5-Nitroisatin-derived thiosemicarbazones: potential antileishmanial agents. (October 2014)

• Record Type: Journal Article
• Authors: Pervez, Humayun; Manzoor, Nazia; Yaqub, Muhammad; Khan, Khalid Mohammed
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 29:Number 5(2014:Oct.)
• Page Start: 628
• Page End: 632
• Publication Date: 2014-10
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2013.836641
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title>Abstract</title> <p>A series of 29 previously reported <italic>N</italic>⁴-substituted 5-nitroisatin-3-thiosemicarbazones <bold>2</bold>–<bold>30</bold> has been screened for leishmanicidal potential. Compounds <bold>2</bold>–<bold>4</bold>, <bold>7</bold>, <bold>8</bold>, <bold>10</bold>–<bold>13</bold>, <bold>15</bold>–<bold>19</bold>, <bold>21</bold>, <bold>23</bold>, <bold>24</bold>, <bold>26</bold>, <bold>28</bold> and <bold>30</bold> exhibited good to excellent antileishmanial activities with IC₅₀ values ranging from 0.44 ± 0.02 to 32.38 ± 0.66 µg/mL. Of these, <bold>5</bold>, <bold>7</bold>, <bold>19</bold> and <bold>28</bold> proved to be the most active antileishmanial agents, displaying activities with IC₅₀ values 1.78 ± 0.35, 0.44 ± 0.02, 1.91 ± 0.04 and 4.28 ± 0.75 µg/mL, respectively, which were even better than the standard drug, pentamidine (IC₅₀ = 5.09 ± 0.04 µg/mL). This study presents the first example of exhibition of leishmanicidal potential by isatin-thiosemicarbazones and as such furnishes a solid basis for further research on these compounds to develop more potent antileishmanial agents.</p> </abstract>