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1,2,4,5-Tetraoxane derivatives/hybrids as potent antimalarial endoperoxides: Chronological advancements, structure-activity relationship (SAR) studies and future perspectives.
T A, Abdul Rahaman; Rajendra, Thakar Neha; Suhas, Kshirsagar Prasad; Ippagunta, Sirish K; Chaudhary, Sandeep.
Affiliation
  • T A AR; Department of Medicinal Chemistry, Laboratory of Bioactive Heterocycles and Catalysis (BHC lab), National Institute of Pharmaceutical Education and Research-Raebareli (Transit Campus), Lucknow, India.
  • Rajendra TN; Department of Medicinal Chemistry, Laboratory of Bioactive Heterocycles and Catalysis (BHC lab), National Institute of Pharmaceutical Education and Research-Raebareli (Transit Campus), Lucknow, India.
  • Suhas KP; Department of Medicinal Chemistry, Laboratory of Bioactive Heterocycles and Catalysis (BHC lab), National Institute of Pharmaceutical Education and Research-Raebareli (Transit Campus), Lucknow, India.
  • Ippagunta SK; Department of Biotechnology, All India Institute of Medical Sciences (AIIMS), New Delhi, India.
  • Chaudhary S; Department of Medicinal Chemistry, Laboratory of Bioactive Heterocycles and Catalysis (BHC lab), National Institute of Pharmaceutical Education and Research-Raebareli (Transit Campus), Lucknow, India.
Med Res Rev ; 44(5): 2266-2290, 2024 09.
Article in En | MEDLINE | ID: mdl-38618882
ABSTRACT
Malaria is a life-threatening disease that affects tropical and subtropical regions worldwide. Various drugs were used to treat malaria, including artemisinin and derivatives, antibiotics (tetracycline, doxycycline), quinolines (chloroquine, amodiaquine), and folate antagonists (sulfadoxine and pyrimethamine). Since the malarial parasites developed drug resistance, there is a need to develop new chemical entities with high efficacy and low toxicity. In this context, 1,2,4,5-tetraoxanes emerged as an essential scaffold and have shown promising antimalarial activity. To improve activity and overcome resistance to various antimalarial drugs; 1,2,4,5-tetraoxanes were fused with various aryl/heteroaryl/alicyclic/spiro moieties (steroid-based 1,2,4,5-tetraoxanes, triazine-based 1,2,4,5-tetraoxanes, aminoquinoline-based 1,2,4,5-tetraoxanes, dispiro-based 1,2,4,5-tetraoxanes, piperidine-based 1,2,4,5-tetraoxanes and diaryl-based 1,2,4,5-tetraoxanes). The present review aims to focus on covering the relevant literature published during the past 30 years (1992-2022). We summarize the most significant in vitro, in vivo results and structure-activity relationship studies of 1,2,4,5-tetraoxane-based hybrids as antimalarial agents. The structural evolution of different hybrids can provide the framework for the future development of 1,2,4,5-tetraoxane-based hybrids to treat malaria.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tetraoxanes / Antimalarials Limits: Animals / Humans Language: En Journal: Med Res Rev Year: 2024 Document type: Article Affiliation country: India Country of publication: United States

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tetraoxanes / Antimalarials Limits: Animals / Humans Language: En Journal: Med Res Rev Year: 2024 Document type: Article Affiliation country: India Country of publication: United States