MUMBAI, India, Sept. 28 -- Intellectual Property India has published a patent application (202511012500 A) filed by Council Of Scientific And Industrial Research An Indian on February 13, 2025, for Piperazine Adducts Of Dehydrocostuslactone And Costunolide As Antileishmanial Agent And Process For The Preparation Thereof.
Inventors include Prasoon Kumar Gupta; Kuljit Singh; Anil Bhushan; Diksha Kumari; and Zabeer Ahmed.
The application for the patent was published on September 25, 2026, under issue no. 39/2026.
Abstract: This invention provides a novel expedient one step synthetic procedure for the preparation of derivatives of dehydrocostus lactone and costunolide using diverse piperazine under very mild reaction condition and short period of time. The synthesized derivatives have improved safety profile along with anti-leishmanial killing potential. The potent leads displayed significant leishmanicidal potency and satisfactory selectivity against major macrophage cell lines (J774.A1 and RAW 264.7). Further, ex vivo analysis validated their potential for the clearance of intracellular amastigote burden with a better anti-amastigote selectivity index. The potent hits 1po and 2pp caused alteration in structural morphology, intracellular ROS generations, depletion in ATP pool indicating mitochondrial disfunction, accumulation of lipid inclusions, and disruption of sterol membrane. This study confirmed efficacy of synthesised derivatives against L. donovani supported by exploration of mechanistic insight. Further exploration of potent derivatives may lead to development of novel drug candidates to fight against parasitic infections
Disclaimer: Curated by HT Syndication.
