- Antimicrobial activities of synthetic arylidine nicotinic and isonicotinic hydrazones
-
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.
- 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)
-
- Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies
-
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
- Zafar, Humaira,Hayat, Muhammad,Saied, Sumayya,Khan, Momin,Salar, Uzma,Malik, Rizwana,Choudhary, M. Iqbal,Khan, Khalid Mohammed
-
p. 2351 - 2371
(2017/04/03)
-
- Eco-friendly and highly efficient synthesis, including multigram synthesis, of aldehyde isonicotinoyl hydrazones using sonochemistry
-
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
- 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)
-
- 3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles: A new scaffold for the selective inhibition of monoamine oxidase B
-
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.
- 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)
-
- 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
-
(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.
- Somogyi, Laszlo
-
p. 1235 - 1246
(2008/09/18)
-
- Halogenated isoniazid derivatives as possible antitubercular and antineoplastic agents. Note 1
-
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
- Vigorita,Basile,Zappala,Gabrielli,Pizzimenti
-
p. 893 - 906
(2007/10/02)
-