Search: onr:"swepub:oai:DiVA.org:umu-119066" >
Thiazolino 2-Pyrido...
Thiazolino 2-Pyridone Amide Inhibitors of Chlamydia trachomatis Infectivity
-
- Good, James A. D., 1985- (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.
-
- Silver, Jim, 1975- (author)
- Umeå universitet,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS),Institutionen för molekylärbiologi (Medicinska fakulteten),Umea Univ, Umea Ctr Microbial Res, S-90187 Umea, Sweden.;Umea Univ, Dept Mol Biol, S-90187 Umea, Sweden.;Umea Univ, Lab Mol Infect Med Sweden MIMS, S-90187 Umea, Sweden.
-
- Núñez-Otero, Carlos, 1992- (author)
- Umeå universitet,Institutionen för klinisk mikrobiologi,Umea Univ, Dept Clin Microbiol, S-90185 Umea, Sweden.
-
show more...
-
- Bahnan, Wael, 1985- (author)
- Umeå universitet,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS),Institutionen för molekylärbiologi (Medicinska fakulteten),Umea Univ, Umea Ctr Microbial Res, S-90187 Umea, Sweden.;Umea Univ, Dept Mol Biol, S-90187 Umea, Sweden.;Umea Univ, Lab Mol Infect Med Sweden MIMS, S-90187 Umea, Sweden.
-
- Krishnan, K. Syam (author)
- Umeå universitet,Umeå Centre for Microbial Research (UCMR),Kemiska institutionen,Umea Univ, Dept Chem, S-90187 Umea, Sweden.;Umea Univ, Umea Ctr Microbial Res, S-90187 Umea, Sweden.;Mannam Mem NSS Coll, Dept Chem, Kollam 691571, Kerala, India.
-
- Salin, Olli (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.
-
- Engström, Patrik (author)
- Umeå universitet,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS),Institutionen för molekylärbiologi (Medicinska fakulteten),Umea Univ, Umea Ctr Microbial Res, S-90187 Umea, Sweden.;Umea Univ, Dept Mol Biol, S-90187 Umea, Sweden.;Umea Univ, Lab Mol Infect Med Sweden MIMS, S-90187 Umea, Sweden.;Univ Calif Berkeley, Dept Mol & Cell Biol, Berkeley, CA 94720 USA.
-
- Svensson, Richard (author)
- Uppsala universitet,Institutionen för farmaci
-
- Artursson, Per (author)
- Uppsala universitet,Institutionen för farmaci
-
- Gylfe, Åsa, 1972- (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.
-
- Bergström, Sven (author)
- Umeå universitet,Umeå Centre for Microbial Research (UCMR),Molekylär Infektionsmedicin, Sverige (MIMS),Institutionen för molekylärbiologi (Medicinska fakulteten),Umea Univ, Umea Ctr Microbial Res, S-90187 Umea, Sweden.;Umea Univ, Dept Mol Biol, S-90187 Umea, Sweden.;Umea Univ, Lab Mol Infect Med Sweden MIMS, S-90187 Umea, Sweden.
-
- Almqvist, Fredrik, 1967- (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.
-
show less...
-
(creator_code:org_t)
- 2016-02-22
- 2016
- English.
-
In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 59:5, s. 2094-2108
- Related links:
-
https://urn.kb.se/re...
-
show more...
-
https://doi.org/10.1...
-
https://urn.kb.se/re...
-
show less...
Abstract
Subject headings
Close
- The bacterial pathogen Chlamydia trachomatis is a global health burden currently treated with broad-spectrum antibiotics which disrupt commensal bacteria. We recently identified a compound through phenotypic screening that blocked infectivity of this intracellular pathogen without host cell toxicity (compound 1, KSK 120). Herein, we present the optimization of 1 to a class of thiazolino 2-pyridone amides that are highly efficacious (EC50 <= 100 nM) in attenuating infectivity across multiple serovars of C. trachomatis without host cell toxicity. The lead compound 21a exhibits reduced lipophilicity versus 1 and did not affect the growth or viability of representative commensal flora at 50 mu M. In microscopy studies, a highly active fluorescent analogue 37 localized inside the parasitiphorous inclusion, indicative of a specific targeting of bacterial components. In summary, we present a class of small molecules to enable the development of specific treatments for C. trachomatis.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Mikrobiologi inom det medicinska området (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Microbiology in the medical area (hsv//eng)
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
Find in a library
To the university's database
- By the author/editor
-
Good, James A. D ...
-
Silver, Jim, 197 ...
-
Núñez-Otero, Car ...
-
Bahnan, Wael, 19 ...
-
Krishnan, K. Sya ...
-
Salin, Olli
-
show more...
-
Engström, Patrik
-
Svensson, Richar ...
-
Artursson, Per
-
Gylfe, Åsa, 1972 ...
-
Bergström, Sven
-
Almqvist, Fredri ...
-
show less...
- About the subject
-
- MEDICAL AND HEALTH SCIENCES
-
MEDICAL AND HEAL ...
-
and Basic Medicine
-
and Microbiology in ...
-
- NATURAL SCIENCES
-
NATURAL SCIENCES
-
and Biological Scien ...
-
and Biochemistry and ...
-
- MEDICAL AND HEALTH SCIENCES
-
MEDICAL AND HEAL ...
-
and Basic Medicine
-
and Pharmaceutical S ...
- Articles in the publication
-
Journal of Medic ...
- By the university
-
Umeå University
-
Uppsala University