Synthesis and potent antimicrobial activity of novel coumarylthiazole α-aminophosphonates derivatives.

Molecular Diversity
Bilal LitimAbbes Boukhari

Abstract

Herein, we reported a novel series of α-aminophosphonates derivatives (IV)a-m bearing an important pharmacophore coumarylthiazole moiety. All the new compounds have been synthesized via Kabachnik-Fields reaction under ultrasonic irradiation. The products were obtained in good yield with a simple workup and were confirmed using various spectroscopic methods. All these compounds (IV)a-m were screened for their in vitro for antimicrobial activity against thirteen Gram-negative bacteria and five Gram-positive bacteria and Candida albicans strains. The results showed that all the synthesized compounds exhibited moderate antibacterial activities against both references and multidrug-resistant and antifungal strains. The compound (IV)e showed the highest activities against all pathogens of the tested microbial strains with MIC of 0.125 μg/mL. The compounds (IV)h, (IV)f, (IV)b, and (IV)d exhibited moderate and promising activities with MIC of 0.125 μg/mL. Structure-activity relationship revealed that inhibitory activity of the synthesized compounds is related to the type of the substituted group on phenyl rings, and these results showed that the electron-donating groups at ortho and para positions have a high relationship increasing an...Continue Reading

References

Mar 6, 2007·European Journal of Medicinal Chemistry·R G KalkhambkarR Nagendra Rao
Nov 17, 2007·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Irina O ZhuravelValentin P Chernykh
Nov 14, 2012·Nucleosides, Nucleotides & Nucleic Acids·Abdalla E A HassanAbdelfattah Z Haikal
Dec 3, 2014·European Journal of Medicinal Chemistry·Abdul Rouf, Cihangir Tanyeli
Aug 27, 2015·Journal of Enzyme Inhibition and Medicinal Chemistry·Belma Zengin KurtMustafa Kucukislamoglu
Aug 17, 2018·Mini Reviews in Medicinal Chemistry·Swarnagowri Nayak, Santhosh L Gaonkar
Feb 6, 2020·Journal of Receptor and Signal Transduction Research·Rasool Shaik NayabNaga Raju Chamarthi

❮ Previous
Next ❯

Related Concepts

Related Feeds

Candidiasis

Candidiasis is a common fungal infection caused by Candida and it can affect many parts for the body including mucosal membranes as well as the gastrointestinal, urinary, and respiratory tracts. Here is the latest research.

Candidiasis (ASM)

Candidiasis is a common fungal infection caused by Candida and it can affect many parts for the body including mucosal membranes as well as the gastrointestinal, urinary, and respiratory tracts. Here is the latest research.

Candida albicans

Candida albicans is an opportunistic, fungal pathogen of humans that frequently causes superficial infections of oral and vaginal mucosal surfaces of debilitated and susceptible individuals. Discover the latest research on Candida albicans here.