Quinazoline is a compound with amalgamated heterocyclic system popular for their biological activities. Quinazoline is a compound made up six membered fused aromatic rings i,e a benzene ring with pyrimidine ring. Its chemical formula is CHNO. It is yellow colour and found in the crystalline form. Molecular optimization of potentially lead compounds through a chemist is an needy and upcomming approach for the discovery of new pharmaceuticals. More than two combinations of pharmacophore and making them one moiety is a noval and popular procedure of exploitation of synthesis now a days and this cause an additive increment of biological activities with taking away of surplus side effects. Present communication studies about the structure origin, diversity and chemical modification with change in pharmacological activities of Quinazoline.
Imide is the configuration of amide in which the nitrogen atom is affix to two carbonyl group. Imide mention to any compound which carry the divalent radical. Phthalimide possess a structural feature CHNO and an imide ring which help them to be biologically active and pharmaceutically useful.Phthalimides have served as starting materials and intermediates for the synthesis of many types of alkaloids and pharmacophores.In view of broad biological activity of phthalimide, we herein plan to synthesize a series of new phthalimide derivatives by incorporating new pharmacophores at various positions with the hope to get therapeutically active compounds. The aim the study is to synthesize phthalimide derivatives by using microwave assisted synthesis method and compare the activity of the synthesized molecules. Thus, the current communication employed the technology gracefully for the synthesis, identification and characterization of some novel derivatives by the reaction of Phthalic anhydride with urea, glycine, aniline, sulphanilic acid to yield various Phthalimide derivatives using domestic microwave by getting percentage yield 70.7%, 76.65%, 80.21% and 73.78% of synthesized compound BBBand Brespectively. The compound B(92.86%) showed higher percentage practical yield. All synthesized compound(s) were subjected to melting point determination, TLC analysis, column chromatography (for purification), H-NMR and Mass Spectrometry. All synthesized derivatives were subjected for DDPH scavenging activity, in which compound Bwas found to have high anti-oxidant potential (69.56%) when ascorbic acid was taken as standard. All the chemicals used were of highly pure and procured from Central Drug House (New Delhi).
Heterocyclic compounds especially, five or six-member heterocyclic compounds, having one to three hetero-atoms in their nucleus take part in metabolism of all living cells. And this information gives the lead for synthesizing heterocyclic derivatives. This research work has focused on development of new method for synthesis of some new amino acid substituted 1,2,4-trizole derivative from 1, 3, 4-Oxadizole nucleus. The nucleus of the 1, 3, 4-Oxadizole was first produced by reaction of Isoniazide and 3-chlorobenzeldehyde which is then converted into 1,2,4-trizole derivative by the loss of water molecule. After that incorporation of different amino acid (luecine and glycin) leads new amino acid substituted 1,2,4-trizole derivative. The newly synthesized derivative Compound A1 and A2 were characterized by optical rotation, melting point, TLC, UV spectroscopy and IR. The antibacterial was screened using Disc diffusion method with ciprofloxacin as reference drug and antioxidant activity by in-vitro DPPH method using ascorbic acid as standard drug. Synthesized compound A1 showed maximum MIC against S. aureus as compared to Compound A2. For antioxidant activity, compound A1 showed maximum percentage inhibition as compared to Compound A2.
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