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This research suggests an ideal method for synthesizing propargyl amine adducts by a three-component condensation of dibenzyl amine (DBA), aldehyde, and phenylacetylene (known as A 3 coupling reactions). The aimed synthesis was carried out using a gold catalyst, chlouro auric acid (HAuCl 4 ) and compared with Cu(I) systems to check the involvement of metals to generate enantiomerically pure compounds (4 a-4 j).No major deactivation of the catalyst was observed after repeated use in a similar reaction system (> 10 times). The derived motifs' spectroscopic profiling ( 1 H NMR, 13 C NMR, APT, IR and MS) has confirmed the structural fragments in a single core. Moreover, the applications of the derived motifs confirmed the comparable antimicrobial activity in some selected Gram-positive and Gram-negative bacterial; and fungi strains. Our consequences show that the scaffolds 4 d and 4 i having 4-F and 4-NMe 2 substitution in the araldehyde system exhibited potent antimicrobial activity in most used bacterial and fungi strains.

Background: A new series of ten composites with sulphur based carboxylic acid and benzylamine were synthesized by Ugi 4-components reaction (Ugi-4CR) and screened for antituberculosis activity against the Mycobacterium tuberculosis H37Rv strain. Objective: Target compounds were isolated, purified, identified, and characterized by MS, FT-IR, 1H-NMR, APT, and 13C-NMR then the antituberculosis activity was examined by Microplate Alamar Blue Assay (MABA) method. Methods: This study was based on the articulation of carboxamide linkage bearing S-linkage in the core unit by reacting four different units, i.e., 2-(pyrimidin-2-ylthio)acetic acid, aromatic aldehyde, benzylamine and tertiary butyl isocyanide at RT in an atom economy route of synthesis. The desired product (5a-5j) was synthesized via one-pot and Metal-free conditions. Results: Compounds (5a-5j) synthesized in good yields and compared to MIC values of Isoniazid 0.05 (µg/mL), Rifampicin 0.1 (µm/mL), and Ethambutol 1.56 (µg/mL) as a positive control. Conclusion: Synthesized compounds give excellent yield. Among the ten derivatives, compound 5f has comparable antituberculosis activity