| 摘要 |
<p>The invention provides a new antimicrobial phenazine derivative which has the structural Formula I <CHEM> characterized by one of the following five sets (a - e) of values for R, R<1> and R<2> (a) R = CH3- ; R<1> = H ; R<2> = Cl (b) R = CH3. CH2-; R<1> = H ; R<2> = Cl (c) R = CH3. CH2-; R<1> = Br; R<2> = H (d) R = CH3. CH2-; R<1> = Cl; R<2> = Cl (e) R = CH3. CH2-; R<1> = Br; R<2> = Cl The last three compounds (Ic), (Id) and (Ie) are preferred. A method for preparing these compounds is also provided, comprising (1) reacting a substituted nitrobenzene (III) with a substituted and formylated aniline (IV) to produce a substituted 2-nitrodiphenylamine (V), (2) reducing the product of Step (1) to form a 2-aminodiphenylamine (VI); (3) oxidatively condensing the product of Step (2) to unite two molecules thereof forming a substituted 3-anilino-2-imino-10-phenyl-2,10-dihydrophenazine (VII); and (4) reacting the product of Step 3 with methylamine or ethylamine. The compounds are useful in the treatment of ailments caused by various named bacterial families and species, especially Mycobacterium avium and M leprae, and in the treatment of opportunistic infections in patients whose immune system is compromised.</p> |
