Flavonoid Based Development of Synthetic Drugs: Chemistry and Biological Activities

Chemistry & Biodiversity, Год журнала: 2024, Номер unknown

Опубликована: Окт. 28, 2024

Abstract The toxicity associated with synthetic drugs used for treating various diseases is common. This led to a growing interest in searching and incorporating natural functional core structures such as flavonoid their derivatives via chemical modifications overcome the problems enhance biological spectrum. Natural flavonoids are accepted due safety environment owing varieties of activities anti‐Alzheimer, antimicrobial, anticancer, anti‐inflammatory, antidiabetics, antiviral properties. Based on structure, classified into classes flavone, flavanol, flavanone, isoflavone, Anthocyanin, etc. present review focuses potential role ring‐containing derivatives, highlighting ability prevent treat non‐communicable diabetes, Alzheimer's, cancer. pharmacological flavonoid's mainly attributed antioxidant effects against free radicals, reactive oxygen species well act enzymes inhibitors. covers strategies structure activity relationship (SAR), silico studies improve efficacy these compounds. SAR, molecular docking analysis will enable medicinal chemists search further, develop potent newer therapeutic agents.

Язык: Английский

---

Design, Synthesis, and Biological Activity Studies of Myricetin Derivatives Containing a Diisopropanolamine Structure

Journal of Agricultural and Food Chemistry, Год журнала: 2024, Номер 72(45), С. 25034 - 25044

Опубликована: Ноя. 5, 2024

A series of myricetin derivatives containing diisopropanolamine were designed and synthesized. The in vitro inhibitory effects the target compounds on 9 fungal pathogens 3 bacterial also evaluated. A12 had best effect against Xanthomonas oryzae pv. (Xoo), with an EC50 value 4.9 μg/mL, which was better than zinc–thiazole (ZT: = 7.3 μg/mL) thiodiazole–copper (TC: 65.5 μg/mL); A25 Phomopsis sp. (Ps), 17.2 azoxystrobin (Az: 22.3 μg/mL). In vivo inhibition tests performed kiwifruit for rice leaves A12. At 200 curative activity leaf blight 40.7%, that ZT (37.2%) TC (32.9%), protective 44.8%, (39.5%) (34.6%). kiwi soft rot disease 70.1%, Az (62.8%). Preliminary elucidation possible mechanisms action carried out by experiments fluorescence microscopy, scanning electron formation biofilms, density functional theory calculations, so on.

Язык: Английский

---

Antifungal activity of chalcone derivatives containing 1,2,3,4‐tetrahydroquinoline and studies on them as potential SDH inhibitors

Pest Management Science, Год журнала: 2024, Номер unknown

Опубликована: Ноя. 12, 2024

A large number of pathogenic fungi have caused serious damage to the global crop yield, and drug resistance is always a topic that cannot be avoided for traditional fungicides. Therefore, finding efficient, green, low-toxic fungicides our primary task, which brings opportunities development natural product green pesticides.

Язык: Английский

---

Flavonol derivatives containing piperazine and quinoxaline fragments: synthesis and antifungal activity

Molecular Diversity, Год журнала: 2024, Номер unknown

Опубликована: Сен. 3, 2024

Язык: Английский

---

Novel flavonoid derivatives containing benzothiazole as potential antiviral agents: design, synthesis, and biological evaluation

Research Square (Research Square), Год журнала: 2024, Номер unknown

Опубликована: Окт. 7, 2024

A series of flavonol derivatives containing benzothiazole were designed and synthesized. The structures all the compounds characterized by NMR HRMS. results bioactivity assay showed that some target possessed outstanding in vivo antiviral activity against tobacco mosaic virus (TMV). Among them, median effective concentration (EC₅₀) L20 was 90.5 µg/mL for curative activities TMV, which better than ningnanmycin (NNM: 252.0 µg/mL). microcalorimetric thermophoresis (MST) molecular docking experiments had a strong binding ability with TMV-CP; malondialdehyde (MDA) superoxide dismutase (SOD) measurements also fully confirmed stimulated plant immune system strengthened plant's resistance to diseases lowering MDA content increasing SOD activity. In addition, chlorophyll test experiment found could reduce destructive effect viruses on chloroplasts, increase chlorophyll, promote photosynthesis. conclusion, above experimental suggested be further investigated as new drugs.

Язык: Английский

---

Novel Flavonol Derivatives Containing Quinoxaline: Insights into the Antifungal Mechanism against Sclerotinia sclerotiorum

Journal of Agricultural and Food Chemistry, Год журнала: 2024, Номер 72(43), С. 23766 - 23775

Опубликована: Окт. 17, 2024

In this study, 12 pairs of tautomeric flavonol derivatives containing quinoxaline were synthesized. The results antifungal activity showed that in the enol–keto tautomerism, target compounds keto (YB series) had better inhibitory against Sclerotinia sclerotiorum (S.s.) than enol (YA series). YB9 strongest S.s., and median effective concentration (EC50) value was 1.0 μg/mL, which azoxystrobin (Az, 35.3 μg/mL). vivo fungal inhibition experiments protective rape leaves 83.4% at 200 superior to Az (70.2%). succinate dehydrogenase molecular docking a stronger effect YA9. oxalic acid content determination could reduce pathogenic ability S.s. Then, further verified by scanning electron microscopy, fluorescence cell membrane permeability, leakage, malondialdehyde content.

Язык: Английский

---

New chalcone derivatives containing morpholine-thiadiazole: Design, synthesis and evaluation of against tobacco mosaic virus

Fitoterapia, Год журнала: 2024, Номер 179, С. 106272 - 106272

Опубликована: Окт. 22, 2024

Язык: Английский

---

Novel flavonoid derivatives containing 1,2,4-triazole Schiff bases as potential antifungal agents: design, synthesis, and biological evaluation

Bioorganic Chemistry, Год журнала: 2024, Номер 153, С. 107965 - 107965

Опубликована: Ноя. 16, 2024

Язык: Английский

---