{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,2]],"date-time":"2026-09-02T15:17:43Z","timestamp":1788362263087,"version":"build-2803163510"},"reference-count":32,"publisher":"American Chemical Society (ACS)","issue":"3","license":[{"start":{"date-parts":[[2018,3,14]],"date-time":"2018-03-14T00:00:00Z","timestamp":1520985600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/pubs.acs.org\/page\/policy\/authorchoice_termsofuse.html"}],"funder":[{"DOI":"10.13039\/501100001409","name":"Department of Science and Technology, Ministry of Science and Technology","doi-asserted-by":"publisher","award":["SR\/FTP\/CS-12\/2006"],"award-info":[{"award-number":["SR\/FTP\/CS-12\/2006"]}],"id":[{"id":"10.13039\/501100001409","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2018,3,31]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>In the search of therapeutic agents for emerging drug-resistant parasites, the synthesis of newer classes of 8-quinolinamines has emerged as a successful chemotherapeutic approach. We report synthesis of 8-quinolinamines bearing 5-alkoxy, 4-methyl, and 2-tert-butyl groups in the quinoline framework and their amino acid conjugates as broad-spectrum anti-infectives. 8-Quinolinamines exhibited potent in vitro antimalarial activity [IC50 = 20\u20134760 ng\/mL (drug-sensitive Plasmodium falciparum D6 strain) and IC50 = 22\u20134760 ng\/mL (drug-resistant P. falciparum W2 strain)]. The most promising analogues have cured all animals at 25 mg\/kg\/day against drug-sensitive Plasmodium berghei and at 50 mg\/kg\/day against multidrug-resistant Plasmodium yoelii nigeriensis infections in Swiss mice. The in vitro antileishmanial activities (IC50 = 0.84\u20135.0 \u03bcg\/mL and IC90 = 1.95\u20137.0 \u03bcg\/mL) comparable to standard drug pentamidine were exhibited by several of the synthesized 8-quinolinamines. At the same time, very promising antifungal activities (Candida albicans\u2500IC50 = 4.93\u201319.38 \u03bcg\/mL; Candida glabrata\u2500IC50 = 3.96\u201319.22 \u03bcg\/mL; Candida krusei\u2500IC50 = 2.89\u201318.95 \u03bcg\/mL; Cryptococcus neoformans\u2500IC50 = 0.67\u201318.64 \u03bcg\/mL; and Aspergillus fumigatus\u2500IC50 = 6.0\u201319.32 \u03bcg\/mL) and antibacterial activities (Staphylococcus aureus\u2500IC50 = 1.33\u201318.9 \u03bcg\/mL; methicillin-resistant S. aureus\u2500IC50 = 1.38\u201315.34 \u03bcg\/mL; and Mycobacterium intracellulare\u2500IC50 = 3.12\u201320 \u03bcg\/mL) were also observed. None of the 8-quinolinamines exhibited cytotoxicity and therefore are a promising structural class of compounds as antiparasitic and antimicrobials.<\/jats:p>","DOI":"10.1021\/acsomega.7b02047","type":"journal-article","created":{"date-parts":[[2018,3,14]],"date-time":"2018-03-14T09:02:20Z","timestamp":1521018140000},"page":"3060-3075","source":"Crossref","is-referenced-by-count":11,"title":["Synthesis and Biological Evaluation\nof 8-Quinolinamines\nand Their Amino Acid Conjugates as Broad-Spectrum Anti-infectives"],"prefix":"10.1021","volume":"3","author":[{"given":"Meenakshi","family":"Jain","sequence":"first","affiliation":[{"name":"National Institute of Pharmaceutical Education and Research , , Sector 67, S. A. S. Nagar , ,","place":["Punjab, India, 160 062"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"C. V. Ravi P.","family":"Reddy","sequence":"additional","affiliation":[{"name":"National Institute of Pharmaceutical Education and Research , , Sector 67, S. A. S. Nagar , ,","place":["Punjab, India, 160 062"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Moumita","family":"Halder","sequence":"additional","affiliation":[{"name":"National Institute of Pharmaceutical Education and Research , , Sector 67, S. A. S. Nagar , ,","place":["Punjab, India, 160 062"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Savita","family":"Singh","sequence":"additional","affiliation":[{"name":"National Institute of Pharmaceutical Education and Research , , Sector 67, S. A. S. Nagar , ,","place":["Punjab, India, 160 062"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Randheer","family":"Kumar","sequence":"additional","affiliation":[{"name":"National Institute of Pharmaceutical Education and Research , , Sector 67, S. A. S. Nagar , ,","place":["Punjab, India, 160 062"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sagar Gajbe","family":"Wasudeo","sequence":"additional","affiliation":[{"name":"National Institute of Pharmaceutical Education and Research , , Sector 67, S. A. S. Nagar , ,","place":["Punjab, India, 160 062"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Prati Pal","family":"Singh","sequence":"additional","affiliation":[{"name":"National Institute of Pharmaceutical Education and Research , , Sector 67, S. A. S. Nagar , ,","place":["Punjab, India, 160 062"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shabana I.","family":"Khan","sequence":"additional","affiliation":[{"name":"The University of Mississippi , , University, , ,","place":["Oxford, Mississippi, United States, 38677"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Melissa R.","family":"Jacob","sequence":"additional","affiliation":[{"name":"The University of Mississippi , , University, , ,","place":["Oxford, Mississippi, United States, 38677"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Babu L.","family":"Tekwani","sequence":"additional","affiliation":[{"name":"The University of Mississippi , , University, , ,","place":["Oxford, Mississippi, United States, 38677"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9180-2812","authenticated-orcid":true,"given":"Rahul","family":"Jain","sequence":"additional","affiliation":[{"name":"National Institute of Pharmaceutical Education and Research , , Sector 67, S. A. S. Nagar , ,","place":["Punjab, India, 160 062"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2018,3,14]]},"reference":[{"key":"2026090210455862000_cit1","doi-asserted-by":"publisher","first-page":"S14","DOI":"10.1038\/484s14a","article-title":"The numbers\ngame","volume":"484","author":"Shetty","year":"2012","journal-title":"Nature"},{"key":"2026090210455862000_cit2","unstructured":"World Health Organization (WHO).\n          .  World Malaria Report, 2017. http:\/\/www.who.int\/malaria\/publications\/world-malaria-report-2017\/en\/."},{"key":"2026090210455862000_cit3","unstructured":"World Health Organization (WHO).\n          .  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