01334nas a2200217 4500000000100000008004100001260001600042653001200058653001100070653002300081653001200104653002500116653001300141100001200154700001600166245009000182300000800272490000700280520081500287022001401102 1989 d c1989 Feb 2410aDapsone10aHumans10aLeprostatic Agents10aleprosy10aMycobacterium leprae10aRifampin1 aSaane P1 aTimmerman H00aPharmacochemical aspects of leprosy. Recent developments and prospects for new drugs. a3-80 v113 a

From a pharmacochemical point of view the existing anti-leprotics as well as possible innovations in the chemotherapy of leprosy are discussed. Of the main anti-leprotics, which are used nowadays--dapsone, rifampicin, clofazimine, isoniazide, ethionamide and prothionamide--the mechanism of action, the main problems in their application and possibilities to develop improved variants are reviewed. Based on the chemistry of Mycobacterium leprae, the target systems for new anti-leprotics are identified. These systems include the cell wall, the catabolism of reactive oxygen species, the metabolisms of carbon sources, the amino acid metabolism and the uptake of iron. Two possible new lead structures from other fields, 4-quinolones and mycobacterial ribonucleotide reductase inhibitors are presented.

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