Synthesis and structure-activity relationships of 7-[3-(1- aminoalkyl)pyrrolidinyl]- and 7-[3-1-aminocycloalkyl)pyrrolidinyl]-quinolone antibacterials

DOI: 10.1248/cpb.42.1442

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1442 - 1454 (1994)

Update date:2022-07-30

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Authors:

Kimura Kimura

Atarashi

Takahashi

Hayakawa

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Article abstract of DOI:10.1248/cpb.42.1442

A series of 7-[3-(1-aminoalkyl and 1-aminocycloalkyl)-1- pyrrolidinyl]quinolones have been prepared and their biological properties evaluated. Among them, 1-(S)-aminoalkyl derivatives exhibited potent antibacterial activities against gram-positive and gram-negative organisms. They had moderate lipophilicity and high aqueous solubility compared to their aminomethyl counterparts; e.g., the 3-(1-aminoethyl)-1-pyrrolidinyl compound (83) showed superior pharmacokinetic properties to its aminomethyl counterpart (6).

Full text of DOI:10.1248/cpb.42.1442

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