2. Academic Validation
  3. Quinazolines and quinazolinones as ubiquitous structural fragments in medicinal chemistry: An update on the development of synthetic methods and pharmacological diversification

Quinazolines and quinazolinones as ubiquitous structural fragments in medicinal chemistry: An update on the development of synthetic methods and pharmacological diversification

  • Bioorg Med Chem. 2016 Jun 1;24(11):2361-2381. doi: 10.1016/j.bmc.2016.03.031.
Imtiaz Khan 1,  Sumera Zaib 2,  Sadaf Batool 3,  Naeem Abbas 4,  Zaman Ashraf 5,  Jamshed Iqbal 6,  Aamer Saeed 7
Affiliations

Affiliations

  • 1 Department of Chemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan. Electronic address: ikhanqau@gmail.com.
  • 2 Department of Biochemistry, Hazara University, Garden Campus, Mansehra, Pakistan; Centre for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan.
  • 3 Department of Bioinformatics and Biotechnology, International Islamic University, Islamabad 44000, Pakistan.
  • 4 Department of Chemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan.
  • 5 Department of Chemistry, Allama Iqbal Open University, Islamabad 44000, Pakistan.
  • 6 Centre for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan.
  • 7 Department of Chemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan. Electronic address: aamersaeed@yahoo.com.
PMID: 27112448 DOI: 10.1016/j.bmc.2016.03.031
Abstract

Nitrogen-rich heterocycles, particularly quinazolines and quinazolinones, represent a unique class of diversified frameworks displaying a broad spectrum of biological functions. Over the past several years, intensive medicinal chemistry efforts have generated numerous structurally functionalized quinazoline and quinazolinone derivatives. Interest in expanding the biological effects, demonstrated by these motifs, is growing exponentially, as indicated by the large number of publications reporting the easy accessibility of these skeletons in addition to the diverse nature of synthetic as well as biological applications. Therefore, the main focus of the present review is to provide an ample but condensed overview on various synthetic approaches providing access to quinazoline and quinazolinone compounds with multifaceted biological activities. Furthermore, mechanistic insights, synthetic utilization, structure-activity relationships and molecular modeling inputs for the potent derivatives have also been discussed.

Keywords

Biological activity; Drug discovery; Enzyme inhibitors; Heterocycles; Quinazolines; Quinazolinones.

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