Evaluation of some novel heterocyclic compounds for antifertility, antiinflammatory and analgesic activities

2003 
Some novel heterocyclic compounds have been evaluated for antifertility activity in Wistar rats. Compounds 3 and 4 showed 66.3% and 83.4% antiimplantation potency when compared with control. Compounds 1, 2 and 5-10 did not exhibit any antiimplantation activity. Uterine weight was increased significantly with compounds 3 and 4 when compared to control. Histological studies indicated the increase in the diameter, thickness of endometrium and height of the endometrial epithelium of the uterus revealing estrogenic activity of compounds 3 and 4. The estrogenic activity was significant when compared to control. Compounds have been evaluated for antiinflammatory activity using carrageenan-induced rat paw oedema model. Phenylbutazone (100 mg/ kg), was used as the standard. Compounds 1, 2 and 3 exhibited significant antiinflammatory activity at the dose of 15 mglkg, whereas compounds 5, 6 and 7 showed significant antiinflammatory activity at the dose of 30 mglkg. Compounds 1, 2 and 4-7 exhibited 58.9%, 58.1%, 66.2%, 64.5%, 63.0% and 63.0% inhibition respectively in carrageenan-induced rat paw oedema, while the standard showed an inhibition of 63.8%. Compound 4 exhibited maximum antiinflammatory activity. Analgesic activity of the compounds 1 to 4 was evaluated using acetic acid-induced writhing model at 15 mg/kg. Acetyl salicylic acid (150 mglkg) was used as a standard. Compounds 2 and 4 showed significant analgesic activity of 67.2% and 66.1% maximum possible effect respectively, when compared to standard acetylsalicylic acid which exhibited 74.9% maximum possible effect.
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