Abstract
This chapter discusses enzyme inhibition, drug resistance and drug synergism, and reversible enzyme inhibitors. Enzyme inhibition is a promising approach for the rational discovery of new leads or drugs. Enzyme inhibitors are grouped into two general categories: reversible and irreversible inhibitors. In reversible inhibitor, noncovalent interactions are involved, while irreversible enzyme inhibitors involve a covalent bond. Enzyme inhibitors are often similar in molecular structure to substrates or products of the target enzyme. Consequently, lead compounds are readily obtained for enzyme targets. The mechanisms of resistance involve changes in the target site for antibiotic interaction because that confers resistance to all compounds with the same mechanism of action. When drugs are given in combination, their effects can be antagonistic, subadditive, additive, or synergistic. Drug synergism arises when the therapeutic effect of two or more drugs used in combination is greater than the sum of the effects of the drugs administered individually.
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