Miscellaneous Quinolones

The product from the formal replacement of the benzimidazolone function in itasetron (57-6, Chapter 10) by a quinolone has been reported to display much the same serotonin antagonists activity of the former. In the absence of a specific reference to the synthesis, the starting quinolone is speculatively formed by reaction of cyclo-hexylaniline (50-1) with EMME to produce the enamide (50-2) from displacement 

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In this chapter, an attempt has been made to present a total number of 20 QSAR models (12 QSAR models for topo I inhibitors and eight QSAR models for topo II inhibitors) on 11 different heterocyclic compound series (an-thrapyrazoles, benzimidazoles, benzonaphthofurandiones, camptothecins, desoxypodophyllotoxins, isoaurostatins, naphthyridinones, phenanthridines, quinolines, quinolones, and terpenes) as well as on some miscellaneous heterocyclic compounds for their inhibition against topo I and II. They have been found to be well-correlated with a number of physicochemical and structural parameters. The conclusion, from the analysis of these 20 QSAR, has been drawn that the inhibition of topo I is largely dependent on the hydrophobicity of the compounds/substituents. On the other hand, steric parameters (molar refractivity, molar volume, and Verloop s sterimol parameters) are important for topo II inhibition. 

A number of drugs of miscellaneous class are capable of producing various degrees of renal damage and will be reviewed in this Chapter. Some have been used extensively in the past for the treatment of general infections (sulfonamides), others have had specific indications (pentamidine, dapsone), and others such as quinolones are of more recent application. Many of these, however, are of current interest because of their use in treating the complications occurring in patients with acquired immunodeficiency syndrome (AIDS). 

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