{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,1,21]],"date-time":"2026-01-21T04:36:12Z","timestamp":1768970172882,"version":"3.49.0"},"reference-count":68,"publisher":"MDPI AG","issue":"4","license":[{"start":{"date-parts":[[2021,2,20]],"date-time":"2021-02-20T00:00:00Z","timestamp":1613779200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>The cell wall of Mycobacterium tuberculosis (Mtb) has a unique structural organisation, comprising a high lipid content mixed with polysaccharides. This makes cell wall a formidable barrier impermeable to hydrophilic agents. In addition, during host infection, Mtb resides in macrophages within avascular necrotic granulomas and cavities, which shield the bacterium from the action of most antibiotics. To overcome these protective barriers, a new class of anti-TB agents exhibiting lipophilic character have been recommended by various reports in literature. Herein, a series of lipophilic heterocyclic quinolone compounds was synthesised and evaluated in vitro against pMSp12::GFP strain of Mtb, two protozoan parasites (Plasmodium falciparum and Trypanosoma brucei brucei) and against ESKAPE pathogens. The resultant compounds exhibited varied anti-Mtb activity with MIC90 values in the range of 0.24\u201331 \u00b5M. Cross-screening against P. falciparum and T.b. brucei, identified several compounds with antiprotozoal activities in the range of 0.4\u201320 \u00b5M. Compounds were generally inactive against ESKAPE pathogens, with only compounds 8c, 8g and 13 exhibiting moderate to poor activity against S. aureus and A. baumannii.<\/jats:p>","DOI":"10.3390\/molecules26041141","type":"journal-article","created":{"date-parts":[[2021,2,21]],"date-time":"2021-02-21T22:04:15Z","timestamp":1613945055000},"page":"1141","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Easy-To-Access Quinolone Derivatives Exhibiting Antibacterial and Anti-Parasitic Activities"],"prefix":"10.3390","volume":"26","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-6282-043X","authenticated-orcid":false,"given":"Richard M.","family":"Beteck","sequence":"first","affiliation":[{"name":"Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Audrey","family":"Jordaan","sequence":"additional","affiliation":[{"name":"SAMRC\/NHLS\/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, Faculty of Health Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town 7925, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ronnett","family":"Seldon","sequence":"additional","affiliation":[{"name":"SAMRC Drug Discovery and Development Research Unit, University of Cape Town, Cape Town 7700, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2734-0999","authenticated-orcid":false,"given":"Dustin","family":"Laming","sequence":"additional","affiliation":[{"name":"Centre for Chemico- and Biomedicinal Research, Rhodes University, Makhanda 6140, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4409-1955","authenticated-orcid":false,"given":"Heinrich C.","family":"Hoppe","sequence":"additional","affiliation":[{"name":"Centre for Chemico- and Biomedicinal Research, Rhodes University, Makhanda 6140, South Africa"},{"name":"Department of Biochemistry and Microbiology, Faculty of Science, Rhodes University, Makhanda 6140, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4146-0930","authenticated-orcid":false,"given":"Digby F.","family":"Warner","sequence":"additional","affiliation":[{"name":"SAMRC\/NHLS\/UCT Molecular Mycobacteriology Research Unit, Department of Pathology, Faculty of Health Sciences, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town 7925, South Africa"},{"name":"Wellcome Centre for Infectious Diseases Research in Africa, University of Cape Town, Cape Town 7925, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0725-5738","authenticated-orcid":false,"given":"Setshaba D.","family":"Khanye","sequence":"additional","affiliation":[{"name":"Centre for Chemico- and Biomedicinal Research, Rhodes University, Makhanda 6140, South Africa"},{"name":"Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Rhodes University, Makhanda 6140, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2021,2,20]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"6","DOI":"10.1111\/imr.12264","article-title":"Co-evolution of Mycobacterium tuberculosis and Homo sapiens","volume":"264","author":"Brites","year":"2015","journal-title":"Immunol. 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