PubMed · 620329
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H A Fleming. 1978-02-04. Preventing infective endocarditis.. https://doi.org/10.1136/bmj.1.6108.303
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An ideal antithrombotic drug should inhibit thrombosis without affecting hemostasis. It should have a long half life. It should be absorbed after oral administration; it should be safe and it should have a wide therapeutic range. These criteria are discussed using new antithrombotics as examples.
A series of [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acids and their esters were prepared and evaluated for antibacterial activity. The derivatives with a hydrogen or methyl group at C-1, fluorine at C-6, and piperazinyl or 4-methyl-1-piperazinyl group at C-7 showed superior in vitro antibacterial activity, and the derivatives with 4-methyl-1-piperazinyl group at C-7 had potent in vivo activity. Compound 29a (NM394) showed excellent in vitro antibacterial activity and low toxicity but poor absorption from the gastrointestinal tract. Compound 29ee (NM441), an N-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl] derivative of 29a, was found to possess a favorable pharmacokinetic profile and oral activity superior to that of ciprofloxacin in experimental animals.