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Novel pleuromutilin derivatives with substituted 6-methylpyrimidine: Design, synthesis and antibacterial evaluation.

Abstract：

:A series of novel pleuromutilin derivatives with substituted 6-methylpyrimidine moieties was designed, synthesized, and evaluated for their antibacterial activities. Most of the tested compounds exhibited potent antibacterial activities against Staphylococcus aureus ATCC 25923 (S. aureus-25923), methicillin-resistant Staphylococcus epidermidis ATCC 51625 (MRSE-51625), methicillin-resistant Staphylococcus aureus BNCC 337371 (MRSA-337371), Streptococcus dysgalactiae (S. dysgalactiae) and Streptococcus agalactiae (S. agalactiae). Compounds 5c and 5g were the most active and displayed bacteriostatic activities against MRSA. In vivo mouse systemic infection experiment showed that 5c significantly improved the survival rate of mice (ED50 = 18.02 mg/kg), reduced the bacterial load and alleviated the pathological changes in the lungs of the affected mice.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Fan Y,Liu Y,Wang H,Shi T,Cheng F,Hao B,Yi Y,Shang R

doi

10.1016/j.ejmech.2020.112735

subject

Has Abstract

pub_date

2020-12-01 00:00:00

pages

112735

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)30707-8

journal_volume

207

pub_type

杂志文章

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