55436-34-5Relevant academic research and scientific papers
EXPANDED THERAPEUTIC POTENTIAL IN NITROHETEROARYL ANTIMICROBIALS
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Paragraph 0317, (2015/01/07)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to imidazole, thiazole, and furan derivatives and their use as therapeutic agents.
Design and synthesis of novel 2H-chromen-2-one derivatives bearing 1,2,3-triazole moiety as lead antimicrobials
Kushwaha, Khushbu,Kaushik, Nagendra,Lata,Jain, Subhash C.
supporting information, p. 1795 - 1801 (2014/04/17)
A series of novel 2H-chromen-2-one derivatives decorated with 1,2,3-triazole moiety were designed and synthesized using the click reaction of azidoalkyloxy-2H-chromen-2-ones with different propargylamines. Propargylamines were obtained by alkylation of various heterocyclic amines with propargyl bromide. Newly synthesized compounds and intermediates were evaluated for their antifungal activity against four fungi (Aspergillus niger, Aspergillus fumigatus, Aspergillus flavus and Candida albicans). Antibacterial studies were also carried out against three Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis and Staphylococcus epidermis) and four Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi and Klebsiella pneumoniae). In vitro, bioassay results showed that all the synthesized compounds exhibited excellent activity against fungal strains Aspergillus fumigatus, Aspergillus flavus and Candida albicans. Interestingly, all the compounds have shown even superior activity than the reference drug miconazole against Aspergillus fumigatus. Morpholine and N-acetyl piperazine containing compounds 10c and 10e have shown promising activity against various bacterial strains. Compound 10e was found to be most active against Pseudomonas aeruginosa. Based on, in silico pharmacokinetic studies, compounds 10a-e were identified as lead compounds for future investigation due to their lower toxicity, high drug score values and good oral bioavailability as per OECD guidelines.
Non anticholinergic gastric acid secretion inhibitors. New piperazine and related derivatives
Tricerri,Elitropi,Panto,et al.
, p. 555 - 562 (2007/10/08)
Some of the new piperazine derived compounds exhibited interesting gastric antisecretory properties without anticholinergic action. 1 Piperonyl 4 (3,7,11 trimethyl 2,6,10 dodecatrienyl) piperazine was the most active as an antisecretory agent in rat. Some analogous compounds, with the piperazine ring replaced by other heterocyclic or acyclic amines, were also prepared. Structure activity relationships are discussed.
