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.

Cinnamic Acid Derivatives and Their Biological Efficacy.

Coumarins are naturally occurring molecules with a versatile range of activities. Their structural and physicochemical characteristics make them a privileged scaffold in medicinal chemistry and chemical biology. Many research articles and reviews compile information on this important family of compounds. In this overview, the most recent research papers and reviews from 2020 are organized and analyzed, and a discussion on these data is included. Multiple electronic databases were scanned, including SciFinder, Mendeley, and PubMed, the latter being the main source of information. Particular attention was paid to the potential of coumarins as an important scaffold in drug design, as well as fluorescent probes for decaging of prodrugs, metal detection, and diagnostic purposes. Herein we do an analysis of the trending topics related to coumarin and its derivatives in the broad field of drug discovery.

https://www.mdpi.com/1420-3049/26/2/501/pdf

Plant-microbial interaction: The mechanism and the application of microbial elicitor induced secondary metabolites biosynthesis in medicinal plants.

Utilization of the common functional groups in bioactive molecules: Exploring dual inhibitory potential and computational analysis of keto esters against α-glucosidase and carbonic anhydrase-II enzymes.

Design and synthesis of novel quinazolinone-pyrazole derivatives as potential α-glucosidase inhibitors: Structure-activity relationship, molecular modeling and kinetic study.

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

The invention discloses a coumarin derivative as well as a preparation method and application thereof. The chemical structural formula of the coumarin derivative is represented by a formula (I) or a formula (II), wherein in the formula, R1 is H, CH3, OCH3, F, Cl, Br, CF3 or OH, and R2 is H or OCH3. The coumarin derivative disclosed by the scheme of the invention is stable in structure, has a goodinhibition effect on the activity of an alpha-glucosidase inhibitor, is small in toxic and side effects, and has a good application prospect in the fields of diabetes treatment and prevention and treatment, especially in the preparation of medicines for treating type II diabetes.

Coumarin derivative as well as preparation method and application thereof

The invention discloses an indolone derivative with [alpha]-glucosidase inhibitory activity and a preparation method and application thereof. The indolone derivative has a structure as shown in a formula I, in the formula, R is substituted or unsubstituted aryl or heteroaryl. The indolone derivative can be used for preparing compositions, medicines and health-care products for preventing and/or treating diabetes mellitus. According to the invention, a series of 5-fluoroindolone compounds are designed and synthesized by taking a 5-fluoroindolone structure as a parent nucleus through a chemicalsynthesis method; and meanwhile, the related biological activity and structure-activity relationship are deeply discussed, so that a solid theoretical basis is provided for finding and discovering high-efficiency and low-toxicity [alpha]-glucopyranase inhibitor drug lead compounds.

Indolone derivative with [alpha]-glucosidase inhibitory activity and preparation method and application thereof

The invention discloses an alpha-glucosidase inhibitor and application thereof. The alpha-glucosidase inhibitor comprises a compound with the following structural formula: R1 is independently selectedfrom a hydrogen atom, an alkyl group, an alkoxy group, halogen, a halogenated alkyl group or a hydroxyl group; R1 is located at the ortho-position, meta-position or para-position of a benzene ring. The active component of the inhibitor is a cinnamate-magnolol derivative, and the cinnamate-magnolol derivative has relatively strong alpha-glucosidase inhibition activity which can be about 25-50 times that of acarbose, and the inhibitor can be used for treating or adjunctively treating diabetes mellitus II, and has good potential medical and health-care values.

Deng Xuyang

Papers

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

Coumarin derivative as well as preparation method and application thereof

Indolone derivative with [alpha]-glucosidase inhibitory activity and preparation method and application thereof

Alpha-glucosidase inhibitor and application thereof