Anees A Siddiqui

2-Pyrazoline derivatives are synthesized by diverse reaction schemes and display a broad spectrum of potential pharmacological activities. The derivatives are present in numerous pharmacologically active molecules such as azolid/ tandearil (anti-inflammatory), phenazone/ amidopyrene/ methampyrone (analgesic and antipyretic), anturane (uricosuric) and indoxacarb (insecticide). New therapeutic agents having improved potency and lesser toxicity are developed by changing in their structure, and it has offered a high degree of diversity that has proven useful for the new drug development. The aim of the present research was thus focused on 2-pyrazoline-1-carboxamide derivatives. The 2-pyrazoline-1-carboxamide derivatives were synthesized by convenient, economical methods in less reaction time and with better yield of products with high level of purity. The compounds numbered 4d-4e, 4j-4k, and 4m-4t were most protective against MES even at 30 mg/kg dose levels. The synthesized compounds were showing minimal neurotoxicity. Thus, it is concluded that all the tested compounds are protective against MES at 100-300 mg/kg dose levels and show promising anticonvulsant activity.

The chance of discovering a new drug is 1 in 10,000 and development costs about 40 million dollars per new drug. This gives the emphasis on the development of new scientific approaches in the discovery of new drugs, "Drug design". It involves the study of the effects of biologically active compounds on the basis of molecular interactions in terms of molecular structure or its physiochemical properties. The current trend in drug design is to develop new clinically effective agents through the structural modification of the lead nucleus which is a prototype compound that has the desired pharmacological activity but may have many undesirable characteristics. The identification of such lead compounds and optimum bioactive position on the basic skeleton is the area of drug design.