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Patent developments via Schiff bases in medicinal chemistry

机译:Patent developments via Schiff bases in medicinal chemistry

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Schiff bases can be readily synthesized by simple condensing carbonyl compounds (i.e., aldehyde or ketone) with primary amines. They have an azomethine (-C = N-) linkage that joins two or more aromatic or heterocyclic skeletons to create diverse molecular skeletons with fascinating biological properties. Schiff bases are flexible and adaptable compounds that coordinate all metals to synthesize stable metal complexes with various medicinal uses 1. As reflected in the literature, Schiff bases are a diverse group of molecules with myriad therapeutic applications. Moreover, there is an increasing number of Schiff base drugs in the market. Herein, the development of patents relating to Schiff bases in a pharmaceutical context from 2015 to date is reported and discussed.The Schiff base 1-(2-chloro-1H-indol-3-yl)-N-(4-phenyl-1,3-thiazol-2-yl)methanimine has been patented by Puranik et al. as an anti-inflammatory medication. The compound was tested in vivo for anti-inflammatory activity in the paw edema model in Wistar albino rats. The drug was administered orally and inhibited the edema by 84.21 over 12 h, whereas the standard ibuprofen presented 82.1 edema inhibition at a comparable dosage (30 mg/kg). The Schiff base was demonstrated to be faster acting than the standard, with 22.64 inhibition in the first and 53.62 in the second h, as compared with 16.98 and 37.68 by the standard in the first and second h after dosing, respectively. Even at a lesser dose of 20 mg/kg, the edema was inhibited by the Schiff base drug 44.92 over 2 h 2.

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