期刊
MINI-REVIEWS IN MEDICINAL CHEMISTRY
卷 16, 期 12, 页码 996-1012出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389557516666160611015815
关键词
Anti-inflammatory; Cyclooxygenase inhibitors; Inflammation; Pyridazinone
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.
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