The leaf, stem and root decoctions of Petiveria alliacea (referred to as Anamu or Apacin (Guatemala), Guinea–Hen weed (English), Awogba or Ojusaju (Yoruba), kanunfari (Hausa) and Akwa-ose (Igbo) have been used as a diuretic, antispasmodic, sedative, analgesic and anti-inflammatory agents in traditional medicine. Cold maceration and Soxhlet extraction techniques were used to obtain oils from the leaf, stem and root of P. alliacea. The oils were analysed for their antimicrobial properties using brothmicrodilution technique while their antioxidant properties were determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) tests. The antimicrobial tests on the following micro-organisms Salmonella typhi, Staphylococcus aureus, Bacillus subtilis, Escherichia coli,as well as the anti-fungi test on Rhizopus sp., and Aspergillus niger, showed that the hexane and ethanol cold leaf extracts were most effective in limiting the growth of Salmonella typhi with minimum inhibitory concentration (MIC)value of 3.125 µg/mL and minimum bactericidal concentration (MBC)value of 6.25 µg/mL. The ethanol leaf extracts using Soxhlet extraction technique were most effective at MIC value of 3.125 µg/mL on Staphylococcus aureus, Escherichia coli. Likewise, the hexane and ethanolcold leaf extracts were most effective in limiting the growth of Rhizopus sp. and Aspergillus niger with MIC value of 3.125 µg/mL and minimum fungicidal concentration (MFC) value of 6.25 µg/mL.

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, 1 H and 13 C NMR which were spectroscopic techniques. The compounds have essential candidature for further study, in biological activity so as to unleash their medicinal potential.

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-4H-pyrazol-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.

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, 1 H and 13 C NMR. The technique used herein was found to be efficient and cost-effective for the production of the series of carboxamide diversified sulfonamide 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.