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Design, synthesis and evaluation of novel phenanthridine triazole analogs as potential antileishmanial agents. 2022

Adinarayana Nandikolla, and Srinivasarao Singireddi, and Karan Kumar Banoth, and Sankaranarayanan Murugesan, and Himanshu Aggarwal, and Rafael Balaña-Fouce, and Melcón-Fernandez Estela, and Venkata Gowri Chandra Sekhar Kondapalli
Department of Chemistry, Birla Institute of Technology & Science, Pilani, Hyderabad Campus, Jawahar Nagar, Kapra Mandal, Hyderabad, Telangana, 500078, India.

Aim: To synthesize and screen phenanthridine and 1,2,3-triazole derivatives for antileishmanial activity. Methodology: Synthesized analogs were tested for antileishmanial activity against transgenic strain of Leishmania infantum promastigotes and ex vivo infections. Results: Compounds T01, T08 and T11 revealed significant activity with EC50 <30 μm and lacked toxicity in mouse spleen and HepG2 cells. T01 with EC50 3.07 μm is fourfold more potent than the drug miltefosine (EC50 12.6 μM) against L. infantum promastigotes. In silico studies indicate that the analogs are nontoxic. A molecular docking analysis was also carried out on the T01 and T08 to investigate the binding pattern at the active site of the chosen target trypanothione reductase. Conclusion: The results of this study reveal that phenanthridine triazoles exhibit antileishmanial activity.

UI MeSH Term Description Entries
D010617 Phenanthridines
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000981 Antiprotozoal Agents Substances that are destructive to protozoans. Schizonticides,Agents, Antiprotozoal
D014230 Triazoles Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3. Triazole
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus
D062105 Molecular Docking Simulation A computer simulation technique that is used to model the interaction between two molecules. Typically the docking simulation measures the interactions of a small molecule or ligand with a part of a larger molecule such as a protein. Molecular Docking,Molecular Docking Simulations,Molecular Docking Analysis,Analysis, Molecular Docking,Docking Analysis, Molecular,Docking Simulation, Molecular,Docking, Molecular,Molecular Docking Analyses,Molecular Dockings,Simulation, Molecular Docking
D018314 Leishmania infantum A parasitic hemoflagellate of the subgenus Leishmania leishmania that infects man and animals and causes visceral leishmaniasis (LEISHMANIASIS, VISCERAL). Human infections are confined almost entirely to children. This parasite is commonly seen in dogs, other Canidae, and porcupines with humans considered only an accidental host. Transmission is by Phlebotomus sandflies. Leishmania (Leishmania) infantum,Leishmania donovani chagasi,Leishmania donovani infantum,Leishmania (Leishmania) chagasi,Leishmania chagasi,Leishmania chagasi chagasi,Leishmania chagasi subsp. Chagasi,Leishmania infantum chagasi,Leishmania leishmania infantum,chagasi chagasi, Leishmania,chagasi, Leishmania,chagasi, Leishmania chagasi,chagasi, Leishmania infantum,donovani chagasi, Leishmania,donovani infantum, Leishmania,infantum chagasi, Leishmania,infantum, Leishmania donovani,infantum, Leishmania leishmania,leishmania infantum, Leishmania

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