88569-32-8Relevant academic research and scientific papers
Synthesis and in vitro antiplasmodial activities of fluoroquinolone analogs
Dixit, Sandeep K.,Mishra, Nidhi,Sharma, Manish,Singh, Shailja,Agarwal, Alka,Awasthi, Satish K.,Bhasin
, p. 52 - 59 (2012/07/28)
Fluoroquinolone analogs were synthesized by simple alkylation followed by click chemistry and evaluated for their antimalarial in vitro against chloroquine sensitive strain of Plasmodium falciparum while ciprofloxacin was used as standard. Our results showed that the compound 12 was found most active with IC50 value of 1.33 μg/mL while ciprofloxacin showed IC 50 = 8.81 μg/mL. Therefore, screening of either known or unknown quinolone/fluoroquinolone analogs are worthwhile to find more potent antimalarial drugs which might prove useful in the treatment of mild or severe malaria in human either alone or in combination with existing antimalarial drugs.
Microwave activated solid support synthesis of new antibacterial quinolones
Kidwai, Mazaahir,Misra, Preeti,Dave, Bhavesh,Bhushan, Kumar R.,Saxena, Rajendra K.,Singh, Meena
, p. 1207 - 1212 (2007/10/03)
A novel synthesis of 6-fluoro-7-(5-aryl-1,3,4-thiadiazol/oxadiazol-2-yl-sulfanyl)-4-quinolone-3- carboxylic acids from 7-chloro-6-fluoro-4-quinolone-3-carboxylic acid and 5-substituted 1,3,4-thiadiazoles/oxadiazoles on basic alumina under microwave activation is described. All compounds were screened for their in vitro antibacterial activity against B. lichenformis, 2689, K. aerogens 2281, S. typhimurium 2501, E. herbicola 2491, and P. vulgaris 2027 and found to possess activities comparable to that of the standard drug norfloxacin.
Microwave assisted synthesis and antibacterial activity of new quinolone derivatives
Kidwai, Mazaahir,Misra, Preeti,Kumar, Rajesh,Saxena, Rajendra K.,Gupta, Rani,Bradoo, Sapna
, p. 961 - 965 (2007/10/03)
A series of novel 6-fluoro-7-(5-alkyl-1,3,4-thiadiazol/oxadiazol-2-ylsulfanyl)-4-quino-lone-3- carboxylic acids were synthesized using microwave irradiation. The compounds were tested for their in vitro antibacterial activity. All compounds containing the 1,3,4-thiadiazole/oxadiazole moiety at position 7 showed promising antibacterial activity.
Quinolone nucleosides: 6,7-dihalo-N-β- and α-glycosyl-1,4-dihydro-4- oxo-quinoline-3-carboxylic acids and derivatives. Synthesis, antimicrobial and antiviral activity
Al-Masoudi, Najim A.,Al-Soud, Yaseen A.,Ehrmann, Micheal,De Clercq, Erik
, p. 2255 - 2266 (2007/10/03)
Reaction of the silylated 6,7-dihaloquinoline bases 10-12 with 1-O- acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose (13) gave ethyl 7-chloro-6- flouro-1,4-dihydro-4-oxo-1-(2,3,5-tri-O-benzoyl-β-D- ribofuranosyl)quinoline-3-carboxylate (14) and the free acids
Synthesis and Biological Evaluation of 4-Quinolone Ribosides
Cruz, Angeles de la,Elguero, Jose,Goya, Pilar,Martinez, Ana,Clercq, Erik De
, p. 845 - 850 (2007/10/02)
The preparation of ribosides of 4-oxoquinoline-3-carboxylic acid derivatives is described.All the reported compounds were evaluated for antiviral and antibacterial activity.
Tautomerism and acidity in 4-quinolone-3-carboxylic acid derivatives
De La Cruz, Angeles,Elguero, Jose,Goya, Pilar,Martinez, Ana,Pfleiderer, Wolfgang
, p. 6135 - 6150 (2007/10/02)
Prototropic tautomerism in 4-quinolone-3-carboxylic acid derivatives has been studied with particular emphasis on the influence of the ring substituents on the equilibrium. The techniques used include UV, 1H-NMR, 13C-NMR (solution and 13C-NMR CP/MAS (solid state) and semiempirical and ab initio calculations. The pKa values of some quinolone derivatives have been determined and correlated with data obtained from semiempirical methods.
SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF SOME 1-(2-PROPYNYL) AND 1-PROPADIENYL DERIVATIVES OF 1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXYLIC ACIDS AND SIMILAR HETEROCYCLES
Radl, Stanislav,Kovarova, Lenka,Holubek, Jiri
, p. 439 - 448 (2007/10/02)
N-Alkylation of IIIa, IIIb, IIId-IIIf, and 9-acridanone with 3-bromopropyne in dimethyl sulfoxide in the presence of potassium carbonate yielded N-(2-propynyl) derivatives IVa-IVe and VIa, respectively.Ethyl esters IVa, IVb, and IVe were hydrolyzed to IVf-IVh, respectively.Compounds IVf, IVg, IVc treated with bases yielded N-propadienyl derivatives Va-Vc.On the other hand 2-substituted compounds IVd and IVh did not change under the same conditions.Compound VIa treated with powdered potassium hydroxide in dimethyl sulfoxide at room temperature yielded N-(1-propynyl)derivative VII.
