ALUMINA CATALYST: SYNTHESIS OF NOVEL QUINAZOLINE DERIVATIVES AND THEIR SOLUBILITY INCREASES THROUGH INCLUSION WITH β-CYCLODEXTRIN
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2019, Vol 11, Issue 2
Abstract
Objective: To synthesis a novel methodology of bioactive quinazoline derivatives under greener process to an excellent yields and increases their solubility via inclusion with β-cyclodextrin (CD). Methods: Derivatives of quinazoline compounds were prepared by the mixture of 3-amino-2-phenylquinazolin-4(3H)-one, derived from 2-phenyl-4H-benzo[1,3]oxazin-4-one by refluxing with hydrazine, substituted aromatic aldehyde and alumina intimately in an agate mortar and pestle under solvent-free condition. Using various techniques for preparing inclusion complexes, kneaded method is the best method for encapsulation in host-guest complex chemistry. All compounds including inclusion complexes were characterised by spectral methods. Results: Synthesized a series of novel quinazoline compounds under a very easier greener process with a commercially available reagent. However, their low bioavailability, due to low absorption and solubility, can limit their potential applications. CD was used to resolve this solubility problem. CD can easily accommodated the guest molecules to encapsulate inside its cavity due to interior the hydrophobic nature with a hydrophilic exterior part to form thermodynamically more stable molecular microcapsules, commonly name as host-guest complexes or inclusion complexes. In this sense, CD was utilized to enhance not only the solubility and bioavailability of these quinazoline compounds but also their antibacterial capacity. The formation of inclusion complex was thus confirmed by ultraviolet-visible spectroscopy (UV-VIS), Fourier Transform Infrared Spectrometry (FT-IR), differential scanning calorimetry (DSC) and solubility study technique. Conclusion: Here we have successfully unfolded an eco-friendly methodology for the synthesis of derivatives of quinazoline and increased their solubility via host-guest inclusion technique. From the spectral analysis, it was concluded that the quinazoline compound is fully encapsulated inside the cavity of the CD.
Authors and Affiliations
Mossaraf Hossain, Ashis Kumar Nanda
Keywords
Related Articles
- EP ID EP566036
- DOI 10.22159/ijpps.2019v11i2.30338
- Views 92
- Downloads 0
MODULATING THE BIOSYNTHESIS OF A BIOACTIVE STEROIDAL SAPONIN, CHOLESTANOL GLUCOSIDE BY LASIODIPLODIA THEOBROMAE USING ABIOTIC STRESS FACTORS
Objective: The present study investigates the modulation of cholestanol glucoside (CG) biosynthesis by Lasiodiplodia theobromae in response to oxidative, osmotic and heat shock stresses.Methods: The fungal cultures were...
PHYTOCHEMICAL, ANTI-INFLAMMATORY, ANTIOXIDANT, CYTOTOXIC AND ANTIBACTERIAL STUDY OF CAPPARIS CARTILAGINEA DECNEFROM YEMEN
Objective: To investigate phytochemicals and biological activities of Capparis cartilaginea extracts.Methods: The methanolic extracts of leaves, stem and twigs of C. cartilaginea were screened for their phytochemicals. T...
IDENTIFICATION OF LEAD COMPOUNDS WITH COBRA VENOM DETOXIFICATION ACTIVITY IN ANDROGRAPHIS PANICULATA (BURM. F.) NEES THROUGH IN SILICO METHOD
Objective: To validate the cobra venom detoxification activity in Andrographis paniculata and identification of lead molecules.Methods: The structures of phytochemicals were procured from databases or created by ChemSket...
ANTIBACTERIAL AND ANTIFUNGAL ACTIVITY OF LEAVES OF THESPESIA POPULNEA
Objective: To find out the antibacterial and antifungal activity of T. populnea leaves against bacterial and fungal strains.Methods: T. populnea leaves were extracted successively with different solvents viz., hexane, ch...
FORMULATION AND EVALUATION OF TABLET PREPARED BY COAMORPHOUS SYSTEM CONTAINING ANTI-HYPERTENSIVE AND ANTI-HYPERLIPIDEMIC DRUG
Objective: Amlodipine besylate (AML) and Atorvastatin calcium (ATR) belong to biopharmaceutical classification system (BCS) class II (i.e. low solubility and high permeability) which leads to variable bioavailability. He...