- Synthesis and Pharmacological Evaluation of a New Class of 2-(2-Aminothiazol-4-yl)-2-hydrazonoacetamido Cephalosporins
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A series of 2-(2-aminothiazol-4-yl)-2-hydrazonoacetamido cephalosporins 1a-h was prepared.Whenever possible, E and Z isomers were isolated, and their relative stabilities and their interconversions were tested.The antibacterial activity was tested against Gram-positive and Gram-negative bacteria.For compound 1c, whose Z and E forms do not interconvert rapidly, the Z form was the more active one.Among the other compounds, for which the E form is the only stable one for practical purposes, compound 1a was the most active.When compared with cefuroxime and cefotaxime, compound 1a showed slightly lower antibacterial activity but good serum level and half-life values.
- Brandt, Alberto,Cerquetti, Marina,Corsi, G. Bruno,Pascucci, Giorgio,Simeoni, Antonio,et al.
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- N-hydroxyphthalimide/cobalt(II) catalyzed low temperature benzylic oxidation using molecular oxygen
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A variety of (substituted) aryl glyoxylates is formed in good to excellent yield under very mild conditions by direct oxidation of the corresponding arylacetic esters or mandelic acid esters with molecular oxygen and N-hydroxyphthalimide/cobalt(II) acetate as catalyst. Heteroaromatic analogs are more difficult to oxidize with this system. The effect of substitution in the aromatic ring of N-hydroxyphthalimide on the oxidation of ethylbenzene has been studied. Electron withdrawing substituents accelerate the oxidation of ethylbenzene and promote the formation of acetophenone. Electron donating substituents lead to decreased rates of oxidation and enhance the selectivity for 1-phenylethanol. (C) 2000 Elsevier Science Ltd.
- Wentzel, Bastienne B,Donners, Maurice P.J,Alsters, Paul L,Feiters, Martinus C,Nolte, Roeland J.M
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p. 7797 - 7803
(2007/10/03)
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- 2-Lower alkyl-7-substituted-2 or 3-cephem 4-carboxylic acid compounds
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Compounds of the formula: STR1 wherein R1 is (C1 to C6) alkyl. R2 is carboxy or a protected carboxy group, R3 is amino or a protected amino group and A is hydroxyimino (C1 to C6) alkylene or (C1 to C6)-alkoxyimino (C1 to C6) alkylene, and pharmaceutically acceptable salt thereof, have been found to be active against various pathogenic microorganisms.
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- 2-Lower alkyl-7-substituted amino-2 or 3-cephem-4-carboxylic acid compounds
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A compound of the formula: STR1 wherein R1 is (C1 to C6) alkyl, R2 is carboxy or a protected carboxy group, R3 is amino or a protected amino group, and A is carbonyl or hydroxy (C1 to C6) alkylene, and pharmaceutically acceptable salt thereof, which is active against pathogenic bacteria, and methods for preparing the same.
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- 2-Lower alkyl-7-substituted-2 or 3-cephem-4-carboxylic acid compounds and pharmaceutical compositions
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A compound of the formula: STR1 wherein R1 is (C1 to C6) alkyl, R2 is a carboxy or a protected carboxy group, R3 is amino or a protected amino group and A is hydroxyimino (C1 to C6) alkylene or (C1 to C6)-alkoxyimino (C1 to C6)alkylene, And pharmaceutically acceptable salt thereof.
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