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An appreciable number of compounds in use today as pharmacotherapeutic agents have been laboratory synthesized through the miracle of chemistry. Medicinal chemistry remains a challenging science and with hundreds of thousands of new organic chemicals prepared annually throughout the world and of which, a few enter into pharmacological screens to determine if they have useful biological activity. Changes in the chemical nature of a compound can lead to varied pharmacological actions. This fact can be used to design new derivatives. The primary role of the Medicinal Chemist has become one of improving upon existing drugs by increasing their potency and duration of action and by decreasing toxic side effects, as well as creating new drugs by molecular modification. This is achieved through organic synthesis concomitant with pharmacological testing. The present work describes synthesis of compounds and their structure elucidation based on modern analytical techniques such as 1H NMR and Massspectrometry. The pharmacological screening of these compounds has also been done concomitantly.