Synthesis and antibacterial activity of novel 4-pyrrolidinylthio carbapenems Part IV. 2-Alkyl substituents containing cationic heteroaromatics linked via a C-C bond
| العنوان: | Synthesis and antibacterial activity of novel 4-pyrrolidinylthio carbapenems Part IV. 2-Alkyl substituents containing cationic heteroaromatics linked via a C-C bond |
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| المؤلفون: | Shuichi Tawara, Fumiyuki Shirai, Hidenori Azami, Hiroshi Sasaki, Minoru Sakurai, Keiji Matsuda, David A. Barrett, Yoshimi Matsumoto, Takeshi Terasawa, Toshiyuki Chiba, Akira Tanaka |
| المصدر: | Bioorganicmedicinal chemistry. 9(4) |
| سنة النشر: | 2001 |
| مصطلحات موضوعية: | Staphylococcus aureus, Magnetic Resonance Spectroscopy, Pyrrolidines, Spectrophotometry, Infrared, Stereochemistry, Clinical Biochemistry, Substituent, Pharmaceutical Science, Microbial Sensitivity Tests, Biochemistry, Chemical synthesis, chemistry.chemical_compound, Mice, Structure-Activity Relationship, Dogs, Drug Discovery, Moiety, Animals, Humans, Pseudomonas Infections, Molecular Biology, Alkyl, Antibacterial agent, chemistry.chemical_classification, Mice, Inbred ICR, Bacteria, Organic Chemistry, Cationic polymerization, Haplorhini, Staphylococcal Infections, Anti-Bacterial Agents, Rats, chemistry, Carbapenems, Area Under Curve, Pseudomonas aeruginosa, Lactam, Molecular Medicine, Indicators and Reagents, Antibacterial activity, Bacterial Outer Membrane Proteins |
| الوصف: | The synthesis and biological activity of a novel series of 2-alkyl-4-pyrrolidinylthio-beta-methylcarbapenems containing a variety of cationic heteroaromatic substituents linked via a C-C bond is described. As a result of these studies, we selected FR21818 (In) as a candidate compound for development. FR21818 exhibited a well balanced spectrum of antibacterial activity, including Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus (MRSA), excellent urinary recovery, good stability against renal dehydropeptidase-I (DHP-I). no antigenicity and mutagenicity, weak toxicities, and good efficacy and therapeutic effect on mice systemic infections. Affinities to PBP's, permeability of outer membrane, and plasma levels in mice, dog, and cynomolgous monkey of FR21818 are also reported. |
| تدمد: | 0968-0896 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26dc49fdda65b8bc7f69c269ba3b7d85 https://pubmed.ncbi.nlm.nih.gov/11354680 |
| Rights: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....26dc49fdda65b8bc7f69c269ba3b7d85 |
| قاعدة البيانات: | OpenAIRE |
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