- Novel macrolides and ketolides having antimicrobial activity
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The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-γ lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.
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Page/Page column 45
(2009/10/06)
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- Structure-activity relationships of tyrosinase inhibitory combinatorial library of 2,5-disubstituted-1,3,4-oxadiazole analogues
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Here the tyrosinase inhibition studies of library of 2,5-disubstituted-1,3, 4-oxadiazoles have been reported and their structure-activity relationship (SAR) also have been discussed. The library of the oxadiazoles was synthesized under the microwave irradiation and was structures of these were characterized by different spectral techniques. From this study it could be concluded that for a better inhibition of tyrosinase, electronegative substitution is essential as most probably the active site of the enzyme contain some hydrophobic site and position is also very important for the inhibition purposes due to the conformational space. The electronegativity of the compounds is somewhat proportional to the inhibitory activity. The compound 3e (3′-[5-(4′- bromophenyl)-1,3,4-oxadiazol-2-yl]pyridine) exhibited most potent (IC 50 = 2.18 μM) inhibition against the enzyme tyrosinase which is more potent than the standard potent inhibitor l-mimosine (IC50 = 3.68 μM). This molecule can be the best candidate as a lead compound for further development of drug for the treatments of several skin disorders.
- Khan, Mahmud Tareq Hassan,Choudhary, Muhammad Iqbal,Khan, Khalid Mohammed,Rani, Mubeen,Atta-ur-Rahman
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p. 3385 - 3395
(2007/10/03)
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