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H.G. Kathrotiya et al. / Chinese Chemical Letters 23 (2012) 273–276
Antimicrobial study of all the title derivatives revealed good to moderate inhibition except compound 6q
(R1 OCH3, R2 Ph, X N–CH2CH3) found exceedingly potent against bacterial species E. coli. Whereas, all the
compounds, against B. subtilis and B. cereus, found poorly active. In addition, all the synthesized compounds were
screened for their antifungal activitiy against A. parasiticus and S. rolfsii and were found significantly active upon
comparison with Griseofulvin.
The structure–activity relationship (SAR) study revealed that antifungal screening of compounds having
substitution X O displayed better activity and X N–Et showed poor activity against Griseofulvin. Compounds
containing X O (6a, 6d, 6g, 6j, 6m and 6p) were extremely active but, upon replacing with X N–Et/N–Me (6b, 6c,
6e, 6f, 6h, 6i, 6k, 6l, 6n, 6o, 6q and 6r) resulted in poor activity towards S. rolfsii. While, substitution X N–Et (6b, 6e
and 6h) derivatives have shown poor activity and upon replacing with X N–Me (6c, 6f and 6i) enhanced potency
against fungal pathogen A. parasiticus. Moreover, against A. parasiticus, R2 Me derivative (6w) exhibited moderate
activity, upon changing R2 Ph (6x) resulted in increased inhibitory action.
Reviewing and comparing the activity data, it is worthy to mention that the compounds of this series possess better
fungicidal activity as well as poor bactericidal activity and antimicrobial activity of the target compounds depends not
only on the bicyclic heteroaromatic pharmacophore appended through aryl ring but also on the nature of the peripheral
substituents and may also upon their spatial relationship and positional changes.
Acknowledgment
The authors are grateful to the Department of Chemistry, S P University, India for providing laboratory facilities.
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