WCK 4034: A promising oxazolidinone for treating gram positive infections
| Autor: | Satish Bhawsar, Shivaji Pawar, Prasad Deshpande, Ravindra Yeole, Rajesh Chavan, Manohar Nandanwar, Sachin Bhagwat, Mahesh Patel |
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| Rok vydání: | 2022 |
| Předmět: |
Methicillin-Resistant Staphylococcus aureus
Staphylococcus aureus Organic Chemistry Clinical Biochemistry Linezolid Pharmaceutical Science Microbial Sensitivity Tests Biochemistry Anti-Bacterial Agents Dogs Streptococcus pneumoniae Drug Discovery Molecular Medicine Animals Molecular Biology Oxazolidinones |
| Zdroj: | Bioorganicmedicinal chemistry letters. 71 |
| ISSN: | 1464-3405 |
| Popis: | Increased resistance to gram positive infections have highlighted the limitations of currently available drug treatments including penicillins, macrolides and glycopeptides. As an alternative to address these challenges; Linezolid, the first antibiotic from oxazolidinone class, have shown the promising activities against such infections, although associated toxicological issues limiting the use of linezolid for prolonged treatments. In order to circumvent disadvantages allied with the marketed drugs, we herein reporting the synthesis of WCK 4034, an oxazolidinone antibiotic through our structure activity relationship (SAR) program. Through this exercise, WCK 4034, has shown competitive MIC values against Methicillin Sensitive S. aureus (MSSA, Sta-001), Methicillin Resistant S. aureus (MRSA, Sta-032), S. pneumoniae ATCC 49619 and H. influenza ATCC 35054 species as like linezolid. Although with an additional advantage; WCK 4034 has been found superior during dog PK studies as compare to Linezolid. With the preliminary studies in our hand, we herein assuming these improved pharmacokinetic values would be helpful. Moreover, WCK 4034 has successfully completed pre-clinical studies and ready to enter the clinical space, and paved the way for in house development of other oxazolidinone NCEs. |
| Databáze: | OpenAIRE |
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