| Literature DB >> 35852367 |
Karthik Ramalingam1, Sonali Gangwar1,2, Deep Chandra Balodi1,2, Apeksha Anand1,2, Shailendra Yadav1,2, Subhasish Biswas3, Anil Kumar Karunakaran Sasikala3, Kailash Chand Gupta4, Sanjay Batra3,2, Neena Goyal1,2.
Abstract
Chemotherapy is the key intervention to control visceral leishmaniasis (VL), a neglected tropical disease. Current regimens include not only a few drugs but also present several drawbacks, including moderate to severe toxicity, cost, long-term administration, patient compliance, and growing drug resistance. Thus, the need for better treatment options against VL is a priority. In an endeavor to find an orally active and affordable antileishmanial agent, we evaluated the therapeutic potential of compounds belonging to the (2Z,2'Z)-3,3'-(ethane-1,2-diylbis(azanediyl))bis(1-(4-halophenyl)-6-hydroxyhex-2-en-1-ones) series, identified as inhibitor(s) of Leishmania donovani dipeptidylcarboxypeptidase, a novel drug target. Among them, compound 3c exhibited best in vivo antileishmanial efficacy via both intraperitoneal and oral routes. Therefore, the present study led to the identification of compound 3c as the lead candidate for treating VL.Entities:
Keywords: Leishmania donovani; dipeptidylcarboxypeptidase; in vivo efficacy; inhibitor; visceral leishmaniasis
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Year: 2022 PMID: 35852367 PMCID: PMC9380552 DOI: 10.1128/aac.02361-21
Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN: 0066-4804 Impact factor: 5.938