Abstract:
:The new chemical entities febuxostat and topiroxostat have been approved by the US Food and Drug Administration, opening new avenues for exploiting different heterocycles other than purines as xanthine oxidase (XO) inhibitors. A different series of substituted 2-benzamido-4-methylthiazole-5-carboxylic acid derivatives (5a-r) was synthesized and characterized by the collective use of IR, 1 H and 13 C NMR, and mass spectroscopy, for the treatment of gout and hyperuricemia. In vitro studies of the synthesized derivatives revealed that the presence of a fluoro group at the para position in 5b (IC50 = 0.57 μm) and a chloro group in 5c (IC50 = 0.91 μm) signifies excellent XO inhibitory activity among the series, along with their DPPH free radial scavenging activity. In vivo serum uric acid inhibition studies established that 5b and 5c displayed 62 and 53% uric acid inhibition, respectively. Studies on enzyme kinetics indicated that 5b acts as a mixed type inhibitor. In silico prediction by various softwares also helped in the recognition of potent XO inhibitors.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Ali MR,Kumar S,Afzal O,Shalmali N,Ali W,Sharma M,Bawa Sdoi
10.1002/ardp.201600313subject
Has Abstractpub_date
2017-02-01 00:00:00issue
2eissn
0365-6233issn
1521-4184journal_volume
350pub_type
杂志文章abstract::A series of 5-(o-tolyl)-1H-tetrazole derivatives were synthesized and evaluated for their anticonvulsant activities. 1-(2-Methylbenzyl)-5-(o-tolyl)-1H-tetrazole (3h) showed important anticonvulsant activity against the MES-induced seizures, as well as lower neurotoxicity with an ED50 value of 12.7 mg/kg and a TD50 val...
journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:10.1002/ardp.19923250205
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journal_title:Archiv der Pharmazie
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abstract::Reaction of K2PtCl4 with the substituted 2-aminomethylpyridines 9, 14, and 22 affords the corresponding dichloroplatinum(II) complexes 3-5. Compounds 3 and 22 show remarkable relative binding affinities for the estrogen receptor. Towards the hormone-independent P388-tumor of the CD2F1-mouse the platinum(II) complexes ...
journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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更新日期:2017-09-01 00:00:00