A new series of 2,2′-bipyridyl analogues with high activity against AIDS-complicating micro-organisms

Timmerman, Henk; Goot, H. van der; Seydel, Joachim K.

doi:10.1007/bf01974989

Pharmaceutisch Weekblad Scientific Edition

1991

DOI: 10.1007/bf01974989

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A new series of 2,2′-bipyridyl analogues with high activity against AIDS-complicating micro-organisms

Henk Timmerman¹,

H. van der Goot²,

Joachim K. Seydel³

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1994

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“…De Zwart and associates (3)(4)(5) have reported a new class of compounds, 2,2'-bipyridyl analogs, exhibiting potent antimycoplasmal properties. Subsequently, in preliminary studies, Timmerman and coworkers (20) have demonstrated antimycobacterial activities of these analogs, and Seydel and associates (19) have studied relationship between inhibitory activities of these analogs and membrane composition of various bacteria and fungi. Recently, we have demonstrated the bactericidal activities of these analogs against several clinical isolates of M. avium and M. tuberculosis (16).…”

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In vitro activities of 2,2'-bipyridyl analogs against Mycobacterium leprae

Dhople

Ibáñez

Dhople

1994

Antimicrob Agents Chemother

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In vitro susceptibility ofMycobacterium leprae to two bipyridyl analogs was studied by using two biochemical parameters to measure the metabolic activity of the organism. VUF-8514 at 0.16 ,uglml, but not VUF-8842, completely inhibited the metabolic activity of M. keprae, and the action was bactericidal. When compared to rifampin (MIC 0.3 ,ug/ml), VUF-8514 was equally bactericidal against M. keprae. The aim of the present study was to evaluate the activities of these analogs, in comparison to that of rifampin, against M. leprae in an in vitro culture system. Antimicrobial agents. The 2,2'-bipyridyl analogs, VUF-8514 (isoquinoline derivative) and VUF-8842 (1,10-phenanthroline derivative) were obtained from H. Timmerman of Free University, Amsterdam, The Netherlands. The structural formulae and chemistry of these compounds have been described earlier (3)(4)(5) (7). ATP determinations were carried out by the firefly bioluminescent technique described earlier (8), while the procedure of Khanolkar and coworkers (17) was followed for the measurement of thymidine uptake.The effect of drug on M. leprae in primary culture was evaluated after incubating cultures for 4 weeks at 34°C. To determine if the effects were bacteriostatic or bactericidal, the cells from 4-week-old primary cultures were washed twice with fresh DH medium and then suspended in fresh DH medium without the drug and incubated at 34°C for four more weeks. At this time, ATP and [3H]thymidine uptake assays were again performed.Sampling for the assays from primary and subcultures was done as described previously. The results presented here were derived from three separate experiments, using different M. leprae strain in each experiment. In each experiment, triplicate assays were done for each concentration of every drug including rifampin.Susceptibility of M. leprae to bipyridyls. In the control cultures (without drugs), metabolic activity of M. leprae in primary cultures at 4 weeks was 143% of that at zero hour (Table 1). When the cells from these primary cultures were transferred to fresh DH medium, the activity in subcultures was 134% of the original at zero hour of these subcultures (143% increase in primary cultures was adjusted to 100% at zero hour for subcultures). With VUF-8514 at concentrations of 0.08 ,ug/ml and below, the metabolic activity of M. keprae in primary cultures as well as in subcultures was the same in control cultures. However, when the concentration of VUF-8514 in primary cultures was 0.16 ,ug/ml and higher, no metabolic activity could be detected, suggesting the MIC of VUF-8514 against M. leprae was 0.16 ,ug/ml. When these cells from primary cultures were transferred to fresh drug-free DH medium, cells failed to exhibit any metabolic activity, even after 4 weeks. This suggests the bactericidal activity of VUF-8514 on M leprae. On the other hand, VUF-8842 had no inhibitory effect on the metabolic activity of M leprae even at 0.32 ,ug/ml-the highest concentration tested to compare against rifampin, whose MIC against M leprae has been ...

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confidence: 99%

In vitro activities of 2,2'-bipyridyl analogs against Mycobacterium leprae

Dhople

Ibáñez

Dhople

1994

Antimicrob Agents Chemother

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A new series of 2,2′-bipyridyl analogues with high activity against AIDS-complicating micro-organisms

Cited by 1 publication

References 8 publications

In vitro activities of 2,2'-bipyridyl analogs against Mycobacterium leprae

In vitro activities of 2,2'-bipyridyl analogs against Mycobacterium leprae

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