New pyrrolo[1,2-α]quinoxaline-2- or -4-carboxylic acid hydrazide derivatives were synthesized from nitroaniline or 1,2-phenylenediamine, and evaluated in vitro for their antimycobacterial activity as part of a TAACF TB screening program. Two compounds 7c and 13 showed an interesting activity at 6.25 μg/mL against Mycobacterium tuberculosis H37Rv, with a 94 and 100 percentage inhibition, respectively. © 2004 Taylor & Francis Ltd.