Am. Dhople et al., IN-VITRO ACTIVITIES OF 2,2'-BIPYRIDYL ANALOGS AGAINST MYCOBACTERIUM-AVIUM AND MYCOBACTERIUM-TUBERCULOSIS, Tubercle and lung disease, 76(2), 1995, pp. 136-140
Setting: Because of widespread emergence of resistant Mycobacterium tu
berculosis and the high incidence of opportunistic infection caused by
M. avium complex (MAC) in AIDS patients, there is an urgent need for
new drugs against these organisms. Objective: To evaluate the activity
of newly synthesized 2'2-bipyridyl analogues against MAC and M. tuber
culosis. Design: Susceptibility of MAC and M. tuberculosis to VUF-8514
and VUF-8842 were determined by both tube dilution method using 7H9 b
roth and radiometric (BACTEC) method using C-14-palmitic acid. Results
and Conclusions: The MICs of 8514 against MAC and M. tuberculosis wee
1 mug/ml and 0.5 mug/ml respectively, while for 8842 the respective v
alues were 8 mug/ml and 2 mug/ml. In general, the MBC values for both
drugs were two-fold higher than their corresponding MIC values. Howeve
r, both drugs exhibited high bactericidal activities against both orga
nisms. The MICs of clinical isolates of both organisms were in the sam
e range as reference strains; furthermore, two isolates of M. tubercul
osis that showed resistance to rifampicin were found to be susceptible
to 8514. Thus, these two bipyridyl analogues show great promise in ch
emotherapy of tuberculosis and M. avium infection.