144293-91-4Relevant academic research and scientific papers
Antimicrobial activities of synthetic arylidine nicotinic and isonicotinic hydrazones
Hayat, Muhammad,Khan, Khalid Mohammed,Saeed, Sumayya,Salar, Uzma,Khan, Momin,Baig, Taimoor,Ahmad, Aqeel,Parveen, Shahnaz,Taha, Muhammad
, p. 1057 - 1067 (2018/10/31)
Background: Despite availability of variety of antibacterial agents, re-emergance of pathogenic bacteria is still a serious medical concern. Identification of new, safer, and selective antibacterial agents is the key interest in the medicinal chemistry research. Methods: A library of synthetic arylidene nicotinic and isonicotinic hydrazones (1-63) were investigated for antimicrobial activities. Results: A number of derivatives showed significant to moderate antimicrobial activities against Gram positive and Gram negative bacterial cultures. Few compounds also showed antifungal activity against fungal cultures. Minimum Inhibitory Concentration (MIC) was calculated for the most active compounds 1, 7, 11, 19, 34, 46, 50, 51, and 55 against gram positive and gram negative cultures. Conclusion: Newly identified compounds may serve as lead for future research in order to get the more powerful antibacterial agents.
Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies
Zafar, Humaira,Hayat, Muhammad,Saied, Sumayya,Khan, Momin,Salar, Uzma,Malik, Rizwana,Choudhary, M. Iqbal,Khan, Khalid Mohammed
, p. 2351 - 2371 (2017/04/03)
Change in life style and eating habits has led to an increased prevalence of hyperuricemia worldwide. The role of hyperuricemia is no more restricted to gout, but it has a central role in progression of CVD, hypertension, metabolic syndrome, and arthritis
Eco-friendly and highly efficient synthesis, including multigram synthesis, of aldehyde isonicotinoyl hydrazones using sonochemistry
Da Silveira Pinto, Ligia S.,De Souza, Marcus V. N.,Da Silva, Emerson T.,Kaiser, Carlos R.,Wardell, Solange M.S.V.,Wardell, James L.
, p. 585 - 590 (2016/12/18)
Background: The isoniazid has been a key compound in first-line tuberculosis (TB) treatment, usually in combination with other drugs. Following on from the use of isoniazid itself, various derivatives of isoniazid have also been investigated as anti-TB ag
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles: A new scaffold for the selective inhibition of monoamine oxidase B
MacCioni, Elias,Alcaro, Stefano,Cirilli, Roberto,Vigo, Sara,Cardia, Maria Cristina,Sanna, Maria Luisa,Meleddu, Rita,Yanez, Matilde,Costa, Giosuè,Casu, Laura,Matyus, Peter,Distinto, Simona
experimental part, p. 6394 - 6398 (2011/11/06)
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles were designed, synthesized, and tested as inhibitors against human monoamine oxidase (MAO) A and B isoforms. Several compounds, obtained as racemates, were identified as selective MAO-B inhibitors. The enantiomers of some derivatives were separated by enantioselective HPLC and tested. The R-enantiomers always showed the highest activity. Docking study and molecular dynamic simulations demonstrated the putative binding mode. We conclude that these 1,3,4-oxadiazoles derivatives are promising reversible and selective MAO-B inhibitors.
Synthesis, oxidation and dehydrogenation of cyclic N,O- and N,S-acetals. Part III. [1,2] Transformation of N,O-acetals: 3-Acyl-1,3,4-oxadiazolines
Somogyi, Laszlo
, p. 1235 - 1246 (2008/09/18)
(Chemical Equation Presented) Various aldehyde and ketone acylhydrazones are synthesized and, under acylating conditions, cyclized into 3-acyl-1,3,4-oxadiazolines. The scope and limitations of these cyclizations and the possible side reactions (e.g. formation of the open-chain N,O-acylhydrazinocarbinols) are dissected. For the first time, simple, convenient and efficient dehydrogenations of 3-acyl-1,3,4-oxadiazolines to oxadiazoles by treatment with potassium permanganate, or more conveniently, with ammonium cerium(IV) nitrate (CAN) are presented. CAN oxidation of 2,2-disubstituted 3-acyl-1,3,4-oxadiazolines, as well as that of aldehyde diacylhydrazones (open-chain isomers of 2,5-disubstituted 3-acyl-1,3,4- oxadiazolines) regenerates the parent carbonyl compounds.
Halogenated isoniazid derivatives as possible antitubercular and antineoplastic agents. Note 1
Vigorita,Basile,Zappala,Gabrielli,Pizzimenti
, p. 893 - 906 (2007/10/02)
Halogenated arylhydrazones, 2-aryl-4-thiazolidinones and their 1,1-dioxides containing isoniazid (INI) moieties were prepared and explored for antimicrobial (against bacteria, Candida and mycobacteria) and antitumor activities. None of the tested compound
