ABSTRACT
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3.1 INTRODUCTION
Drug discovery, in most cases, relates to an efficient, insightful interpretation of biochemical knowledge and logical application to pharmacological activities. Traditionally, the drug discovery process has relied on screening a large number of chemical and biological specimens to identify potential candidates. Many years ago, crude substances were initially extracted from plants. Plant derivatives were modified to become the active compounds found in aspirin, reserpine, and taxol. Large quantities of the plant material were collected and purified to yield the active component, known as a “lead compound.” Chemists then attempted to modify the lead compound to make it more pharmacologically active, reduce potential toxicity, or change its hydrophobicity so it could easily pass through cell membranes — all properties that rendered the compound more effective as a pharmaceutical agent. Purification of crude substances was gradually replaced by large-scale systemic screening of natural and synthetic compounds. Today, more thorough and efficient knowledge-based strategies are utilized to identify new compounds. Structure-based drug design using computer modeling is also used to simulate chemical modifications. In this way, modification of an existing leading drug or designing a new drug is achieved without physically manipulating every possible compound.
