Table 1 In vitro anti-mycobacterial activity of compounds 3a–j and
8a–j against M. tuberculosis mc27000
tubercular activity profiles. Further, the synthesized ferrocenyl-
chalcone based hybrids also fail to produce any significant
enhancement in the activity profiles of these compounds. In con-
clusion, we have utilized the molecular hybridization protocol
for the synthesis of ferrocene–β-lactam and ferrocenylchalcone–
β-lactam based structural chimeras via Huisgen azide–alkyne
cycloaddition and the evaluation of their anti-tubercular activity.
The described protocol is the first successful attempt on the
inclusion of ferrocene nucleus in the β-lactam family tethered
via triazole linkers having metabolic stability and physicochem-
ical favourability. The synthesized chimeras will also be explored
for their anticancer and antiplasmodial profiles and further work
on the scope and extension of the devised protocol is currently
under progress.
Compound
MIC (μg ml−1
)
3a
3b
3c
3d
3e
3f
3g
3h
3i
3j
8a
8b
8c
8d
8e
8f
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
>100
10–25
Acknowledgements
8g
8h
8i
8j
The authors wish to thank Pr. W.R. Jacobs for the generous gift
of M. tuberculosis mc27000, which has been approved for use in
Biosafety Level 2 containment by the Institutional Biosafety
Committees of the Albert Einstein College of Medicine and the
University of Montpellier. We thank also E. Vialla for excellent
technical assistance. Financial assistance from Department of
Science and Technology, New Delhi under Innovation in Science
Pursuit for Inspired Research (INSPIRE) Fellowship (KK) is
gratefully acknowledged.
Cephalexin
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5780 | Dalton Trans., 2012, 41, 5778–5781
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