321195-74-8Relevant academic research and scientific papers
Design, synthesis, pharmacological evaluation and molecular docking studies of substituted oxadiazolyl-2-oxoindolinylidene propane hydrazide derivatives
Kerzare, Deweshri,Chikhale, Rupesh,Bansode, Ratnadeep,Amnerkar, Nikhil,Karodia, Nazira,Paradkar, Anant,Khedekar, Pramod
, p. 1998 - 2010 (2016/11/03)
The manuscript describes design and synthesis of novel oxadiazolyl-2-oxoindolinylidene propane hydrazides as amide tethered hybrids of indole and oxadiazole and their evaluation for antiinflammatory and analgesic activity. The compounds were synthesized following five step reaction to yield fifteen derivatives as 3-(5-substituted-1,3,4-oxadiazol-2-yl)-N′-[2-oxo-1,2-dihydro-3Hindol-3-ylidene]propane hydrazides. The final derivatives 3-[5-(4-hydroxyphenyl)-1,3,4-oxadiazol-2-yl]-N′-[2-oxo-1,2-dihydro-3H-indol-3-ylidene]propane hydrazide and 3-[5-(4-methylphenyl)-1,3,4-oxadiazol-2-yl]-N′-[2-oxo-1,2-dihydro-3H-indol-3-ylidene]propane hydrazide were found to be highly promising molecules with severity index of 0.35 and 0.56, respectively, which is promising for an analgesic compound. The hydroxy and methyl substitution on phenyl ring system provided with active anti-inflammatory compounds having increase in reaction time of 84.11 and 83.17percent, respectively compared to standard drug at 85.84percent. Molecular docking studies exhibit comparable interaction with synthesized derivatives and standard drug having a dock score of -4.44 by the K-nearest neighbour genetic algorithm method.
Novel arylhydrazone derivatives bearing a rhodanine moiety: Synthesis and evaluation of their antibacterial activities
Li, Wei,Zheng, Chang-Ji,Sun, Liang-Peng,Song, Ming-Xia,Wu, Yan,Li, Yin-Jing,Liu, Yi,Piao, Hu-Ri
, p. 852 - 861 (2014/08/05)
A series of arylhydrazone derivatives bearing a rhodanine moiety have been synthesized, characterized, and evaluated as antibacterial agents. Some of these compounds showed potent antibacterial activities against several different strains of Gram-positive bacteria, including multidrug-resistant clinical isolates. Of the compounds tested, IIk and IIIk were identified as the most effective, with minimum inhibitory concentration values of 2-4 μg/mL against multidrug-resistant Gram-positive organisms, including methicillin-resistant and quinolone-resistant Staphylococcus aureus. None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 at 64 μg/mL.
Identification of a potent new chemotype for the selective inhibition of PDE4
Skoumbourdis, Amanda P.,Huang, Ruili,Southall, Noel,Leister, William,Guo, Vicky,Cho, Ming-Hsuang,Inglese, James,Nirenberg, Marshall,Austin, Christopher P.,Xia, Menghang,Thomas, Craig J.
, p. 1297 - 1303 (2008/09/20)
A series of substituted 3,6-diphenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines were prepared and analyzed as inhibitors of phosphodiesterase 4 (PDE4). Synthesis, structure-activity relationships, and the selectivity of a highly potent analogue against related phosphodiesterase isoforms are presented.
Synthesis and SAR evaluation of 1,2,4-triazoles as A2A receptor antagonists
Alanine, Alexander,Anselm, Lilli,Steward, Lucinda,Thomi, Stefan,Vifian, Walter,Groaning, Michael D.
, p. 817 - 821 (2007/10/03)
The synthesis and in vitro structure-activity relationships (SAR) of a series of triazoles as A2A receptor antagonists is reported. This resulted in the identification of potent, selective and permeable 1,2,4-triazoles such as 42 for further op
Triazole derivatives
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, (2011/03/17)
The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.
