- Synthesis and antibacterial activity of pyrimidinylureidopenicillins
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The 6R-[(R)-2-[3-[5-pyrimidinyl]ureido]-2-(4-hydroxyphenyl)acetamido]-penicill anic acids, prepared by two synthetic routes, exhibit broad antimicrobial activity against Gram-positive and Gram-negative bacteria. Their structure-activity relationships are discussed. 6R-[(R)-2-[3-[2-(p-aminosulfonyl)anilino-4-hydroxy-5-pyrimidinyl]ureido]-2 -(4-hydroxyphenyl)acetamido]-penicillanic acid, sodium salt (VX-VC 43), the most active compound, shows very low MIC (minimal inhibitory concentration) values against clinically important Gram-negative bacteria, primarily Pseudomonas aeruginosa.
- Wetzel,Woitun,Reuter,Maier,Lechner
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p. 343 - 348
(2007/10/02)
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