Synthesis and antitubercular activity of some mannich bases derived from isatin isonicotinic acid hydrazone

The purpose of this study based on the design and synthesis of a new series of 4-[1-[substitutedaminomethyl]]-2-oxo-2,3-dihydro-1H-3-indolylidene-pyridine- carboxylic acid hydrazones [2a-g] in a trial to overcome the resistance developed with the therapeutic uses of isonicotinic acid hydrazide [isoniazid, INH]. The new compounds were prepared by reacting isatin isonicotinic acid hydrazone with formalin and the appropriate secondary amines. The structures of the newly synthesized compounds were elucidated using different spectral data [IR, 1 HNMR, and 13 CNMR] as well as elemental methods of analyses. The lipophilicity of the synthesized compounds supercedes that of INH as expressed by Clog P.The new compounds [2a-g] as well as INH as a reference drug were tested for their antitubercular activity against bovine Mycobacterium tuberculosis at a dose level of 10 micromol. The tested compounds exhibited comparable inhibitory activity against the tested TB strain comparing to INH a reference drug

Antileishmanial agents: synthesis of allopurinol prodrugs for oral administration

Synthesis of six prodrugs of allopurinol (4-hydroxypyrazolo-(3,4-d)pyrimidine) is described. These compounds were given orally to male and female BALB/C (sensitive) and C57BL/6 (partially resistant) strains of mice, wich had been previously infected with Leishmania mexicana. The results show that at end of the treatment there was weak regression of lesions confirmed through measurement of nodule diameter in the infected animals