01909nas a2200361   4500000000100000008004100001260001300042653001200055653001900067653001200086653001600098653002700114653003300141653001100174653001100185653001300196653001200209653000900221653002400230653002500254653001500279653001700294100002300311700001500334700001900349700001700368245008300385856004100468300001100509490000700520520100600527022001401533       1993                            d  c1993 Sep10aAbdomen10aAdipose Tissue10aAnimals10aClofazimine10aDisease Models, Animal10aDrug Evaluation, Preclinical10aFemale10aHumans10aKinetics10aleprosy10aMice10aMolecular Structure10aMycobacterium leprae10aPhenazines10aPigmentation1 aVan Landingham R M1 aWalker L L1 aO'Sullivan J F1 aShinnick T M00aActivity of phenazine analogs against Mycobacterium leprae infections in mice.  uhttp://ila.ilsl.br/pdfs/v61n3a05.pdf  a406-140 v613 a<p>Twenty-five compounds structurally related to clofazimine were tested for their ability to inhibit the growth of Mycobacterium leprae using the kinetic method of drug evaluation in the mouse foot pad model of leprosy. Seven of the phenazine derivatives displayed anti-M. leprae activity comparable to that of clofazimine when administered at a concentration of 0.01% (w/w) in the diet. Three of the compounds, B746, B4087, and B4101, were active when administered at 0.001% in the diet. At a dietary concentration of 0.0001%, B4087 and B4101 were slightly more active than clofazimine, while B746 was less active. In the kinetic method of drug evaluation, greater anti-M. leprae activity of phenazine derivatives was generally associated with greater pigmentation of abdominal fat. Of the compounds which did not cause pigmentation when fed at a concentration of 0.01% in the diet B4090 was the most active. This compound also inhibits the growth of a clofazimine-resistant M. smegmatis strain.</p>  a0148-916X