{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,23]],"date-time":"2026-10-23T21:45:51Z","timestamp":1792791951331,"version":"4.5.0"},"reference-count":15,"publisher":"American Society for Microbiology","issue":"4","license":[{"start":{"date-parts":[[2000,4,1]],"date-time":"2000-04-01T00:00:00Z","timestamp":954547200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2000,4]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n                  <jats:p>\n                    Mefloquine was found to have bactericidal activity against methicillin- and fluoroquinolone-susceptible and -resistant strains of\n                    <jats:italic>Staphylococcus aureus<\/jats:italic>\n                    and\n                    <jats:italic>Staphylococcus epidermidis<\/jats:italic>\n                    and gentamicin- and vancomycin-resistant strains of\n                    <jats:italic>Enterococcus faecalis<\/jats:italic>\n                    and\n                    <jats:italic>Enterococcus faecium<\/jats:italic>\n                    . The MICs were 16 \u03bcg\/ml, and the minimal bactericidal concentrations (MBCs) were 16 to 32 \u03bcg\/ml. These concentrations cannot be achieved in serum. Mefloquine was active at a more achievable concentration against penicillin-susceptible and -resistant\n                    <jats:italic>Streptococcus pneumoniae<\/jats:italic>\n                    , with MICs of 0.2 to 1.5 \u03bcg\/ml. Mefloquine was not active against gram-negative bacteria and yeasts. In an attempt to find more active derivatives, 400 mefloquine-related compounds were selected from the chemical inventory of The Walter Reed Army Institute of Research. We identified a series of compounds containing a piperidine methanol group attached to pyridine, quinoline, and benzylquinoline ring systems. These had activities similar to that of mefloquine against\n                    <jats:italic>S. pneumoniae<\/jats:italic>\n                    but were far more active against other gram-positive bacteria (MICs for staphylococci, 0.8 to 6.3 \u03bcg\/ml). They had activities similar to that of amphotericin B against\n                    <jats:italic>Candida<\/jats:italic>\n                    spp. and\n                    <jats:italic>Cryptococcus neoformans<\/jats:italic>\n                    . Combinations of the compounds with gentamicin and vancomycin were additive against staphylococci and pneumococci. The MIC and MBC of gentamicin were decreased by four- to eightfold when this drug was combined with limiting dilutions of the compounds. There was no antagonism with other antimicrobial drugs. The compounds were rapidly bactericidal. They appear to act by disrupting cell membranes. Combinations of the compounds with aminoglycoside antibiotics may have potential for therapeutic use.\n                  <\/jats:p>","DOI":"10.1128\/aac.44.4.848-852.2000","type":"journal-article","created":{"date-parts":[[2002,7,27]],"date-time":"2002-07-27T06:06:42Z","timestamp":1027750002000},"page":"848-852","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":92,"title":["Antimicrobial Activities of Mefloquine and a Series of Related Compounds"],"prefix":"10.1128","volume":"44","author":[{"given":"C. M.","family":"Kunin","sequence":"first","affiliation":[{"name":"<!--label omitted: 1-->Department of Internal Medicine, The Ohio State University, Columbus, Ohio,1 and"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"W. Y.","family":"Ellis","sequence":"additional","affiliation":[{"name":"<!--label omitted: 2-->The Walter Reed Army Institute of Research, Washington, D.C.2"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.43.8.1870"},{"key":"e_1_3_2_3_2","first-page":"387","article-title":"In vitro susceptibility of selected non-protozoa to mefloquine.","volume":"40","author":"Bromke B. J.","year":"1993","unstructured":"Bromke B. J. McGinn M. In vitro susceptibility of selected non-protozoa to mefloquine. Acta Microbiol. Hung. 40 1993 387 389","journal-title":"Acta Microbiol. 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G.\n          Goodman and Gilman's the pharmacologic basis of therapeutics\n          8th ed.\n          1993\n          McGraw-Hill Book Co.\n          New York N.Y"},{"key":"e_1_3_2_8_2","doi-asserted-by":"publisher","DOI":"10.1128\/jb.169.5.2322-2325.1987"},{"key":"e_1_3_2_9_2","doi-asserted-by":"crossref","first-page":"11","DOI":"10.1016\/0732-8893(95)00148-4","article-title":"Antigonococcal activity of 11 drugs used for therapy or prophylaxis of malaria.","volume":"23","author":"Mehaffy P. C.","year":"1995","unstructured":"Mehaffy P. C. Barrett M. S. Putnam S. D. Jones R. N. Antigonococcal activity of 11 drugs used for therapy or prophylaxis of malaria. Diagn. Microbiol. Infect. Dis. 23 1995 11 13","journal-title":"Diagn. Microbiol. Infect. 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The crisis in antibiotic resistance. Science 157 1992 1064 1073","journal-title":"Science"},{"key":"e_1_3_2_14_2","unstructured":"Sambrook\n              J.\n              Fritsch\n              E. F.\n              Maniatis\n              T.\n          Molecular cloning: a laboratory manual\n          2nd ed.\n          1989\n          Cold Spring Harbor Laboratory Press\n          Cold Spring Harbor N.Y"},{"key":"e_1_3_2_15_2","doi-asserted-by":"crossref","first-page":"399","DOI":"10.4269\/ajtmh.1997.57.399","article-title":"Comparison of whole blood and serum levels of mefloquine and its carboxylic acid derivative.","volume":"57","author":"Todd G. D.","year":"1997","unstructured":"Todd G. D. Hopperus Buma A. P. Green M. D. Jaspers C. A. Lobel H. O. Comparison of whole blood and serum levels of mefloquine and its carboxylic acid derivative. Am. J. Trop. Med. Hyg. 57 1997 399 402","journal-title":"Am. J. Trop. Med. Hyg."},{"key":"e_1_3_2_16_2","doi-asserted-by":"crossref","first-page":"615","DOI":"10.1007\/s002280050523","article-title":"Lack of bioequivalence of a generic mefloquine tablet with the standard product.","volume":"54","author":"Weidekamm E.","year":"1998","unstructured":"Weidekamm E. Rusing G. Caplain H. Sorgel F. Crevoisier C. Lack of bioequivalence of a generic mefloquine tablet with the standard product. Eur. J. Clin. Pharmacol. 54 1998 615 619","journal-title":"Eur. J. Clin. 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