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Author Ravi Jain

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Biological evaluation of novel side chain containing CQTrICh-analogs as antimalarials and their development as PfCDPK1 kinase inhibitors

Iram Irfan, Amad Uddin, Ravi Jain, Aashima Gupta, Sonal Gupta, John Napoleon, Afzal Hussain, Mohamed Alajmi, Mukesh Joshi, Phool Hasan, Mohammad Abid, Shailja Singh,

To combat the emergence of drug resistance against the existing antimalarials, novel side chain containing 7-chloroquinoline-indole-chalcones tethered with a triazole (CQTrICh-analogs 7 (a-s) and 9) were designed and synthesized by reacting substituted 1-phenyl-3-(1-(prop-2-yn-1- yl)-1H-indol-3-yl) prop-2-en-1-one and 1-(prop-2-yn-1-yl)-1H-indole-3-carbaldehyde with 4- azido-7-chloroquinoline, respectively via a ‘click’ reaction. The selected CQTrICh-analogs: 7l and ... Read more >>

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Multistage and transmission-blocking tubulin targeting potent antimalarial discovered from the open access MMV pathogen box.

Geeta Kumari, Ravi Jain, Raj Kumar Sah, Inderjeet Kalia, Manu Vashistha, Pooja Singh, Agam Prasad Singh, Kirandeep Samby, Jeremy Burrows, Shailja Singh,

The development of resistance to current antimalarial therapies remains a significant source of concern. To address this risk,newdrugswithnoveltargetsin distinct developmental stages ofPlasmodiumparasites are required. In the current study,we have targetedP. falciparumTubulin(PfTubulin)proteins which represent some of thepotentialdrug targetsfor malaria chemotherapy. PlasmodialMicrotubules (MTs) play a crucial role during parasite proliferation, growth, and ... Read more >>

Biochem Pharmacol (Biochemical pharmacology)
[2022, 203:115154]

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