Catalyst-Free Expeditious Synthesis Of 2-(4-TERT-BUTYLPHENYL)-3-Sustituted Quinazolin-4(3H)-One Derivatives

Quinazoline and quinazolinone derivatives are well-known bioactive heterocycles owing to their therapeutic diversity and extensive medicinal application in drug design and pharmaceutics. A series of 2-(4-tert-butylphenyl)-3-substituted quinazolin-4(3H)-one derivatives, 2a-q was herein synthesized from benzoylational conversion of anthranilic acid to 2-(4-tertbutylphenyl)-4H-3,1-benzoxazin-4-one, 1 which was the first precursor which was subsequently transformed to the targeted 2,3-disubstituted quinazolin-4(3H)-one derivatives, 2a-q by reacting with some cheap and readily accessible amino-containing moieties via an ameliorable pathway. The catalyst-free synthesis was successfully achieved by careful reaction optimization study using solvent choice and reaction temperature variability as key parameters. The chemical structures of the synthesized compounds were confirmed by IR, UV, 1H-NMR, 13C-NMR and DEPT-135 as well as analytical data. The data obtained were consistent with the proposed structures of the compounds. This targeted quinazoline motifs might pave way for new bioactive template from future drug development

FACILE SYNTHESIS AND SPECTROSCOPIC CHARACTERIZATION OF SULFONAMIDE BEARING DIVERSIFIED CARBOXAMIDE AND HYDRAZINE CARBOXAMIDE MOIETIES

This current research describes the eco-friendly synthesis of N-(s-phenyl)-3-phenyl-2-(phenyl sulfonamido) propanamides which are sulfonamide bearing diversified carboxamide moieties. The incorporation of amido functionality into the sulfonamide moieties was herein achieved in three steps in a cost-effective manner by starting from cheap amino acid, phenyl alanine which was reacted with benzenesulfonyl chloride to produce sulfonamide which upon subsequent esterification followed by amidation furnished carboxamido-incorporated sulfonamide analogs 9a-j in good to excellent yield. The completion of reaction processes was authenticated with Thin Layer Chromatography (TLC) and the chemical structures were validated through the elemental analysis result as well as spectroscopic means which include FT-IR, UV, 1H and 13C NMR. The technique used herein was found to be efficient and cost-effective for the production of the series of carboxamide diversified sulfonamide derivative

Synthesis, morphological, optical properties of functionalized La0.33Ca0.67MnO3 for antibacterial therapy

A functionalized paramagnetic manganite La0.33Ca0.67MnO3 was investigated for its morphological, optical and antimicrobial properties. The manganite was capped by using a citrate ligand. The UV-visible spectrophotometer was used in monitoring the optical bands of the metal-citrate complex. It was observed to absorb in the visible region. The metal-citrate was reacted with a biologically active ligand (N-(3-nitrophenyl)-3-phenyl-2-(phenylsulfonamido) propanamide). The optical bands observed from the metal-citrate were used in monitoring the reaction between the metal-citrate and N-(3-nitrophenyl)-3-phenyl-2-(phenylsulfonamido) propanamide). The morphological property of the product formed was determined using SEMEDAX. The effect of the complex formed on the organic ligand, N-(3-nitrophenyl)-3-phenyl-2- (phenylsulfonamido) propanamide) was determined using 1H and 13C NMR. The bacterial inhibitory property of the metal-citrate- N-(3-nitrophenyl)-3-phenyl-2-(phenylsulfonamido) propanamide) complex was determined against Pseudomonas aeruginosa and Staphylococcus auerus. It was observed to inhibit the growth of Staphylococcus aureus only. The biological activities of the metal-citrate N-(3-nitrophenyl)-3-phenyl-2-(phenylsulfonamido) propanamide) suggest its use as an alternative antibacterial therapy

Facile synthesis of N’-(anthracen-9(10H)-ylidene)-4-(4- hydrophenyl)-6-methyl-2-oxo-1,2,3,4-tetra hydropyrimidine- 5-carbohydrazide and other derivatives

Pyrimidine as vital constituents of nucleic acid is recognized for its role in the chemotherapy of AIDS. Hydrazide-hydrazones are important moieties with notable biological diversity in drug design. Thus, the aim of this present study is to synthetically couple these two frameworks together in order to achieve small molecular targets for possible development of improved therapeutic candidates. This was achieved in a domino reaction starting with one-pot three-component reaction to afford ethyl-4-(4-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4- tetrahydropyrimidine-5-carboxylate, 7 which upon treatment with hydrazine hydrate under acid-mediated condition gave 8,as an essential precursor and reactive intermediate. The expeditious condensation of intermediate 8 with various cyclic and straight chain ketones furnished N’-(anthracen-9(10H)-ylidene)-4-(4-hydrophenyl)-6-methyl-2-oxo-1,2,3,4- tetrahydropyrimidine-5 -carbohydrazide 9a and other 9b-i scaffolds as envisaged. The reaction progress was monitored by thin layer chromatography (TLC) and upon reaction completion, the purification process was carried out with recrystallization and/or column chromatography. The authenticity of the prepared products 9a-i was confirmed by spectroscopic means including IR, UV, 1H-NMR, 13C-NMR and DEPT-135 as well as analytical data. These final products are good candidates for further study as regards anti-plasmodial activity which are been developed and examined

