Abstract:
:A new series of 12 N(4)-substituted isatin-3-thiosemicarbazones 2a-l has been synthesized, characterized and screened for in vitro cytotoxic, phytotoxic and urease inhibitory effects. All the compounds proved to be active in the brine shrimp bioassay; 2a, 2b, 2d, 2f and 2h-l exhibited a high degree of cytotoxic activity (LD(50) = 1.10 x 10(- 5) M-3.10 x 10(- 5) M). In urease-inhibition assay, compounds 2a, 2b, 2e, 2f, 2h-j and 2l proved to be potent inhibitors displaying relatively much greater inhibition of the enzyme with IC(50) values ranging from 20.6 microM to 50.6 microM. Amongst these, 2a and 2f were found to be the most potent ones exhibiting pronounced inhibition with IC(50) value 20.6 microM. All the synthetic compounds showed weak to moderate (10-40%) phytotoxicity at the highest tested concentration (500 microg/mL) indicating their usefulness as inhibitors of soil ureases.
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Pervez H,Chohan ZH,Ramzan M,Nasim FU,Khan KMdoi
10.1080/14756360802188420subject
Has Abstractpub_date
2009-04-01 00:00:00pages
437-46issue
2eissn
1475-6366issn
1475-6374pii
794976409journal_volume
24pub_type
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