Synthesis, antimicrobial evaluation and docking studies of some novel quinazolinone Schiff base derivatives Rezvan Rezaee Nasab, Mahboubeh Mansourian, Farshid Hassanzadeh Abstract The quinazolin-4 3H -one structural motif possesses a wide spectrum of biological activities. DNA gyrase play an important role in induction of bacterial death. It has been shown that many quinazolin-4 3H -one derivatives have antibacterial effects through inhibition of DNA gyrase.
Indian Journal of Pharmaceutical Education and Research, ; 52 4s2: SS Original Article doi: Molecular target specific treatment for the cancer is different from the conventional chemotherapy and radiotherapy in terms of selectivity and specificity towards the cancer cells.
Amongst the different molecular targets for cancer, EGFR tyrosine kinase is considered more promising molecular target for discovery and development of the novel anticancer agents.
EGFR overexpression and deregulation or mutation are observed in the different kinds of epithelial cancer namely non-small-cell lung cancer, colon cancer, breast cancer etc.
Further, the molecular docking simulation was carried out to recognize the interaction of ligands with the active site of EGFR.
All the compounds from the dataset were aligned using the distill alignment method. Further, the molecular docking simulation revealed that all the quinazoline derivatives were situated at the same place as that of the standard drug erlotinib with reasonable penetration at the active site of the EGFR.
Results of this work provide the information regarding the structure activity relationship and important structure requirements for the interaction of compounds at the active site of the receptor.
This information provides a hint for the design of novel analogs as EGFR tyrosine kinase inhibitors.
Downloads pdf PDF, 1. In order to download, print or access these formats you must be logged in.Maneesh et al  synthesized a series of novel 2-trichloromethyl quinazoline derivatives bearing substituted secondary amine group at the 4th position and evaluated for their in vitro anti-tubercular activity .
Quinazolines and quinazolinones are classes of fused heterocycles that are of considerable interest because of the diverse range of their biological properties .Many substituted quinazoline and quinazolinone derivatives possess a wide range of bioactivities such as antimalarial, anticancer, antimicrobial, antifungal, antiviral, antiprotozoan, anti-inflammatory, diuretic, muscle relaxant.
Newly Synthesized Quinazoline Derivatives Hatem A. Abuelizz 1, Rabab El Dib 2,3, Mohamed Marzouk 4,5, seizure activity in some patients, but it frequently remains inadequate and the patients suffer from a applications such as anti-convulsant, anti-glaucoma and anti-cancer .
Maarouf A, El-Bendary E, Goda F. Synthesis and evaluation of some novel quinazolinone derivatives as diuretic agents. Arch Pharm., (10) ().
Mendoza C, Correa J, Nieto R, Marquez A, Aguilar R. Design, synthesis and biological evaluation of quinazoline derivatives as anti-trypanosomatid and anti-plasmodial agents.
Objective: The latest investigation was on synthesis, characterization of novel 4-anilinoquinazoline derivatives for their anti-angiogenic effect.
Method: A series of novel 4-anilino-6,7-dimethoxy quinazoline derivatives were synthesized and characterized using 1H, 13C NMR, FT .
Quinazoline derivatives are reported to have anti-inflammatory, analgesic, antibacterial, and anticancer activities.
The incorporation of "OCH₂CONH₂" (oxymethylcarbamide) at 4th position of the quinazoline ring was found to influence the biological activities of the molecules.