Výsledky vyhledávání - "Thomas E. Renau"

Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure–activity relationships of (N-methyl-piperazinyl)-containing derivatives

Autor: Aesop Cho, Nadeem Iqbal, Bonnie Kuo, Karen Lolans, Deidre Madsen, William J. Watkins, Negar Garizi, Rémy C. Lemoine, Renata Jankowska, Vickie Wong, Maria Ludwikow, Rajeshwar Singh, John Barnard, Lee Chong, Uma Oza, Michael N. Dudley, Thomas E. Renau, Olga Lomovskaya

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:5133-5137

Structure-activity relationships of a novel series of fungal efflux pump inhibitors with respect to potentiation of the activity of fluconazole against strains of Candida albicans and Candida glabrata over-expressing ABC-type efflux pumps are systema

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a828ac29246edd22634c41ef6029772b
https://doi.org/10.1016/j.bmcl.2004.07.071

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The relationship between physicochemical properties, In vitro activity and pharmacokinetic profiles of analogues of diamine-Containing efflux pump inhibitors

Autor: Yakira Landaverry, Nicole Williams, Suzanne Chamberland, Thomas E. Renau, Vrushali Tembe, Deidre Madsen, Roger Leger, Rose Yen, Keith Huie, Michael N. Dudley, Jason Z. Zhang, David A. Griffith, Renee Litman, William J. Watkins

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:4241-4244

Following the optimization of diamine-containing efflux pump inhibitors with respect to in vitro potentiation activity, in vivo stability and acute toxicity, we addressed the question of how to control the pharmacokinetic properties of the series. Up

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b42c96aabcbc333e3d3d025e836d8a54
https://doi.org/10.1016/j.bmcl.2003.07.030

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MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 2: achieving activity in vivo through the use of alternative scaffolds

Autor: Kumi Yoshida, Haruko Kawato, Yoshida Kenichi, William J. Watkins, Ving J. Lee, Yohei Ishida, Tsuyoshi Otani, Thomas E. Renau, Yoshihiro Yokomizo, Hiroko Ishida, Kazuki Hoshino, Masami Ohtsuka, Toshiharu Ohta, Yuichi Kurosaka, Kiyoshi Nakayama

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:4205-4208

Problems of low solubility, high serum protein binding, and lack of efficacy in vivo in first generation MexAB-OprM specific efflux pump inhibitors were addressed. Through the use of pharmacophore modelling, the key structural elements for pump inhib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ce3776787ba0face41d9b9b2e1c5165
https://doi.org/10.1016/j.bmcl.2003.07.027

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MexAB-OprM-Specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 1: Discovery and early strategies for lead optimization

Autor: Yoshida Kenichi, Shigeru Hosono, William J. Watkins, Haruko Kawato, Yoshihiro Yokomizo, Kiyoshi Nakayama, Kumi Yoshida, Toshiharu Ohta, Kazuki Hoshino, Roger Leger, Masami Ohtsuka, Ving J. Lee, Jason Z. Zhang, Yohei Ishida, Thomas E. Renau, Hiroko Ishida

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:4201-4204

The identification of a series of compounds that specifically inhibit efflux by the MexAB-OprM pump system in Pseudomonas aeruginosa is described. Synthesis and in vitro structure-activity relationships (SARs) are outlined. Early leads lacked activit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d452727d2a774f33b9b5ed19e7e931ef
https://doi.org/10.1016/j.bmcl.2003.07.024

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An Efficient Synthesis of 5-Bromopyridine-2-carbonitrile

Autor: Miroslav Rapta, David Y. Markevitch, Scott J. Hecker, Thomas E. Renau

Publikováno v: Synthetic Communications. 33:3285-3289

5-Bromopyridine-2-carbonitrile was efficiently synthesized in two steps from 2,5-dibromopyridine with an overall yield of 75%.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29aa91f3238168d765212c0a1b3a62db
https://doi.org/10.1081/scc-120023985

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Nonnucleoside Pyrrolopyrimidines with a Unique Mechanism of Action against Human Cytomegalovirus

Autor: Thomas E. Renau, M. Reza Nassiri, Leroy B. Townsend, Jennie G. Jacobson, Dominica G. Sweier, Julie M. Breitenbach, John C. Drach

Publikováno v: Antimicrobial Agents and Chemotherapy. 43:1888-1894

Based upon a prior study which evaluated a series of nonnucleoside pyrrolo[2,3- d ]pyrimidines as inhibitors of human cytomegalovirus (HCMV), we have selected three active analogs for detailed study. In an HCMV plaque-reduction assay, compounds 828,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b740ee7ce2a4a09d15865e8f3a1d611
https://doi.org/10.1128/aac.43.8.1888

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Structure-activity relationships of quinolone agents against mycobacteria: effect of structural modifications at the 8 position

Autor: Stephen J. Gracheck, John M. Domagala, Robert C. Reynolds, Gregory E. Roland, Julie A. Dever, Martin A. Shapiro, M R Jacobs, Thomas E. Renau, E. T. Joannides, Joseph P. Sanchez, Jeffrey W. Gage

Publikováno v: Antimicrobial Agents and Chemotherapy. 40:2363-2368

A series of quinolones with substitutions at the 8 position has been prepared as part of a study to examine the relationship between structural modifications at this position and activity against mycobacteria. The compounds were prepared by procedure

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e9e9c9ee18fab082ca1f24d37eb8490
https://doi.org/10.1128/aac.40.10.2363

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The synthesis of 3-bromo-2,4,5-trifluorobenzoic acid and its conversion to 8-bromoquinolonecarboxylic acids

Autor: Joseph P. Sanchez, John M. Domagala, Thomas E. Renau

Publikováno v: Journal of Heterocyclic Chemistry. 33:1407-1411

A series of 8-bromo-4-oxo-3-quinolinecarboxylic acids was prepared via the borate ester, 8. The key intermediate in the synthesis of the final products 10a-10d was 3-bromo-2,4,5-trifluorobenzoic acid (3), conveniently prepared in two steps from the k

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::795a7c7ab8e832746de02d91fa8308f8
https://doi.org/10.1002/jhet.5570330466

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Structure−Activity Relationships of the Quinolone Antibacterials against Mycobacteria: Effect of Structural Changes at N-1 and C-7

Autor: Martin A. Shapiro, Stephen J. Gracheck, Julie A. Dever, Thomas E. Renau, John M. Domagala, Joseph P. Sanchez, Jeffrey W. Gage

Publikováno v: Journal of Medicinal Chemistry. 39:729-735

The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has demonstrated the need for alternative chemotherapy against Mycobacterium tuberculosis. As part of a study to optimize the quinolone antibacterials agains

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::347e75ca02154daf9ecad9e09912a208
https://doi.org/10.1021/jm9507082

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