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Ph.D.
(Pharmacy)
DESIGN, SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL
EVALUATION OF SOME NOVEL QUINAZOLINE DERIVATIVES FOR
METABOLIC DISORDERS
Ph.D. Scholar : Modh Pratik Girishbhai
Research Supervisor : Dr. L. J. Patel

Regi. No.: 17146021002
Abstract :
A novel series of quinazolinone derivatives was designed based on a literature review,
basic chemistry principles and docking study using AutoDock software. All designed
compounds with good docking scores and inhibitory constants were checked for their
Druglikeness and ADME properties using the SwissADME web tool. They show good
drug-likeness properties, TPSA and absorption parameters and synthesis protocol of
such selected targets of quinazolinone-4(3H)-one derivative was achieved.

This synthesis protocol includes a synthesis of benzamide derivatives from anthranilic
acid using acid-amine reaction, followed by the cyclization using catalytic
ptoluenesulfonicacid monohydrate and oxidation using (diacetoxyiodo)benzene to give
Bromo substituted quinazolin-4(3H)-ones, which were cross coupled to suitable boronic
acid and alkyne derivatives using Suzuki-Miyaura and Sonogashira conditions
respectively with a suitable catalyst, base and solvent system to afford corresponding 2,
3 and 6 substituted quinazolin-4(3H)-ones (GUNI-1 to GUNI-30) with moderate to high
yields.

Synthesized compounds and key intermediates were characterized by FTIR, LC-MS,
1HNMR and a few with 13C-NMR analysis and their structure were confirmed as desired.
In vitro biological evaluation was carried out for synthesized targets for anti-obesity and
anti-diabetic activity using pancreatic lipase inhibition, alpha-amylase and
alphaglucosidase inhibition and non-enzymatic inhibition of hemoglobin glycosylation
assay with reported methods and some compounds show good potential for ant-obesity
and anti-inhibitory activity.

Key words: Quinazolin-4(3H)-one/Quinazolinone, Obesity, Diabetes, Metabolic disorders,
Docking, Druglikeness, AutoDock, carbon-carbon cross-coupling reactions, cyclization,
pancreatic lipase inhibition, anti-obesity agents, alpha-amylase/alpha-glucosidase
inhibition, In Vitro, In silico

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