Synthesis and antibacterial/antitubercular activity evaluation of symmetrical trans-cyclohexane-1,4-diamine derivatives

INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY(2013)

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摘要
A library of symmetrical trans-cyclohexane-1,4-diamine derivatives have been synthesized and evaluated for their activity against the M. tb H(37)Rv strain. Most of the synthesized compounds show moderate to weak activity against M. tb H(37)Rv strain. Out of twenty-seven compounds tested, four compounds having substitution at p-position on the aromatic ring exhibit activity with MIC99 value ranging from 12.5 - 25 mu M. Compound 9u having i-propyl group substitution at p-position is found to be the most potent among all the tested compounds with MIC99 value of 12.5 mu M against M. tb H(37)Rv strain. All these compounds have also been tested against Methicilin resistant Staphylococcus aureus (MRSA), and four of the compounds 9c, 91, 9p and 9s possess good antibacterial activity with IC50 ranging from 128 mg/L - 256 mg/L.
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关键词
Bromhexine,trans-cyclohexane-1,4-diamine,Mycobacterium tuberculosis,tuberculosis,methicillin resistant Staphylococcus aureus (MRSA)
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