2,5-Disubstituted 1,3,4-oxadiazole compounds are one of the most attractive classes for researchers due to their pharmacological activities. In the current research, a new series of 2-[[5-alkyl/aralkyl-1,3,4-oxadiazol-2-yl]thio]-N-[4-(4-morpholinyl)phenyl]acetamides (6a–m) were prepared by converting different aryl/aralkyl organic acids (1a–m) successively into corresponding esters (2a–m), hydrazides (3a–m) and 5-aryl/aralkyl-1,3,4-oxadiazol-2-thiols (4a–m). Finally, the target compounds 6a–m were synthesized by stirring 5-aryl/aralkyl-1,3,4-oxadiazol-2-thiols (4a–m) with 2-bromo-N-[4-(4-morpholinyl)phenyl]acetamide (5) in the presence of N,N-dimethylformamide (DMF) and sodium hydride (NaH). The structures of the synthesized compounds were elucidated through IR, ¹H-NMR, ¹³C-NMR and mass spectral data. The compounds were also screened for antimicrobial and hemolytic activity and most of them were found to be active against the selected microbial species at variable extent relative to reference standards. The compounds, 6d and 6f were active against the selected panel of microbes and the former was the most potent one. This series showed less toxicity and may be considered for further biological screening and application trial except 6h and 6l, possessing higher cytotoxicity.

Triazole-based acetamides serve as important scaffolds for various pharmacologically active drugs. In the present work, structural hybrids of 1,2,4-triazole and acetamides were furnished by chemically modifying 2-(4-isobutylphenyl) propanoic acid (1). Target compounds 7a–f were produced in considerable yields (70–76%) by coupling the triazole of compound 1 with different electrophiles under different reaction conditions. These triazole-coupled acetamide derivatives were verified by physiochemical and spectroscopic (HRMS, FTIR, ¹³CNMR, and ¹HNMR,) methods. The anti-liver carcinoma effects of all of the derivatives against a HepG2 cell line were investigated. Compound 7f, with two methyl moieties at the ortho-position, exhibited the highest anti-proliferative activity among all of the compounds with an IC₅₀ value of 16.782 µg/mL. 7f, the most effective anti-cancer molecule, also had a very low toxicity of 1.190.02%. Molecular docking demonstrates that all of the compounds, especially 7f, have exhibited excellent binding affinities of −176.749 kcal/mol and −170.066 kcal/mol to c-kit tyrosine kinase and protein kinase B, respectively. Compound 7f is recognized as the most suitable drug pharmacophore for the treatment of hepatocellular carcinoma.

The study focuses on the fabrication of silver nanoparticles (Ag NPs) using aqueous extracts of Allium sativum as reducing agents. Silver ion becomes a good carrier of bioactive compounds of Allium sativum, so their biochemical potential such as total phenolic and flavonoids were evaluated. Results showed that as a concentration increases TPC and TFC were also increased. Similar to their secondary metabolite, scavenging potential of Ag NPs of Allium sativum was also monitored. Green synthesized Ag NPs exhibited significant antibacterial activity 24±2.6, 22±1.4, 19±2.7 and 20±3.17 against B. subtilis, S. aureus, E. coli and P. multocida bacterial strains respectively. Moreover, Ag NPs of garlic did not show any mutagenicity against mutant strain of S. typhimurium TA98 & TA100. Brine shrimp lethality assay (BSLA) showed their dose dependent effect. Finally, green synthesized Ag NPs of garlic presented anti-proliferative effect against HEPG2 cell line.

A series of new N-substituted derivatives of 3-[(5-{1-[(4-chlorophenyl)sulfonyl]-3-piperidinyl}-1,3,4-oxadiazol-2-yl)sulfanyl]propanamide (7a–q) was synthesized to evaluate new drug candidates for Alzheimer’s disease. 4-Chlorobenzenesulfonyl chloride (a) and ethyl piperidin-3-carboxylate (b) were converted into 5-{1-[(4-chlorophenyl)sulfonyl]-3-piperidinyl}-1,3,4-oxadiazol-2-thiol (3) through a series of three steps. A series of electrophiles, N-alkyl/aralkyl/aryl-3-bromopropanamide (6a–q), was synthesized by gearing up 3-bromopropionyl chloride (5) with different alkyl/aralkyl/aryl amines (4a–q). Target compounds were synthesized by reacting compound 3 with different electrophiles, 6a–q, under basic conditions in an aprotic polar solvent. The synthesized compounds were subjected to spectral analysis, EI-MS, IR, ¹H-NMR and ¹³C-NMR, for structural elucidation. The compounds were screened for enzyme inhibition activity against acetyl cholinesterase (AChE) enzyme. The validity of synthesized compounds as new drug candidates was also evaluated through haemolytic activity.