Abstract:
:Fifteen novel pyridazinone substituted benzenesulfonylurea derivatives (3a-o) were synthesized from corresponding sulfonamides derivatives via novel carbamates (2a-e). These were characterized by elemental analysis and various spectroscopic methods viz. IR, (1)H NMR, (13)C NMR and MS. Blood sugar lowering effect of thirteen (3a-c, 3e, 3g-o) sulfonylurea derivatives at the dose of 20 mg/kg (p.o.) were assessed using glucose tolerance test in normal and NIDDM (n2-STZ) rat models. All compounds except 3c, 3e and 3o almost completely prevented the rise of blood glucose of NIDDM rats as compared with NIDDM control. While compounds 3c and 3o showed more than 50% prevention in the rise of blood glucose levels. In glucose-fed normal rats these compounds at the same dose except 3e significantly prevented the rise of blood glucose (more than 50%) when compared with control of glucose-fed normal rats. From the results, novel compounds (3a-c, 3g-n) exhibited considerably potent blood glucose lowering activity and may be used as lead compounds for developing new antidiabetic drugs. Some structure-activity relationship was observed while varying nature of 'Ar' and 'R'.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Rathish IG,Javed K,Bano S,Ahmad S,Alam MS,Pillai KKdoi
10.1016/j.ejmech.2008.12.013subject
Has Abstractpub_date
2009-06-01 00:00:00pages
2673-8issue
6eissn
0223-5234issn
1768-3254pii
S0223-5234(08)00597-7journal_volume
44pub_type
杂志文章abstract::A series of 3-arylidene-5-(4-chloro-phenyl)-2(3H)-furanones (2-13) and their nitrogen analogues 1-benzylpyrrolones (14-18) were synthesized. The compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation actions. Some of the newly synthesized compounds showed good anti-inflamma...
journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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