26593-17-9Relevant academic research and scientific papers
Library design, synthesis and biological exploration of novel 3,4′-bicarbostyril derivatives as potent antimicrobial, antitubercular and antimalarial agents
Jardosh, Hardik H.,Vala, Nileshkumar D.,Patel, Manish P.
, p. 881 - 899 (2017/04/13)
Abstract: A library comprises diversely substituted novel 3,4′-bicarbostyril derivatives have been designed by molecular hybridization technique and synthesized via multi-component reaction. Compounds G22 (MIC = 12.5 μg/mL) and G38 (MIC = 25 μg/mL) exhibited 99% inhibition against Mycobacterium tuberculosis, while compounds G40 (IC50 = 0.019 μg/mL) and G20 (IC50 = 0.028 μg/mL) found to have excellent activity against Plasmodium falciparum. Compounds G37 (MIC = 25 μg/mL) and G8, G18, and G38 (MIC = 50 μg/mL) elicited excellent antimicrobial activity compared to standard drugs. Biological results revealed that the potency of the title compounds strongly depends on the length and flexibility of various spacers at N?1, the electronic influence of substituent at R1 and lipophilicity of CH3 group at R2 position on bicarbostyril system. Graphical Abstract: [InlineMediaObject not available: see fulltext.]
Green synthesis and pharmacological screening of polyhydroquinoline derivatives bearing a fluorinated 5-aryloxypyrazole nucleus
Karad, Sharad C.,Purohit, Vishal B.,Raval, Dipak K.,Kalaria, Piyush N.,Avalani, Jemin R.,Thakor, Parth,Thakkar, Vasudev R.
, p. 16000 - 16009 (2015/03/04)
A novel series of polyhydroquinoline scaffolds 8a-p has been designed and synthesized under ultrasonic irradiation by a one-pot three-component cyclocondensation reaction of 3-methyl-5-substituted aryloxy-1-phenyl-1H-pyrazole-4-carbaldehydes 3a-d with malononitrile 7 and various enhydrazinoketones 6a-e in the presence of piperidine as basic catalyst. All the synthesized compounds have been characterized by various spectroscopic techniques and elemental analysis. All the synthesized compounds were evaluated for their in vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi, in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain and also for their in vitro antimalarial activity against Plasmodium falciparum. Compounds 8c, 8i, 8j, 8l and 8m exhibited excellent antimalarial potency. The cytotoxicity of the synthesized compounds was tested using a bioassay of S. pombe cells at the cellular level. Compounds 8i, 8j, 8k and 8l were found to have maximum toxicity, while compounds 8e, 8m, 8c were found to be less cytotoxic. Some of them displayed luminous antibacterial activity and reasonable antituberculosis activity as compared with the first line drugs.
New N-arylamino biquinoline derivatives: Synthesis, antimicrobial, antituberculosis, and antimalarial evaluation
Shah, Nimesh M.,Patel, Manish P.,Patel, Ranjan G.
scheme or table, p. 239 - 247 (2012/09/08)
A new series of N-arylamino biquinoline derivatives 5a-x were synthesized by reaction of 2-chloro-3-formyl quinolines 2a-d with malononitrile and various enhydrazinoketones 4a-f in absolute ethanol. The newly synthesized compounds were evaluated for their in vitro antimicrobial activity against a representative panel of pathogenic strains and antituberculosis activity against Mycobacterium tuberculosis H37Rv. Compounds 5h and 5s exhibited excellent antibacterial activity and some of the compounds demonstrated moderate antituberculosis activities compared with the first line drugs. The compounds were evaluated in vitro for their activity against the growth of Plasmodium falciparum, the malaria causing parasite. Some of them showed antimalarial activity with IC50 values as low as 0.005-0.009 μg/mL.
3-Aryl- and 2,3-diaryl-4-oxo-4,5,6,7-tetrahydro-indazoles. 1. Reactions of phenyl- and tosyl-hydrazones of dimedone and cyclohexane-1,3-dione with substituted benzaldehydes
Strakova,Strakovs,Petrova
, p. 1398 - 1404 (2007/10/03)
Sixteen 3-aryl-4-oxo-2-phenyl-4,5,6,7-tetrahydroindazoles were obtained from the reaction of the phenylhydrazones of dimedone and cyclohexane-1,3-dione with 3-bromo-, 4-bromo-, 4-chloro-, 4-fluoro-, 2-hydroxy-, 4-hydroxy-, 4-methoxy-, 2-nitro-, 3-nitro-,
Reactions of cyclic enhydrazinoketones with arylidene derivatives of malononitrile. Synthesis of fused N-substituted 1,4-dihydropyridines
Lichitsky,Yarovenko,Zavarzin,Krayushkin
, p. 1251 - 1254 (2007/10/03)
A new method for the synthesis of fused N-amino-1,4-dihydropyridines was proposed. The method is based on the addition of cyclic enhydrazinoketones to arylidenemalononitriles. The structures of the compounds synthesized were studied using 1H NMR spectroscopy.
