- ANTIVIRAL AND ANTIMICROBIAL COMPOUNDS
-
Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.
- -
-
-
- On the binding site of quinolone antibacterials. An attempt to probe the Shen model
-
Quinolone-nuclei acid base hybrids were synthesized in an effort to probe a mechanistic model and a proposed mode of antibacterial action where stacked pairs of quinolones interact with DNA through H-bonding.
- Hanessian, Stephen,Saladino, Raffaele,Nunez, Jose Cid
-
p. 2333 - 2338
(2007/10/03)
-
- Synthesis and antibacterial activity of 1-(substituted pyrrolyl)-7- (substituted amino)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids
-
Seventeen quinolone compounds characterized by having a fluorine atom at the 6-position, a substituted amino at the 7-position, and a substituted pyrrolyl at the 1-position were synthesized for the first time. The in vitro antibacterial activities of thes
- Liu,Guo
-
p. 3469 - 3473
(2007/10/02)
-
- Cycloaracylation of Enamines, I. - Synthesis of 4-Quinolone-3-carboxylic Acids
-
Starting with o-halobenzoyl chlorides 4 and open-chain secondary enamines 5, a new synthesis of 4-quinolone-3-carboxylic acids 12 is described.The reaction of 7-haloquinolone-3-carboxylic acids 12a-k with aliphatic amines 14 produces highly active antibacterial 7-aminoquinolone-3-carboxylic acids 15.The main product of the 1-cyclopropyl series, "ciprofloxacin" (15a), is being developed as a broad-spectrum chemotherapeutic agent.
- Grohe, Klaus,Heitzer, Helmut
-
-
- Synthesis and Structure-Activity Relationships of Novel Arylfluoroquinolone Antibacterial Agents
-
A series of novel arylfluoroquinolones has been prepared.These derivatives are characterized by having a fluorine atom at the 6-position, substituted amino groups at the 7-position, and substituted phenyl groups at the 1-position.Structure-activity relationship (SAR) studies indicate that the in vitro antibacterial potency is greatest when the 1-substituent is either p-fluorophenyl or p-hydroxyphenyl and the 7-substituent is either 1-piperazinyl, 4-methyl-1-piperazinyl, or 3-amino-1-pyrrolidinyl.The electronic and spatial properties of the 1-substituent, as well as the steric bulk, play important roles in the antimicrobial potency in this class of antibacterials.As a result of this study, compounds 45 and 41 were found to possess excellent in vitro potency and in vivo efficacy.
- Chu, Daniel T. W.,Fernandes, Prabhavathi B.,Claiborne, Akiyo K.,Pihuleac, Eva,Nordeen, Carl W.,et al.
-
p. 1558 - 1564
(2007/10/02)
-