Abstract
The solution-phase combinatorial synthesis of aryl chalcones was studied by synthesizing a 6x4 array mini library. The mini libraries of chalcones were synthesized by condensation of 4-substituted acetophenones and various aryl/heteroaryl carbaldehydes. All the synthesized mini libraries were screened for antibacterial activity using serial dilution method. The mini-libraries 3{1a,2a–d}, 3{1b,2a–d}, 3{1a–f,2a} and 3{1a–f,2c}were found to be most active of the synthesized mini libraries. The common elements present in the identified pool of interest were used to individually synthesize four compounds which were individually subjected to antibacterial activity evaluation. The compound 3-(4-chlorophenyl)-1-(4-methoxyphenyl)prop-2-en-1-one exhibited significant activity that was better than that of the other three compounds synthesized. The anti-bacterial activity of the identified hit was also found to be better than all mini-libraries, indicating utility of combinatorial synthesis and the assumption there in for lead identification.
Highlights
There are few reports on solution phase combinatorial synthesis and combinatorial antibacterial screening, despite the simplicity, time and material saving involved in the process
The synthetic availability and interesting structural features of chalcones, a ubiquitous structural unit in many biologically active compounds, prompted us to carry out the solution phase combinatorial synthesis of 1-(4-substituted phenyl)-3-(aryl)prop-2-en-1-one derivatives for combinatorial screening leading to identification of structures which could be novel leads for antibacterial activity optimization
For efficient synthesis of larger combinatorial libraries, we were especially interested in identifying a solvent/catalyst that would allow the conjugation process with a minimized load of byproducts
Summary
Aryl/heteroaryl substituted aldehydes and 4-substituted acetophenones, which are versatile reagents in heterocyclic synthesis, were used as components of mini-library. The synthetic availability and interesting structural features of chalcones, a ubiquitous structural unit in many biologically active compounds, prompted us to carry out the solution phase combinatorial synthesis of 1-(4-substituted phenyl)-3-(aryl)prop-2-en-1-one derivatives for combinatorial screening leading to identification of structures which could be novel leads for antibacterial activity optimization. Parallel Solution-Phase Synthesis of 1-(4-substituted phenyl)-3-(aryl)prop-2en-1-one mini-libraries Solution Phase Combinatorial Synthesis and Screening of Mini Libraries of ...
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
