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A new imidazopyridine chemotype has been envisaged through scaffold\u2010hopping approach combined with docking studies for putative\u2010binding interactions with <jats:italic>Plasmodium falciparum<\/jats:italic> phosphatidylinositol\u20104\u2010kinase (<jats:italic>Pf<\/jats:italic>PI4K) target. The docking results steered to the synthesis of compound <jats:bold>1<\/jats:bold> [5\u2010(3\u2010(methylsulfonyl)phenyl)\u20103\u2010(4\u2010(methylsulfonyl)phenyl)\u20103<jats:italic>H<\/jats:italic>\u2010imidazo[4,5\u2010<jats:italic>b<\/jats:italic>]pyridine] followed by the in vitro screening for antiplasmodial activity and ADME\u2010PK studies. Combined with potent antimalarial activity of compound <jats:bold>1<\/jats:bold> (<jats:italic>Pf<\/jats:italic>3D7 IC<jats:sub>50<\/jats:sub>\u00a0=\u200929\u2009nM) with meager in vitro intrinsic clearance, moderate plasma\u2010protein binding, and acceptable permeability, compound <jats:bold>1<\/jats:bold> displayed sustained exposure and high oral bioavailability in mice and can thus have the potential as next generation PI4K inhibitor for in vivo studies.<\/jats:p>","DOI":"10.1111\/cbdd.14170","type":"journal-article","created":{"date-parts":[[2022,11,2]],"date-time":"2022-11-02T15:03:55Z","timestamp":1667401435000},"page":"690-695","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["Identification of 5\u2010(3\u2010(methylsulfonyl)phenyl)\u20103\u2010(4\u2010(methylsulfonyl)phenyl)\u2010<scp>3<\/scp><i>H<\/i>\u2010imidazo[4,5\u2010<i>b<\/i>]pyridine as novel orally bioavailable and metabolically stable antimalarial compound for further exploration"],"prefix":"10.1111","volume":"101","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0907-6699","authenticated-orcid":false,"given":"Mrinalkanti","family":"Kundu","sequence":"first","affiliation":[{"name":"TCG Lifesciences Pvt. 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