Pyridazinone and its derivatives have various ranges of biological and pharmacological activities including anti-inflammatory, antifeedant, anticonvulsant, antidiabetic, herbicidal, antihypertensive, antiplatelet, antifungal, antibacterial, anticancer and antiviral activities. Pyridazinone magic moiety has allowed the generation of a huge number of structurally different derivatives. Most of the pyridazinone derivatives are derived from substitution of the pyridazinone oxygen, nitrogen and C4/C5/C6 carbon positions. Pyridazinone can be used for the synthesis of a large variety of heterocyclic compounds and as intermediate for a broad spectrum of drug synthesis. Constant use of non-steroidal anti-inflammatory drugs is often accompanied by side effects such as bleeding, nephrotoxicity and gastrointestinal lesions. To minimise these side effects some of the pyridazinone derivatives are synthesised with an improved gastrointestinal tract and renal safety profile linked to other non-steroidal anti-inflammatory drugs. In this review, we have discussed the pyridazinone nucleus which serves as an important therapeutic agent in the field of nonsteroidal anti-inflammatory drugs. This nucleus has a wide spectrum in bioorganic and medicinal chemistry and application in drug discovery.
This review encapsulates the recent advances in the synthesis and anticancer activity of Quinoline derivatives.
Among the most common infections of digestive system in human beings are helminth infections. In developing countries, they pose a large threat to the society. Such parasitic diseases cause severe morbidity, including lymphatic filariasis, onchoserciasis and schistosomiasis. Different extracts of the plant material were tested against adult Indian earthworms Pheretima posthuma (Pheritimidae) as test worms. Various concentrations (10, 25 and 50 mg/ml) of all extracts were tested and results were expressed in terms of time for paralysis and time for death of worms. Piperazine citrate (10 mg/ml) was used as the standard reference drug. Results showed that the aqueous extract is more potent as compared to other extracts as it took less time to cause paralysis and death of the earthworms as compared to standard reference drug.
TB is becoming a worldwide problem and it was declared since 1993 by the World Health Organization (WHO), a global health emergency. The current problem of tuberculosis therapy is the emergence of multi-drug resistant (MDR) strains, caused by the improper use of antibiotics in chemotherapy of TB patients. Azatidinones, a β-lactam cyclic amide with four atoms in a ring, has been considered as a magic moiety (wonder nucleus) which possesses almost all types of biological activities. This diversity in the biological response profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. Present article is sincere attempt to review chemistry, method of synthesis of azatidinones and to study azatidinones synthesized in last few years which have shown potent antitubercular activity.
Background: Chemical modification of thiadiazole may lead to a potent therapeutic agent. In this study, biological properties of thiadiazole derivatives were evaluated by assessing their antimicrobial and anti-inflammatory activities. Methods: A series of novel derivatives of N-(5-(1-methyl-indol-3-yl)-1,3,4-thiadiazol-2- yl)-2-(5-substitutedphenyl)-3-(phenylamino)-4,5-dihydropyrazol-1-yl) acetamide have been synthesized and evaluated for their antimicrobial activity. Anti-inflammatory activity was done using carrageenan-induced inflammation in rat paw edema model. In-silico molecular docking studies of the synthesized compounds were performed on crystal structures of Aspergillus niger, Bacillus subtilis, Candida albicans, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Cyclooxygenase-2 (obtained from www.rcsb.org) using GRIP batch docking method of V-life MDS 3.0 software. The structures of the newly synthesized compounds were confirmed by FT-IR, 1H-NMR, 13C-NMR and Mass spectroscopy. Results: Antimicrobial and Anti-inflammatory activity study of the novel synthesized compounds were screened. Synthesized compounds having methoxy substitution on the 3rd and 4th positions of aromatic ring are utmost active amongst all the derivatives. Compounds 6d, 6i, 6j and 6l were found to possess good anti-inflammatory activity having percentage of inhibition to the extent of 46.8%, 48.1%, 49.4%, and 48.5% as compared with Diclofenac. Conclusion: The experimental results were further supported by molecular docking analysis describing the better interaction patterns.
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