KR960703895A - Antibacterial quinolinyl- (1H-1,2,4-triazol-1-yl) alkanol derivatives - Google Patents

Abstract

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof having antibacterial activity:

Wherein R ¹ and R ² are each hydrogen or lower alkyl, R ³ is optionally substituted quinoline or an oxide thereof, and X and Y are each hydrogen, halogen, cyano or lower alkyl.

Description

Antimicrobial quinolinyl- (1H-1,2,4-triazol-1-yl) alkanol derivatives

As this is a public information case, the full text was not included.

Claims (11)

Compound of formula (I) or a pharmaceutically acceptable salt thereof: Wherein R ¹ and R ² are each hydrogen or lower alkyl, R ³ is optionally substituted quinoline or an oxide thereof, and X and Y are each hydrogen, halogen, cyano or lower alkyl. A compound according to claim 1 having the general formula (IA): Wherein R ¹ , R ² , R ³ , X and Y are as defined in claim 1, respectively. The compound of claim 2, wherein R ³ is hydroxy, protected hydroxy, halogen, lower alkoxy, halo (lower) alkyl, halo (lower) alkoxy, lower alkyl, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl And quinolyl optionally substituted by a group selected from the group consisting of amino, nitro, cyano and carboxy or N-oxides thereof. 4. The compound of claim 3, wherein R ³ is hydroxy, halogen, lower alkoxy, halo (lower) alkyl, halo (lower) alkoxy, lower alkyl, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, cyano and carboxy A quinolyl or N-oxide thereof optionally substituted by a group selected from the group consisting of: 5. The compound of claim 4, wherein R ³ is quinolyl, hydroxyquinolyl, haloquinolyl, lower alkoxyquinolyl, halo (lower) alkylnurrolyl, halo (lower) alkoxyquinolyl, lower alkylquinolyl, lower alkylthio Quinolyl, lower alkylsulfinylquinolyl, lower alkylsulfonylquinolyl, cyanoquinolyl, carboxyquinolyl, N-oxide of quinolyl or N-oxide of haloquinolyl. The compound of claim 5 having the general formula (IN). Wherein R ³ , X and Y are each as defined in claim 5 and R ¹ _a is lower alkyl. (B) reacting a compound of formula (II) or a salt thereof with a compound of formula (III) or a salt thereof to obtain a compound of formula (I) or a salt thereof, or Oxidizing an optionally substituted quinolyl or salt thereof to give a compound of formula (I-b) or a salt thereof, or (b) a lower-alkoxy substituent of an optionally substituted quinolyl or salt thereof of a compound of formula (I-c) Hydrolysis to give the compound of formula (I-d) or a salt thereof, or (iii) lower-alkylthio- or lower alkylsulfinyl- of an optionally substituted quinolyl or salt thereof of the compound of formula (I-c) The substituent is oxidized to give a compound of formula (I-f) or a salt thereof, or (c) hydrolyzing an optionally substituted quinolyl or salt of the compound of formula (I-g) Characterized by obtaining the compound of I-h) or a salt thereof A method for preparing a compound of formula (Ⅰ). Wherein R ¹ , R ² , R ³ , X and Y are each as mentioned above, R ³ _a is optionally substituted quinolyl, R ³ _b is an N-oxide of optionally substituted quinolyl, and R ³ _c is quinolyl substituted by lower alkoxy and optionally substituted by suitable substituent (s), R ³ _d is quinolyl substituted by hydroxy and optionally substituted by suitable substituent (s), R ³ _c Is quinolyl substituted by lower alkylthio or lower alkylsulfonyl and optionally substituted by suitable substituent (s), R ³ _f is optionally substituted by lower alkylsulfinyl or lower alkylsulfonyl and optionally substituted substituent (s) Quinolyl substituted by R ³ _g is quinolyl substituted by cyano and optionally substituted by suitable substituent (s), R ³ _h is substituted by carboxy and optionally substituted by suitable substituent (s) Quinolyl. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof as an active ingredient in a mixture with a pharmaceutically acceptable carrier or excipient. A method of treating or preventing a disease caused by an infection by administering a compound of claim 1 or a pharmaceutically acceptable salt thereof to a human or animal. A compound of claim 1, or a pharmaceutically acceptable salt thereof, for use as a medicament. Use of a compound of claim 1 or a pharmaceutically acceptable salt thereof for the manufacture of a medicament. ※ Note: The disclosure is based on the initial application.