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Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based Chlamydia trachomatis inhibitors
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- Kulén, Martina (author)
- Umeå universitet,Kemiska institutionen,Umeå Centre for Microbial Research (UCMR),Umea Univ, Dept Chem, S-90187 Umea, Sweden;Umea Univ, Umea Ctr Microbial Res, S-90187 Umea, Sweden
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- Núñez-Otero, Carlos, 1992- (author)
- Umeå universitet,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS),Institutionen för klinisk mikrobiologi,Umea Univ, Umea Ctr Microbial Res, S-90187 Umea, Sweden;Umea Univ, Lab Mol Infect Med Sweden MIMS, S-90187 Umea, Sweden;Umea Univ, Dept Clin Microbiol, S-90185 Umea, Sweden
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- Cairns, Andrew G. (author)
- Umeå universitet,Kemiska institutionen,Umeå Centre for Microbial Research (UCMR),Umea Univ, Dept Chem, S-90187 Umea, Sweden;Umea Univ, Umea Ctr Microbial Res, S-90187 Umea, Sweden
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- 2019
- 2019
- English.
- In: MedChemComm. - : Royal Society of Chemistry. - 2040-2503 .- 2040-2511. ; 10:11, s. 1966-1987
- Journal article (peer-reviewed)
Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
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