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I. Introduction 703 II. Materials and Methods 706 III. Results and Discussion 707 A. QSAR of COX-

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It also causes sympathetic activation and aldosterone secretion from adrenal glands. All of these actions contribute to the development of hypertension. [17][18][19] Interruption of the RAS has been shown to be an effective means for controlling hypertension in humans as evidenced by the commercially successful ACE inhibitors 20 Captopril 21 and Enalpril. 22 The antihypertensive action of these drugs is due to the decrease in plasma concentration of Ang II. However, angiotensin is not the only biologically important substrate for this enzyme. Studies of Erodes 23 and others have clearly demonstrated that ACE is identi-cal to kinase II, one of the important enzymes involved in the inactivation of bradykinin (an inflammatory peptide), the final mediator of the kallikreinkinin system (Figure 1). Hence, more of the major side effects associated with the clinical use of ACE inhibitors such as dry cough and rashes may be due to bradykinin potentiation. 24 Therefore, a need for more specific means of blocking the effects of Ang II arose.Research in this area was sparked by patents of Takeda Chemical Industries in Japan in 1982. 25 At about the same time, DuPont began work on such an antagonist. This led to the discovery of the first important drug, Losartan, in 1986 26,27 that was very

An excellent example in the field of rational drug design is the discovery and development of more than a dozen drugs for the treatment of AIDS. The major targets for the development of new chemotherapeutic agents are Reverse Transcriptase and Protease, the enzymes encoded by HIV-1. The introduction of HIV-1 protease (HIV-1 PR) inhibitors, in particular, has drastically decreased the mortality and morbidity associated with AIDS. The inhibition of this enzyme results in production of immature and noninfectious virions. In the present review, a comparative quantitative structure activity relationship (QSAR) study of various peptidomimetic and non-peptidomimetic molecules investigated for their inhibitory activity has been reported. Among the various physicochemical properties studied, hydrophobicity, steric and electronic interactions are found to play important role in binding to the receptor.