title: In vitro cytotoxic, antibacterial, antifungal and urease inhibitory activities of some N4- substituted isatin-3-thiosemicarbazones.
abstract: A series of 15 previously reported N(4)-substituted isatin-3-thiosemicarbazones 3a-o has been screened for cytotoxic, antibacterial, antifungal and urease inhibitory activities. Compounds 3b, 3e and 3n proved to be active in cytotoxicity assay; 3e exhibited a high degree of cytotoxic activity (LD(50) = 1.10 x 10(-5) M). Compound 3h exhibited significant antibacterial activity against B. subtilis, whereas compounds 3a, 3k and 3l displayed significant antifungal activity against one or more fungal strains i.e. T. longifusus, A. flavus and M. canis. In human urease enzyme inhibition assay, compounds 3g, 3k and 3m proved to be the most potent inhibitors, exhibiting relatively pronounced inhibition of the enzyme. These compounds, being non-toxic, could be potential candidates for orally effective therapeutic agents to treat certain clinical conditions induced by bacterial ureases like H. pylori urease. This study presents the first example of inhibition of urease by isatin-thiosemicarbazones and as such provides a solid basis for further research on such compounds to develop more potent inhibitors.
authors.affiliation: Department of Chemistry, Bahauddin Zakariya University, Multan, Pakistan. pdhpervez@hotmail.com
authors.forename: Humayun
authors.initials: H
authors.lastname: Pervez
authors.forename: Mohammad S
authors.initials: MS
authors.lastname: Iqbal
authors.forename: Muhammad Younas
authors.initials: MY
authors.lastname: Tahir
authors.forename: Faiz-ul-Hassan
authors.initials: FU
authors.lastname: Nasim
authors.forename: Muhammad Iqbal
authors.initials: MI
authors.lastname: Choudhary
authors.forename: Khalid Mohammed
authors.initials: KM
authors.lastname: Khan
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D003445:Crustacea / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D007510:Isatin / Q000737:chemistry*; D050296:Microbial Viability / Q000187:drug effects; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D014510:Urease / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D004791:Enzyme Inhibitors; D013882:Thiosemicarbazones; D007510:Isatin; D014510:Urease