Day 1 :
Keynote: Anti-Inflammatory activity Of newly synthesized 7-chloro-2-methyl-4H-benzo [d] [1,3]-oxazin-4-one and 3-amino-7-chloro-2-methyl-quinazolin-4(3H)-one
Time : 10:30-11:00
Heterocyclic chemistry comprises at least half of all organic chemistry research worldwide in particular, heterocyclic structures form the basis of many pharmaceutical, agrochemical and veterinary products.
Methods: The condensation of Methyl-2-amino-4-Chlorobenzoate with acetic anhydride yielded the cyclic compound 2-methyl 7-Chloro-1, 3-benzo-oxazine-4-one (1) which further produce 3-Amino-2-Methyl 7-Chloro quinazolin-4(3H)-ones (2) via the reaction with hydrazine hydrate. The compounds synthesized were unequivocally confirmed by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography-Mass spectrophotometry and Elemental analysis. Results: Compound 1 and 2 has Anti-inflammatory activity of 96.78%, 95.71% and 97.62%, 95.35% at 10mg/kg and 20mg/Kg dose levels.
Discussion: Compound 1 has IR spectrum showed signals for carbonyl functional group at 1662 cm-1, C-O and C-H stretch vibrations at 1102 cm-1 and 2871 cm-1respectively. The 1H NMR spectrum showed three aromatic protons at δH 7.59, 7.16 and 6.40 and a vinyl methyl protons at δH 2.57..In the 13C NMR spectrum, the ester carbonyl resonated at δC 168.08, while the aromatic carbons resonated in the range δC 113.40 – 149.23. The resonances at δC 153.13 and δC 22.15 were due to the imine oxygenated carbon (C-1) and the methyl carbon respectively. Compound 2, had NMR data similar to1, except for an additional signal at δH 5.80 in the 1H NMR spectrum which was attributed to the amino protons (2H).
Conclusion: Compound 2 had a higher anti-inflammatory activity than Compound 1. The compounds synthesized had a higher anti-inflammatory activity than Indomethacin, a standard anti-inflammatory drug.
Victor Bekhterev is a specialist in chemical analysis and separation processes. Has experience in the development of methods for the determination of organic compounds in biological objects, food products and environment. Currently, he is a Professor at the Department of engineering and environmental of Sochi state university in Sochi (Russia).
The solution of many problems in the analytical chemistry, ecology, hydrochemistry, biochemistry, pharmacology, toxicology are associated with the extraction and separation of the natural or synthetic organic compounds from aqueous media or from water-containing biological samples. In this report, a new approach to the isolation of hydrophilic organic substances from aqueous media in extractant is proposed: the extraction under the conditions of formation of the phase interface in the initially homogeneous system by thermal action.
A method of extractive freezing-out under the action of centrifugal forces (EFC) with the use of hydrophilic organic solvents has been developed [Patent RU2564999, Patent EP3357873]. The scientific basis of this method has been created, and the regularities of extraction of target components in the conditions of formation of the liquid – solid phase interface have been established. The EFC-methods in combination with GC and HPLC for determination of various organic substances are fast, cheaper and easier than QuEChERS. The expert's working conditions and safety have been improved by using a minimum amount of solvents.
A method of vapor-phase extraction (VPE) of organic substances from aqueous solutions is proposed [Patent RU2296716]. Its methodological foundations are developed, and the conditions for extraction of various substances are optimized. The partition coefficients of some hydrophilic and hydrophobic organic compounds in the water-extractant’s vapor system are determined. On the basis of theoretical representations for VPE the features of changing of the Gibbs energy are established in homological series of low-molecular carboxylic acids and phenols.
Based on this approach, new methods have been developed for determination of important analytes in water (natural and waste) and biological objects: drugs and narcotic substances in human urine, blood and organs, pesticides in the environment and food, food additives, biologically active substances in plants.