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In recent years, we have witnessed a huge progress in developing new drugs. However, the process of their design is expensive and long. Finding an effective synthetic pathway which can be used to synthesize new drugs plays a crucial role here. Undoubtedly, inhibitors of matrix metalloproteinase are very attractive compounds for drug discovery. According to much excisting evidence, they play a fundamental role in a wide variety of pathologies. The implementation of MMPs into processes critical to angiogenesis, tumor invasion etc., has prompted rapid development of new important agents, namely inhibitors of matrix metalloporteinase. In this thesis, different and effective strategies that can be employed to design potential inhibitors against overexpression of matrix metalloproteinases have been demonstrated. Moreover, strategies that can highlight the strength and drawback of each approach have been investigated. We have synthesied a family of different compounds bearing in their molecule oxalyl, phosphonoformyl and bisphosphonate groups� theoretically capable to chelate to metal ions like zinc, calcium or magnesium. These agents are referred to as a potent zinc binding groups (ZBGs). It should be noted that, the past few decades are testament to the ingenuity of chemistry in designing such chemical entries.