{"entity": "researcher", "timestamp": "2026-09-28T11:18:22.180Z", "family": "N\u00fa\u00f1ez-Otero", "given": "Carlos", "initials": "C", "orcid": "0000-0001-7680-0918", "affiliations": ["Ume\u00e5 Centre for Microbial Research , Ume\u00e5 University , 901 87 Ume\u00e5 , Sweden . Email: sven.bergstrom@umu.se ; Email: asa.gylfe@umu.se.", "Laboratory for Molecular Infection Medicine Sweden (MIMS) , Ume\u00e5 University , 901 87 Ume\u00e5 , Sweden.", "Department of Clinical microbiology , Ume\u00e5 University , 901 85 Ume\u00e5 , Sweden."], "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/researcher/b07ebbd0d05548e38572280ccf676d6d.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/researcher/b07ebbd0d05548e38572280ccf676d6d"}}, "publications": [{"entity": "publication", "iuid": "fb74e61f8a7d447188101d84b51b5740", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/fb74e61f8a7d447188101d84b51b5740.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/fb74e61f8a7d447188101d84b51b5740"}}, "title": "Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based Chlamydia trachomatis inhibitors.", "authors": [{"family": "Kul\u00e9n", "given": "Martina", "initials": "M"}, {"family": "N\u00fa\u00f1ez-Otero", "given": "Carlos", "initials": "C", "orcid": "0000-0001-7680-0918", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/b07ebbd0d05548e38572280ccf676d6d.json"}}, {"family": "Cairns", "given": "Andrew G", "initials": "AG"}, {"family": "Silver", "given": "Jim", "initials": "J"}, {"family": "Lindgren", "given": "Anders E G", "initials": "AEG"}, {"family": "Wede", "given": "Emma", "initials": "E"}, {"family": "Singh", "given": "Pardeep", "initials": "P"}, {"family": "Vielfort", "given": "Katarina", "initials": "K"}, {"family": "Bahnan", "given": "Wael", "initials": "W"}, {"family": "Good", "given": "James A D", "initials": "JAD"}, {"family": "Svensson", "given": "Richard", "initials": "R"}, {"family": "Bergstr\u00f6m", "given": "Sven", "initials": "S"}, {"family": "Gylfe", "given": "\u00c5sa", "initials": "\u00c5"}, {"family": "Almqvist", "given": "Fredrik", "initials": "F"}], "type": "journal article", "published": "2019-11-01", "journal": {"title": "Med. Chem. Commun.", "issn": "2040-2511", "volume": "10", "issue": "11", "pages": "1966-1987", "issn-l": "2040-2503"}, "abstract": "Chlamydia trachomatis infections are a global health problem and new approaches to treat C. trachomatis with drugs of high specificity would be valuable. A library of substituted ring fused 2-pyridones has been synthesized and evaluated for their ability to attenuate C. trachomatis infectivity. In vivo pharmacokinetic studies were performed, with the best candidates demonstrating that a C8-methylsulfonamide substituent improved pharmacokinetic properties important for oral administration. C8-Methyl sulfonamide analogue 30 inhibited C. trachomatis infectivity in low micromolar concentrations. Further pharmacokinetic evaluation at an oral dose of 10 mg kg-1 showed an apparent bioavailability of 41%, compared to C8-cyclopropyl and -methoxy analogues which had negligible oral uptake. In vitro ADME (absorption, distribution, metabolism and excretion) testing of solubility and Caco-2 cell permeability revealed that both solubility and permeability is greatly improved with the C8-methyl sulfonamide 30, effectively moving it from BCS (Biopharmaceutical Classification System) class IV to II.", "doi": "10.1039/c9md00405j", "pmid": "32206238", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC7069368"}, {"db": "pii", "key": "c9md00405j"}], "notes": [], "created": "2026-09-23T13:07:00.549Z", "modified": "2026-09-23T13:07:00.610Z"}]}