التفاصيل البيبلوغرافية
العنوان:
MexAB-OprM-Specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 1: Discovery and early strategies for lead optimization
المؤلفون:
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
المصدر:
Bioorganic & Medicinal Chemistry Letters . 13:4201-4204
بيانات النشر:
Elsevier BV, 2003.
سنة النشر:
2003
مصطلحات موضوعية:
Neutropenia , Lactams , Clinical Biochemistry , Biological Transport, Active , Pharmaceutical Science , Diaphragm pump , Microbial Sensitivity Tests , medicine.disease_cause , Biochemistry , Mice , Structure-Activity Relationship , In vivo , Sepsis , Drug Discovery , medicine , Animals , Molecular Biology , Serum Albumin , Antibacterial agent , biology , Pseudomonas aeruginosa , Chemistry , Organic Chemistry , Membrane Transport Proteins , Drug Resistance, Microbial , Gene Expression Regulation, Bacterial , biology.organism_classification , In vitro , Anti-Bacterial Agents , Pseudomonadales , Molecular Medicine , Efflux , Carrier Proteins , Bacterial Outer Membrane Proteins , Protein Binding , Pseudomonadaceae
الوصف:
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 activity in animal models, and efforts to improve solubility and reduce serum protein binding by the introduction of polar groups are discussed.
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d452727d2a774f33b9b5ed19e7e931ef https://doi.org/10.1016/j.bmcl.2003.07.024
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....d452727d2a774f33b9b5ed19e7e931ef
قاعدة البيانات:
OpenAIRE
