European Journal of Chemistry

Quinazolinones linked amino acids derivatives as a new class of promising antimicrobial, antioxidant and anti-inflammatory agents

Main Article Content

Kadalipura Puttaswamy Rakesh
Suhas Ramesh
Honnayakanahalli Marichennegowda Manu Kumar
Shivamallu Chandan
Dase Channe Gowda


Two series of amino acids conjugated quinazolinones (1a-h and 2a-h) were synthesized by acid-amine coupling and the structures of all the compounds were confirmed through spectroscopic techniques such as IR, NMR and HRMS. The synthesized compounds were evaluated for their antimicrobial, antioxidant and anti-inflammatory activities. Biological evaluation study revealed that, the compounds 1f, 2f, 2g and 1g showed good antioxidant activity with 50% of the inhibition concentration (IC50) values 35, 20, 30 and 40 µg/mL, respectively, much better than the standard BHT (IC50 = 45 µg/mL). The compounds 1g, 2e and 2g found to have promising anti-inflammatory activity and almost all the synthesized compounds exhibited good antimicrobial activities (antibacterial and antifungal) against all the selected pathogenic bacteria and fungi. Conjugates containing Trp, Tyr and Pro have shown better activity than the rest of the analogues in the series. The structure-activity relationship was established for these compounds.

icon graph This Abstract was viewed 2573 times | icon graph Article PDF downloaded 949 times

How to Cite
Rakesh, K. P.; Ramesh, S.; Kumar, H. M. M.; Chandan, S.; Gowda, D. C. Quinazolinones Linked Amino Acids Derivatives As a New Class of Promising Antimicrobial, Antioxidant and Anti-Inflammatory Agents. Eur. J. Chem. 2015, 6, 254-260.

Article Details

Crossref - Scopus - Google - European PMC

[1]. Hess, H. J.; Cronin, T. H.; Scriabine, A. J. Med. Chem. 1968, 11, 130-136.

[2]. Ghorab, M. M.; Abdel-Gawad, S. M.; El-Gaby, M. S. A. Il Farmaco 2000, 55, 249-255.

[3]. Al-Obaid, A. M.; Abdel-Hamide, S. G.; El-Kashef, H. A.; Abdel-Aziz, A. A. M.; El-Azab, A. S.; Al-Khamees, H. A.; El-Subbagh, H. I. Eur. J. Med. Chem. 2009, 44, 2379-2391.

[4]. Kumar, A.; Tyagi, M.; Shrivasthava, V. K. Ind. J. Chem. B 2003, 42, 2142-2145.

[5]. Khalil, M. A.; Soliman, R.; Farghaly, A. M.; Bekhit, A. A. Arch. Pharm. 1994, 327, 27-30.

[6]. Shivaram, H. B.; Padmaja, M. T.; Shivnanda, M. K.; Akbarali, P. M. Ind. J. Chem. B 1998, 37, 715-716.

[7]. Nathwami, D.; Wood, M. J. Drugs 1993, 45(6), 866-894.

[8]. Schnappinger, D.; Hillen, W. Arch. Microbiol. 1996, 165, 359-369.

[9]. Lee, H. J.; Lee, K. W. Mech. Ageing. Dev. 2006, 127, 424-431.

[10]. Halliwell, B.; Gutteridge, J. M.; Cross, C. E.; Lab, J. Clin. Med. 1992, 119, 598-620.

[11]. Balakumar, C.; Lamba, P.; Kishore, D. P.; Narayana, B. L.; Venkat, K. V. Eur. J. Med. Chem. 2010, 45, 4904-4913.

[12]. Suhas, R.; Chandrashekar, S.; Gowda, D. C.; Eur. J. Med. Chem. 2011, 46, 704-711.

[13]. Suhas, R.; Chandrashekar, S.; Gowda, D. C. Int. J. Pept. Res. Thera. 2012, 18, 89-98.

[14]. Suresha, G. P.; Suhas, R.; Kapfo, W.; Gowda, D. C. Eur. J. Med. Chem. 2011, 46, 2530-2540.

[15]. Gadek, T. R.; Nicholas, J. B. Biochem. Pharmacol. 2003, 65, 1-8.

[16]. Perez, C.; Paul, M.; Bazerque, P. Acta. Biol. Med. Exp. 1990, 15, 113-115.

[17]. Singh, I.; Singh, V. P. Phytomorphology 2000, 50, 151-157.

[18]. Blois, M. S. Nature 1958, 181, 1199-1200.

[19]. Shinde, U. A.; Phadke, A. S.; Nair, A. M.; Mungantiwar, A. A.; Dikshit, V. J.; Saraf, M. N. Fitoterapia 1999, 70, 251-257.

[20]. Fournier, J.; Bruneau, C.; Dixneuf, P. H.; Lecolier, S. J. Org. Chem. 1991, 56, 4456-4458.

[21]. Mhaske, S. B.; Argade, N. P. J. Org. Chem. 2001, 66, 9038-9040.

[22]. Wohlrab, A.; Lamer, R.; VanNieuwenhze, M. S. J. Am. Chem. Soc. 2007, 129, 4175-4177.

[23]. Shivakumara, K. N.; Prakasha, K. C.; Gowda, D. C. E-J. Chem. 2009, 6(S1), S473-S479.

[24]. Biradar, J. S.; Sasidhar, B. S.; Parveen, R. Eur. J. Med. Chem. 2010, 45, 4074-4078.

[25]. Poeggeler, B.; Pappolla, M. A.; Hardeland, R.; Rassoulpour, A.; Hodgkins, P. S.; Guidetti, P.; Schwarcz, R. Brain. Res. 1999, 815, 382-388.

[26]. Yasin, C.; Hulya, G.; Abdullah, M.; Ilhami, G. Arch. Pharma. Chem. Life Sci. 2012, 345, 323-334.

Supporting Agencies

Center with Potential for Excellence in a Particular Area (CPEPA), UGC, New Delhi
Most read articles by the same author(s)

Dimensions - Altmetric - scite_ - PlumX

Downloads and views


Download data is not yet available.


Metrics Loading ...
License Terms

License Terms


Copyright © 2024 by Authors. This work is published and licensed by Atlanta Publishing House LLC, Atlanta, GA, USA. The full terms of this license are available at and incorporate the Creative Commons Attribution-Non Commercial (CC BY NC) (International, v4.0) License ( By accessing the work, you hereby accept the Terms. This is an open access article distributed under the terms and conditions of the CC BY NC License, which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited without any further permission from Atlanta Publishing House LLC (European Journal of Chemistry). No use, distribution, or reproduction is permitted which does not comply with these terms. Permissions for commercial use of this work beyond the scope of the License ( are administered by Atlanta Publishing House LLC (European Journal of Chemistry).