39136-63-5Relevant articles and documents
Synthesis and potential antimicrobial activity of novel α-aminophosphonates derivatives bearing substituted quinoline or quinolone and thiazole moieties
Litim, Bilal,Djahoudi, Abdelghani,Meliani, Saida,Boukhari, Abbes
, p. 60 - 74 (2021/11/09)
To develop novel antimicrobial agents, and based on the biologically active heterocyclic quinoline and thiazole substituted, a series of novel α-aminophosphonates (9a–h) and (10i–l) derivatives that incorporated quinoline or quinolone, and coumarylthiazole or 5-phenylthiazol-2-amine moieties were designed and synthesized via Kabachnik–Fields reaction in the presence of ionic liquid under ultrasound irradiation. All the new compounds were obtained in good yield with a simple workup and were confirmed using various spectroscopic methods. The in vitro antimicrobial activity of all synthesized compounds were screened in terms of MIC values against the selected strains of Gram-negative and Gram-positive bacteria and two fungal strains using the broth micro-dilution method. The results showed that most of the tested compounds showed moderate inhibitory activities against both Gram‐positive and ‐negative bacteria compared with reference drugs. The following compounds 9e, 9g, 9h, 9i and 9f, 9g, 9h, 10k, 10l are the most active against Gram-positive and Gram-negative bacteria strains, respectively, with MIC values ranging between 0.25 and 128 μg/mL. The synthesized compounds 9b, 9c, 9f, 9g, 9h, 10k, and 10l exhibited excellent antifungal inhibition with MIC values ranging between 0.25 and 32 μg/mL. Structure–activity relationship revealed that the presence of coumarylthiazole moiety and hydroxyl in the quinoline group increased the inhibitory activity against microbial strains pathogens. These results confirm that the synthesized compounds can be potential antimicrobial drugs candidate. [Figure not available: see fulltext.]
Glucose promoted facile reduction of azides to amines under aqueous alkaline conditions
Chandna, Nisha,Kaur, Fatehjeet,Kumar, Shobhna,Jain, Nidhi
supporting information, p. 4268 - 4271 (2017/09/29)
A quick and efficient method for the reduction of azides to amines in water using d-glucose and KOH as green reagents is reported. The protocol is simple, inexpensive, scalable, and can be applied to different aromatic, heteroaromatic and sulphonyl azides. A high level of chemoselectivity is observed for azide reduction in the presence of other reducible functionalities like cyano, nitro, ether, ketone, amide and acid. The reaction gets completed in a short time (5-20 minutes), and furnishes the amines in high yield (85-99%). Unlike conventional hydrogenations, this reduction protocol does not require any metal catalyst, elaborate experimental setup or use of high-pressure equipment.
Novel 2-Aminothiazole Derivatives and Composition for Treating Cancer Comprising the Same
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Paragraph 0052-0054, (2017/06/06)
PURPOSE: A novel 2-aminothiazole derivative and an anticancer composition containing the same are provided to suppress growth and proliferation of various cancer cells and to induce cancer cell apoptosis. CONSTITUTION: A 2-aminothiazole derivative is denoted by chemical formula 1. In chemical formula 1, R1 is phenyl, halogen-substituted phenyl, alkyl of 1-4 carbon atoms, or phenyl-substituted alkyl of C1-4; and R2 is alkyl of C1-9, furyl-substituted alkyl of C1-4, furyl-substituted alkenyl of C1-4. An anticancer composition contains the 2-aminothiazole derivative of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. The anticancer composition is a pharmaceutical composition for preventing or treating cancer.
