Design and Synthesis of a New Class of 4‐Aminoquinolinyl‐ and 9‐Anilinoacridinyl Schiff Base Hydrazones as Potent Antimalarial Agents. (13th March 2014)

• Record Type: Journal Article
• Authors: Sharma, Moni; Chauhan, Kuldeep; Srivastava, Rajeev K.; Singh, Shiv V.; Srivastava, Kumkum; Saxena, Jitendra K.; Puri, Sunil K.; Chauhan, Prem M. S.
• Is Part Of: Chemical biology & drug design. Volume 84:Number 2(2014:Aug.)
• Page Start: 175
• Page End: 181
• Publication Date: 2014-03-13
• Subjects: Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12289
• Languages: English
• ISSNs: 1747-0277

Abstract

<abstract abstract-type="main" id="cbdd12289-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p>A series of novel 4‐aminoquinolinyl and 9‐anilinoacridinyl Schiff base hydrazones have been synthesized and evaluated for their antimalarial activity. All compounds were evaluated <italic>in vitro</italic> for their antimalarial activity against chloroquine‐sensitive strain 3D7 and the chloroquine‐resistant K1 strain of <italic>Plasmodium falciparum</italic> and for cytotoxicity toward Vero cells. Compounds <bold>17</bold>, <bold> 20</bold>, and <bold>21</bold> displayed good activity against the 3D7 strain with IC₅₀ values ranging from 19.69 to 25.38 n<sc>m</sc>. Moreover, compounds <bold>16</bold>, <bold> 17</bold>, <bold> 21</bold>, <bold> 24</bold>, <bold> 32, </bold> and <bold>33</bold> exhibited excellent activities (21.64–54.26 n<sc>m</sc>) against K1 strain and several compounds displayed <italic>β</italic>‐hematin inhibitory activity, suggesting that they act on the heme crystallization process such as CQ. Compounds were also found to be non‐toxic with good selectivity index.</p> </abstract>