Heterogeneous Acid Catalyzed Synthesis and Spectroscopic Characterization of Schiff Bases Derived from Chalcone Derivatives

Schiff bases have continued to gain attention as essential building blocks and versatile pharmacophores in drug development and drug-like molecular entities. Thus, the synthesis of Schiff bases was achieved herein via facile acetic acid catalyzed synthetic transformation of chalcones. The targeted Schiff bases and related compounds 2a-m were accessed by the treatment of amines with chalcone 1 which was previously derived through Claisen-Schmidt reaction between benzaldehyde and acetone, at ambient temperature. Structural characterization was achieved via physicochemical properties and the use of IR, UV, 1H and 13C NMR which were spectroscopic techniques. The compounds have essential candidature for further study, in biological activity so as to unleash their medicinal potential

Facile synthesis of N’-(anthracen-9(10H)-ylidene)-4-(4- hydrophenyl)-6-methyl-2-oxo-1,2,3,4-tetra hydropyrimidine- 5-carbohydrazide and other derivatives

Pyrimidine as vital constituents of nucleic acid is recognized for its role in the chemotherapy of AIDS. Hydrazide-hydrazones are important moieties with notable biological diversity in drug design. Thus, the aim of this present study is to synthetically couple these two frameworks together in order to achieve small molecular targets for possible development of improved therapeutic candidates. This was achieved in a domino reaction starting with one-pot three-component reaction to afford ethyl-4-(4-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4- tetrahydropyrimidine-5-carboxylate, 7 which upon treatment with hydrazine hydrate under acid-mediated condition gave 8,as an essential precursor and reactive intermediate. The expeditious condensation of intermediate 8 with various cyclic and straight chain ketones furnished N’-(anthracen-9(10H)-ylidene)-4-(4-hydrophenyl)-6-methyl-2-oxo-1,2,3,4- tetrahydropyrimidine-5 -carbohydrazide 9a and other 9b-i scaffolds as envisaged. The reaction progress was monitored by thin layer chromatography (TLC) and upon reaction completion, the purification process was carried out with recrystallization and/or column chromatography. The authenticity of the prepared products 9a-i was confirmed by spectroscopic means including IR, UV, 1H-NMR, 13C-NMR and DEPT-135 as well as analytical data. These final products are good candidates for further study as regards anti-plasmodial activity which are been developed and examined.Covenant University is immensely acknowledged by all the authors for her financial support for this work. OOA is grateful to TWAS for sponsorship with Grant No. 14-069 RG/CHE/AF/AC_1.http://iopscience.iop.org/1742-6596am2020Chemistr

Heterogeneous acid catalyzed synthesis and spectroscopic characterization of Schiff bases derived from chalcone derivatives

Please read abstract in the article.Covenant Universityhttp://ejchem.journals.ekb.egam2022Chemistr

Dimethylformamide-mediated synthesis and characterization of novel pyrazole- and pyrimidine-based 3,4- dihydropyrimidine-2(1H)-thione derivatives

Pyrimidine, an essential component of nucleic acid is currently reported for its potential application in Acquired Immune Deficiency Syndrome (AIDS) chemotherapy. Also, pyrazole nucleus, a versatile heterocyclic compound is gaining more attention in drug designs owing to its pharmacological therapeutic potentials. Hence, this present study deals with cost effective synthesis of 6-methyl-4-phenyl-5-(substituted-5-phenyl-4H-pyrazol-3-yl)-3,4- dihydropyrimidine-2(1H)-thione derivatives which are concisely known as pyrazole-based pyrimidine scaffolds. The multicomponent reaction of benzaldehyde, acetyl acetone and thiourea in the presence of catalytic amount of hydrochloric acid (HCl)ab initio produced 5- aceto-4-phenyl-2-thioxo-1,2,3,4-tetrahydropyrimidine, 1. Later, room temperature Claisen- Schmidt condensation of precursor 1 with diverse aromatic aldehydes which were benzaldehyde derivatives led to the formation of α,β-unsaturated carbonyl side chain, 2a-h. Finally, the thermal annellation through synthetic cyclization furnished crude products which were purified by recrystallization to afford 6-methyl-4-phenyl-5-(substituted-5-phenyl-4Hpyrazol- 3-yl)-3,4-dihydropyrimidine-2(1H)-thione derivatives 3a-h in a cheap condition. The chemical structures were authenticated using IR, UV, 1H-NMR and 13C-NMR as well as analytical data. The final products 3a-h possessed good candidature for further investigation regarding their biological activities and pharmacological potential for new drug discovery