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Drug design toxicity problem

Fortunately, there is now a comprehensive body of knowledge on the metabolic reactions that produce reactive (toxic) intermediates, so the drug designer can be aware of what might occur, and take steps to circumvent the possibility. Nelson (1982) has reviewed the classes and structures of drugs whose toxicities have been linked to metabolic activation. Problem classes include aromatic and some heteroaromatic nitro compounds (which may be reduced to a reactive toxin), and aromatic amines and their N-acylated derivatives (which may be oxidized, before or after hydrolysis, to a toxic hydroxylamine or iminoquinone). These are the most common classes, but others are hydrazines and acyl-hydrazines, haloalkanes, thiols and thioureas, quinones, many alkenes and alkynes, benzenoid aromatics, fused polycyclic aromatic compounds, and electron-rich heteroaromatics such as furans, thiophenes and pyrroles. [Pg.93]

Gaining maximum potency is only half the problem in drug design. The other half is to minimize unwanted side effects. Therefore, for the ultimate in maximization of the therapeutic index, regression analysis must also be applied to relate substituent effects to the various kinds of serious toxicity as these become evident. [Pg.45]

Recreational abuse of designer drugs poses a major problem. Evidence concerning the safety of these drugs has shown that MDA and MDMA are toxic to serotonergic neurons in rodent (Ricaurte et al. 1985 Stone et al. 1987 O Heam et al. 1988) and primate brains (Ricaurte et al. 1988). [Pg.30]

QSAR are useful In the design of pesticides and medicinal drugs, and In environmental problems such as the prediction of toxicity and blodegradablllty. An empirical relationship can be properly used only for Interpolation whereas one based solidly on well-established theory can be used at least to some extent for extrapolation as well. It seems of real Importance, then, to determine the nature and slgmiflcance of steric and bulk parameters In QSAR. [Pg.249]


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