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Biodegradable coated paper materials represent one of the most promising alternatives to petroleum-based materials, including plastics and plastic-paper composite materials. Herein, fully biodegrad...

Paper is envisioned as an alternative to plastics in certain applications to overcome the problems associated with the excessive use of plastics. Water and oil repellency is one of the key requirem...

Coated paper substrates are used for a wide range of applications. The biggest challenge that remains unsolved with regard to coated paper is its recyclability. Herein, we report a unique approach ...

Excessive use of synthetic nondegradable polymers has led to the proliferation of microplastics in the oceans as well as polluted landscapes. Herein, we report a new sustainable approach for the de...

Introduction: Oxadiazoles having azo-functionality represent a new and an exciting class of physiologically active heterocyclic compounds. A number of molecules with these moieties have significant role in medicinal chemistry due to their diverse biological activities. Methodology: A series of 1,3,4-oxadiazole-2-thiol derivatives bearing azo-moiety have been designed and synthesized by multistep reaction sequences staring from p-aminobenzoic acid by employing literature know procedures. These compounds were investigated for their antimicrobial, cytotoxic, α-amylase and protein kinase inhibitory and antileishmanial potential. Results and Discussion: The newly synthesized compounds were characterized by spectroscopic techniques (IR, UV-Vis, NMR and MS). Antibacterial activity was investigated against four bacterial strains i.e. E. coli, P. aeruginosa, S. aureusand B. subtilis and good level of microbial inhibition was exhibited by most of the compounds with MIC 6.25 µg/mL. Brine Shrimp lethality assay revealed that the compound 31 is an excellent cytotoxic agent. (E)-5-(4-((4-Butoxyphenyl) diazenyl)phenyl)-1, 3,4-oxadiazole-2-thiol (21) showed good α-amylase inhibition (46.3± 0.45%) and (E)-2-(Decyloxythio)-5-(4-((propoxyphenyl)diazenyl)phenyl)-1,3,4-oxadiazole (30) exhibited excellent antileishmanial activity (88.4± 0.34%) at 10 µg/mL concentration. In case of protein kinase inhibition, remarkably, the oxadiazole-2-thiols (20-25) were found more active than the standard surfactinat tested concentration (25 µg/disc). Conclusion: We have designed, synthesized and characterized an interesting series of biologically active oxadiazole bearing diazene moiety derivatives. Noteworthy, the presence of diazene functionality, polar heterocyclic moiety as well as hydrophobic alkyl chain is special feature of these compounds. These studies provide a basic idea to further explore these types of scaffolds as biologically potent molecules in drug design and development.

Oxadiazoles have broad range of biological applications and have been investigated widely by the scientific community. In this study, we report the synthesis, X-ray diffraction, density functional theory (DFT) and α-amylase inhibition activities of three 1,3,4-oxadiazole derivatives (1–3). The compounds are synthesized in good yields (70–83%) and their structures are confirmed through different spectro-analytical techniques and single crystal X-ray diffraction. Density functional theory (DFT) calculations are performed to validate not only X-ray results, but also to investigate the dispersion of charges and reactivity through frontier molecular orbitals and molecular electrostatic potential (MEP) analyses. α-Amylase inhibition assay is performed in order to find out the enzyme inhibitory potential of the synthesized compounds (1–3). The low IC50 value (86.83 ± 0.23 μg/mL) of compound 2 reflects the potential α-amylase inhibitory activity of the compound as compared to others.

Background: Cancer is a far-reaching and lethal but curable disease. Researchers have investigated numerous anticancer agents with only a few commercially available effective drugs which are very costly. Objective: Herein, we report the synthesis , characterization and anti cancer assays of a series of novel dithiocarbamates derivatives. Methods: All compounds were synthesized from different secondary amines and substituted benzyl chlorides in a single step. The structures of newly synthesized dithiocarbamate derivatives were confirmed by spectroscopic techniques (IR, NMR and HR-MS). Results: The synthesized compounds showed a significant anti-proliferative effect in cancer cells (HeLa) with the maximum inhibitory activity of compound SHD-2 with an IC50 = 0.31 ± 0.09 μM. However, the same compound exhibited 19.2% inhibition towards Baby Hamster Kidney fibroblasts (BHK-21), normal cell lines. Moreover, quantification of cellular DNA by flow cytometry for the evaluation of pro-apoptotic activity in HeLa cells demonstrates that arrest in cell cycle along with apoptosis advance towards drug cytotoxicity. However, molecular docking studies of the potent compound suggested that it binds to the major groove of the DNA. Conclusion: The cytotoxic and pro-apoptotic potential of the potent inhibitor may be further investigated in the animal models to advance their anti-cancer prospective.

Elastase is the only enzyme that has the capability to degrade elastin and collagen, the two proteins essential for skin and bones. The synthesis of some densely substituted piperidines functionalized with the trifluoromethyl group (4a-j) was carried out. The newly prepared compounds were subjected to elastase enzyme inhibitory potential and antioxidant activity assays. Among the series, 4i (IC50 = 0.341 ± 0.001 μM) exhibited the maximum inhibition against elastase. Binding analysis delineated that the fluorine atom of ligand 4i showed hydrogen and hydrophobic bonds with Thr41 and Thr96, with bond distances of 3.84 and 5.631 A, respectively. The obtained results indicate that these trifluoromethyl functionalized piperidine derivatives could be considered as potential candidates to treat skin disorders.