

confidence: 99%

Section: Cinnamic Derivatives With Antidiabetic Activitymentioning

confidence: 99%

Section: Cinnamic Derivatives With Antidiabetic Activitymentioning

confidence: 99%

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Cinnamic Acid Derivatives and Their Biological Efficacy

Ruwizhi

Aderibigbe

2020

IJMS

211

134

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Synthesis and anticancer activities of some new coumarin derivatives including the triazole ring and their in silico molecular docking studies

Menteşe

Güner

Polatlı

et al. 2020

Archiv der Pharmazie

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The synthesis, docking study, and investigation of the anticancer activities of some coumarin derivatives containing the triazole ring are reported in this study. The newly synthesized compounds were screened for their in vitro anticancer activity against the cell lines CRL5807 (human bronchioalveolar carcinoma), CRL5826 (human squamous cell carcinoma), MDA‐MB231 (human breast cancer cells), HTB177 (human lung cancer), PC‐3 (human prostate adenocarcinoma), PANC‐1 (human pancreatic cancer cells), used as cancer cells, and CCD34Lu (normal human lung fibroblasts), used as a healthy cell line. Cytotoxicity effects of the samples were determined by the MTT (3‐(4,5‐dimethyl‐2‐thiazolyl)‐2,5‐diphenyl‐2H‐tetrazolium bromide) assay. In silico studies were also performed to explore the binding interactions of the molecules.

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Pharmacological report of recently designed multifunctional coumarin and coumarin–heterocycle derivatives

Dorababu

2021

Archiv der Pharmazie

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Coumarin is a naturally available molecule and has been identified as a potent pharmacophore due to its pharmacological activity. Because of this, coumarin has been exploited synthetically to prepare a wide range of derivatives. In fact, most coumarin derivatives have been found to be less toxic, which is the most essential property for a drug molecule. Such molecules are being prepared for therapeutic use as broad‐spectrum pharmacological agents. Microbial diseases including viral diseases have become very common and are responsible for many deaths worldwide. In particular, microbial drug resistance is a problem that needs to be tackled in an effective manner. Also, for Alzheimer's disease, which affects most elderly persons, no efficient chemotherapy exists. In addition, although diabetes, a metabolic syndrome, can be treated with many drugs, there is no complete cure. Thus, more potent antidiabetic agents are required for the management of diabetes. Likewise, for the treatment of a wide range of ailments caused by microbes, genetic factors, or lifestyle‐related factors, an efficient drug regimen is needed. In view of this, coumarin derivatives are designed and evaluated. Here, coumarin derivatives that have been reported recently are compiled, classified and evaluated critically. This study briefly takes the structure–activity relationship into consideration and suggests the next suitable step. With a focus on the most potent molecules, the pharmacological activity of the evaluated molecules is described.

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Synthesis and biological evaluation of coumarin derivatives as α-glucosidase inhibitors

Cited by 74 publications

References 50 publications

Cinnamic Acid Derivatives and Their Biological Efficacy

Cinnamic Acid Derivatives and Their Biological Efficacy

Synthesis and anticancer activities of some new coumarin derivatives including the triazole ring and their in silico molecular docking studies

Pharmacological report of recently designed multifunctional coumarin and coumarin–heterocycle derivatives

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