{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,9]],"date-time":"2025-11-09T07:45:18Z","timestamp":1762674318686,"version":"3.41.2"},"reference-count":36,"publisher":"Wiley","issue":"6","license":[{"start":{"date-parts":[[2019,5,8]],"date-time":"2019-05-08T00:00:00Z","timestamp":1557273600000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/100000002","name":"National Institutes of Health","doi-asserted-by":"publisher","award":["R01 AI104416"],"award-info":[{"award-number":["R01 AI104416"]}],"id":[{"id":"10.13039\/100000002","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Archiv der Pharmazie"],"published-print":{"date-parts":[[2019,6]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>Tuberculosis is the \u201cAchilles heel\u201d of the human immunodeficiency (HIV) ministration. HIV\u2010positive people are 16\u201327 times more prone to contract tuberculosis. But the adverse interaction between antiretroviral drugs and antitubercular drugs has made it necessary to look for a single drug regimen for HIV\u2010TB coinfection. Piperidine derivatives have been reported as anti\u2010HIV and anti\u2010TB agents. This inspired us to design, synthesize, and characterize a series of 3,5\u2010bis(furan\u20102\u2010ylmethylidene)\u2010piperidin\u20104\u2010substituted imines (<jats:bold>R1\u2010R25<\/jats:bold>) and these were further screened for in vitro antitubercular activity against <jats:italic>Mycobacterium tuberculosis<\/jats:italic> H37Rv and anti\u2010HIV activity. Molecular docking studies showed energetically favorable binding interactions with both EACP reductase (1ZID.pdb) and reverse\u2010transcriptase (1REV.pdb) targets. The compounds <jats:bold>R7<\/jats:bold>, <jats:bold>R12<\/jats:bold>, <jats:bold>R17<\/jats:bold>, <jats:bold>R18<\/jats:bold>, <jats:bold>R19<\/jats:bold>, <jats:bold>R20<\/jats:bold> were found to be more potent as anti\u2010TB agents than ethambutol (MIC 3.125\u2009\u03bcg\/ml). Compound <jats:bold>R7<\/jats:bold> was found to be moderately active with an IC<jats:sub>50<\/jats:sub> of 2.1\u2009\u00b1\u20090.04\u2009\u03bcM in multicycle infection assays, in comparison with the standard drug, zidovudine (IC<jats:sub>50<\/jats:sub>\u2009=\u20095.7\u2009\u00b1\u20090.04\u2009nM), used as anti\u2010HIV drug. The cytotoxicity assay was done on Vero, MT\u20102, and TZM\u2010bl cells to assess the safety of these compounds and they were found to be safe. From the above results, <jats:bold>R7<\/jats:bold> seems to be a promising lead for anti\u2010HIV and anti\u2010TB activity.<\/jats:p>","DOI":"10.1002\/ardp.201800358","type":"journal-article","created":{"date-parts":[[2019,5,8]],"date-time":"2019-05-08T08:24:04Z","timestamp":1557303844000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["Targeting HIV\u2010TB coinfection by developing novel piperidin\u20104\u2010substituted imines: Design, synthesis, in vitro and in silico studies"],"prefix":"10.1002","volume":"352","author":[{"given":"Avinash","family":"Kumar","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry Manipal College of Pharmaceutical Sciences, MAHE Manipal India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rajappan","family":"Revathi","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Manipal College of Pharmaceutical Sciences, MAHE Manipal India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dharmarajan","family":"Sriram","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Birla Institute of Technology &amp; Science\u2010Pilani Hyderabad India"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Francesca","family":"Curreli","sequence":"additional","affiliation":[{"name":"Laboratory of Molecular Modeling and Drug Design, Kimball Research Institute of the New York Blood Centre New York NY"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Asim K.","family":"Debnath","sequence":"additional","affiliation":[{"name":"Laboratory of Molecular Modeling and Drug Design, Kimball Research Institute of the New York Blood Centre New York NY"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"K. 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