Coumarin: A Privileged Scaffold for the Design and Development of Antineurodegenerative Agents

Abstract

Drug development for neurodegenerative diseases (NDs) is foremost task for the medicinal chemists in the 21st century. Coumarins are exemplary of an assorted and aptitudinally useful set of drugs. Coumarins play a momentous role in several pharmacological and medicinal aspects. Its analogues are anticipated to play a significant role in the development of new therapeutic leads for NDs. Their promising applications in the field of ND medication are exemplified by clinical candidates such as nodakenin that have been potent for demoting memory impairment. Apart from ND, clinically used anticoagulant warfarin, anticoagulant dicoumarol, and antibiotic coumermycin, novobiocin and chartesium grab the interest of researchers in coumarins. It would be worthwhile to look at the different biological processes that could cause neurodegeneration, thereby establishing a link with distinct coumarin derivatives to serve the purpose of medication. This review undertakes estimation of the wide spectrum of studies focusing coumarin to the domain of drug research for ND. Herein, we search for multitarget coumarin‐based inhibitors and their scope for NDs. Future challenges in coumarin‐based drug development have been discussed, and emphases have been laid on the future perspectives of coumarins as possible drugs in the future for the treatment of NDs.

Synthesis and Antiretroviral Activity of 6-Acetyl-coumarin Derivatives against HIV-1 Infection

“…One of the active natural products, coumarin, has attracted attention in recent years due to its diverse pharmacological properties [3][4][5][6][7][8] . Coumarins are highly variable in structure due to possibility of various types of substitutions in its ring skeleton, which influence a variety of pharmacological actions [9][10][11][12][13][14][15] . Various reports showed the antiretroviral potency of coumarins via inhibition of retroviral enzymes i.e.…”

Twelve‐membered macrolactones: privileged scaffolds for the development of new therapeutics

“…Furthermore, examination of the libraries of natural products that have been isolated and characterized reveals the presence of ‘privileged scaffolds’ contained within these molecules (Figure ). The term ‘privileged scaffold’ was coined by Evans in 1988, and prominent examples include the β ‐lactams (the most highly represented scaffold in the clinic), tetracyclines, macrolides, coumarins, and glycopeptides . These scaffolds tend to impart highly favorable characteristics, while alterations to the secondary structure lead to high levels of potency and specificity.…”

Pyrimidine‐Triazolopyrimidine and Pyrimidine‐Pyridine Hybrids as Potential Acetylcholinesterase Inhibitors for Alzheimer's Disease

“… Examples of known AChE inhibitors: Donepezil as indanone derivative, Ensaculin and AP2238 as coumarin derivatives …”

“…Examples of known AChE inhibitors: Donepezil as indanone derivative, Ensaculin and AP2238 as coumarin derivatives. [21] Full Papers DOI: 10.1002/slct.201702599 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 signal transmission. [7] ACh is fractioned into acetyl and choline within synaptic cleft with a turnover number greater than 10 4 s À1 .…”