Home|Journals|Articles by Year|Audio Abstracts
 

Original Article



Design, Synthesis and Preliminary Pharmacological Screening (antimicrobial, analgesic and anti-inflammatory activity) of Some Novel Quinazoline Derivatives

Biswajit Dash, Suvakanta Dash, Damiki Laloo, Chitrani Medhi.




Abstract

Objectives:
The present research work is designed to synthesize some new series of quinazoline-4-one/4-thione derivatives, depending on the pharmacophoric model of antimicrobial, analgesic and anti-inflammatory activity by modifying the structures retaining the fundamental structural features for the activity and screened for their antimicrobial, analgesic and anti-inflammatory properties.
Material and methods:
A series of 7-chloro-3-[substituted (amino/phenyl amino)]-2-phenyl quinazolin-4(3H)-one/thione derivatives and 1-(7-chloro-4-oxo/-2-phenylquinazoline-3 (4H-yl)) substituted urea derivatives were prepared. The reaction scheme proceeds through the intermediate 7-chloro-2-phenyl-4H-benzo[d] [1, 3] oxazin-4-one. The structures of the newly synthesized compounds were characterized from infrared (IR), 1H nuclear magnetic resonance (NMR) and mass spectra (m/z) and elemental analysis. The antimicrobial, analgesic and anti-inflammatory activity was investigated by agar diffusion cup plate method, tail immersion method and carrageenan-induced paw oedema method respectively.
Results:
The physico-chemical and spectroscopic data clearly confirmed the synthesis of quinazoline derivatives with a common skeleton. The synthesized compounds were evaluated for their antimicrobial, analgesic and anti-inflammatory properties. Among them five compounds (IIc, IIg, IIh, IIi and IIj) shows good activity against microbes and two compounds (IIc and IIg) show good activity profile against both pain and inflammation. Three compounds (IIh, IIi and IIj) shows good therapeutic activity only against inflammation.
Conclusion:
The quinazoline derivatives obtained from this research work indicates that the methyl/methoxy group in phenyl hydrazine ring at 3rd position, amine, urea and thiourea substitution at 3rd position of quinzoline derivatives are essential for anti-microbial, analgesic and anti-inflammatory principle. Compounds IIc, IIg, IIh, IIi and IIj were found to be potent compound which may be effective as potential source for the development of anti-microbial, analgesic and anti-inflammatory compound having common quinazoline scaffold with lesser side effects.

Key words: 7-chloro-2-phenyl-4H-benzo[d][1,3]oxazin-4-one,Quinazoline derivatives, Anti-microbial activity, analgesic and anti-inflammatory activity.






Full-text options


Share this Article


Online Article Submission
• ejmanager.com




ejPort - eJManager.com
Refer & Earn
JournalList
About BiblioMed
License Information
Terms & Conditions
Privacy Policy
Contact Us

The articles in Bibliomed are open access articles licensed under Creative Commons Attribution 4.0 International License (CC BY), which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.