Medicinal Chemistry - Volume 19, Issue 7, 2023

Despite major antimicrobial therapeutic advancements, widespread use and misuse of antimicrobial drugs have increased antimicrobial drug resistance, posing a severe danger to public health. In particular, the emergence of multidrug-resistant bacteria has provided considerable difficulty in the treatment of pathogenic infections. As a result, the creation of novel drugs to treat resistant bacteria is one of the most significant Read More

Background: Preclinical studies suggest that senolytic compounds such as quercetin (a natural product) and dasatinib (a synthetic product) decrease senescent cells, reduce inflammation, and alleviate human frailty. This evidence has opened a new field of research for studying the effect of these compounds on age-related dysfunction and diseases. Objective: The present study performed in silico and we identified n Read More

Background: Chalcones are precursors of flavonoids and exhibit a broad spectrum of pharmacological activity. Objective: As anti-inflammatory agents, two series of chalcone derivatives and chalcone-based oximes were synthesized and characterized. To integrate the tetramethylpyrazine moiety into these novel molecules, the multifunctional natural chemical ligustrazine was employed. Methods: A variety of newly synthesi Read More

Introduction: Based on bioactive group splicing, classical bioisosterism, and the rule of alkene insertion, forty-eight aurone, and indanone derivatives were designed and synthesized. They were evaluated for inhibitory activity against C. albicans, E. coli, and S. aureus. Among them, thirty compounds exhibited moderate to excellent antibacterial activity. Methods: The maximum circle of inhibition was 18 mm (compou Read More

Background: Hyperuricemia is closely related to the occurrence of gout, hypertension, diabetes, hyperlipidemia, cardiovascular disease, kidney disease, metabolic syndrome, etc. However, xanthine oxidase inhibitors (XOIs) can fundamentally solve the problem of excessive uric acid. Compared to single-target drugs, multi-target drugs are not prone to adverse reactions and exert a synergistic effect. Therefore, the dis Read More