Podophyllotoxin structure activity relationship for quinolones

Inspection of the extensive published SAR data of podophyllotoxin analogues reveals that the intact ring A is not essential for antimitotic activity. In addition, the . Agui H, Mitani T, Izawa A, Komatsu T, Nakagome T. Studies on quinoline derivatives and related compounds. 5. Synthesis and antimicrobial activity of novel. Podophyllotoxin (PPT), also known as podofilox, is a medical cream that is used to treat genital In contrast, some of its derivatives display binding activity to the enzyme The structure of podophyllotoxin was first elucidated in the s. biological activities, mode of action, and structure-activity relationship of.

Podophyllotoxin derived antitumor agents include etoposide and teniposide. It is used for the treatment of HPV infections with external warts as well as molluscum contagisum infections. PPT is also sold under the names condyline and warticon. Small sores, itching and peeling skin can also follow, for these reasons it is recommended that application be done in a way that limits contact with surrounding, uninfected tissue [16] Neither podophyllin resin nor podophyllotoxin lotions or gels are used during pregnancy because these medications have been shown to be embroytoxic in both mice and rats.

Additionally, antimitotic agents are not typically recommended during pregnancy. The podophyllum resin from which podophyllotoxin is derived has the same effect. For instance, etoposide binds and stabilizes the temporary DNA break caused by the enzyme, disrupts the reparation of the break through which the double-stranded DNA passes, and consequently stops DNA unwinding and replication. Lastly, experimental evidence has shown that these arytetralin lignans can interact with cellular factors to create chemical DNA adducts thus further deactivating DNA.

The molecule also contains four almost planar fused rings. The podophyllotoxin molecule includes a number of oxygen containing functional groups: For example, ring A is not essential to antimitotic activity.

Aromatization of ring C leads to loss of activity, possibly from ring E no longer being placed on the axial position. New quantitative structure-activity relationships at N1 for the quinolone antibacterials. A new synthesis of 7H-pyrido[1,2,3-de][1,4]benzoxazine derivatives including an antibacterial agent, ofloxacin.

Structure-activity relationships of the fluoroquinolones.

Chem Pharm Bull Tokyo Oct;34 Geneva, Switzerland, July In-vitro and in-vivo potency of five new fluoroquinolones against anaerobic bacteria. Activity of E, a new fluoroquinolone, in vitro and in experimental cystitis and pyelonephritis in rats. Monocyclic and tricyclic analogs of quinolones: Synthesis, absolute configuration, and antibacterial activity of 6,7-dihydro-5,8-dimethylfluorooxo-1H,5H- benzo[ij]quinolizinecarboxylic acid.

Difloxacin metabolism and pharmacokinetics in humans after single oral doses. Comparative antibacterial activities of temafloxacin hydrochloride A and two reference fluoroquinolones. Isolation and characterization of norfloxacin-resistant mutants of Escherichia coli K Mutations producing resistance to norfloxacin in Pseudomonas aeruginosa.

Podophyllotoxin - Wikipedia

Genetic and biochemical characterization of norfloxacin resistance in Escherichia coli. Recent advances in pharmaceutical chemistry. J Clin Hosp Pharm. Computer automated structure evaluation of quinolone antibacterial agents. Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydrooxoquinolinecarboxylic acids.


Synthesis and antimicrobial activity of 3-formylquinolone derivatives. Chiral DNA gyrase inhibitors. Synthesis and antimicrobial activity of the enantiomers of 6-fluoro 1-piperazinyl 2'-trans-phenyl-1'-cyclopropyl -1, 4-dihydrooxoquinolinecarboxylic acid.

SAR of Acetylcholine (Explained with structures)

Asymmetric synthesis and biological activity of the enantiomers of 9-fluoromethyl 4-methylpiperazinyl oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazinecarboxylic acid ofloxacin. Genetic and physiological characterization of ciprofloxacin resistance in Pseudomonas aeruginosa PAO.