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Syntheses are described for penicillins (4b~4i, 5a and 5b) which possess a 6/?-(2-heteroaryl-3-substituted)-propenarnido side-chain of fixed geometry. In vitro results for these compounds against a range of Gram-positive and Gram-negative bacteria showedin most cases good stability against both penicillinase and TEM-1 /Mactamase; analogues (4b~4i) bearing a 2-(2-aminothiazol-4-yl) unit showed the best intrinsic activity, the cyclohexyl compound (4b) being the most promising. The 1-acetoxyethyl ester (6) of 4b was also prepared; in experimental animal studies the in vivo properties of this compoundcompared favourably with cefuroxime axetil and are reported together with selected in vivo data for the other compounds.
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
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