Synthesis of some novel oxadiazole and oxadiazoline analogues for their antiinflammatory activity.

نویسندگان

  • Harish Rajak
  • Murli Dhar Kharya
  • Pradeep Mishra
چکیده

The search for newer non-steroidal antiinflammatory drugs (NSAIDs) and the importance of oxadiazoles as antiinflammatory agents prompted us to undertake the synthesis of some novel oxadiazole and related analogues with unreported antiinflammatory activities. The antiinflammatory potential of the compounds was investigated using the carrageenan-induced rat paw edema method and cotton pellet-induced granuloma method. Some compounds demonstrated marked antiinflammatory activities. The antiinflammatory activity of oxadiazoles at doses of 100 mg/kg was shown by their ability to provide 28-55%, 21-36%, and 27-49% protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. On the other hand, the antiinflammatory properties of oxadiazolines at doses of 100 mg/kg was reflected by their ability to provide 15-47%, 22-39%, and 23-47% protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. Structure-activity relationships among synthesized compounds were also studied.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis, Antinociceptive, Antiinflammatory and Antiepileptic Evaluation of Some Novel Indeno[1, 2-b] Quinoxalin-11-ylidenamines

       A series of novel indeno[1, 2-b]quinoxalin-11-ylidenamines 2-9 have been synthesized via condensation of indane[1, 2-b]quinoxalin-11-one (1) with various primary aromatic amines in presence of AcOH for 3 h. Compound 1 was synthesized by condensation of indane-1,2,3-trione with benzene-1,2-diamine in presence of AcOH. The synthesized compounds were characterized by IR, 1H-NMR, ...

متن کامل

Synthesis, Characterization and Anti-Inflammatory Activity of Some 1, 3,4 -Oxadiazole Derivatives

A series of five-membered heterocyclic rings were synthesized by the reaction between benzoyl chloride and various chlolro-nitro-benzoyl chlorides and semi carbazide to form (C1-C7) compounds and was tested for their anti-inflammatory activity determined by rat-paw-oedema method. All the synthesis compounds have been characterized by 1HNMR, IR and Mass spectral data. The compounds were purified...

متن کامل

Synthesis, Characterization and Anti-Inflammatory Activity of Some 1, 3,4 -Oxadiazole Derivatives

A series of five-membered heterocyclic rings were synthesized by the reaction between benzoyl chloride and various chlolro-nitro-benzoyl chlorides and semi carbazide to form (C1-C7) compounds and was tested for their anti-inflammatory activity determined by rat-paw-oedema method. All the synthesis compounds have been characterized by 1HNMR, IR and Mass spectral data. The compounds were purified...

متن کامل

Synthesis of some 1,3,4-oxadiazole derivatives as potential anti-inflammatory agents

The synthesis of some new 1,3,4-oxadiazole derivatives and 1,2,4-triazine-5-one has been described. IR, H NMR and mass spectral data support the structures of newly synthesized compounds. All the compounds have been tested in vivo for their anti-inflammatory activity by carrageenin-induced rat paw edema method. The compounds, which show good antiinflammatory activity, have been screened for the...

متن کامل

Synthesis, Biological Evaluation and Docking Analysis of Some Novel Quinazolin Derivatives as Antitumor Agents

Different acid chlorides (2a-d) reacted with anthranilic acid to produce 2-substituted-3, 1-benzoxazin-4-one (3a-d) which was used as starting material to synthesize some condensed and non-condensed heterocyclic compounds by reaction with nitrogen nucleophiles e.g., hydrazine hydrate, and formamide. Some of the newly synthesized analogues were chosen to evaluate their cytotoxic activity against...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan

دوره 127 10  شماره 

صفحات  -

تاریخ انتشار 2007