A Review of Approaches to the Metallic and Non-Metallic Synthesis of Benzimidazole (BnZ) and Their Derivatives for Biological Efficacy.

Heterocyclic compounds are significant lead drug candidates based on their various structure-activity relationships (SAR), and their use in pharmaceutics is constantly developing. Benzimidazole (BnZ) is synthesized by a condensation reaction between benzene and imidazole. The BnZ structure consists of two nitrogen atoms embedded in a five-membered imide ring which is fused with a benzene ring. This review examines the conventional and green synthesis of metallic and non-metallic BnZ and their derivatives, which have several potential SARs, along with a wide range of pharmacological properties, including anti-cancer, anti-inflammatory, anti-microbial, anti-tubercular, and anti-protozoal properties. These compounds have been proven by pharmacological investigations to be efficient against different strains of microbes. Therefore, in this review, the structural variations of BnZ are listed along with various applications, predominantly related to their biological activities.

Surface-Induced in Situ Sonothermodynamically Controlled Functionalized Graphene Oxide for in Vitro Cytotoxicity and Antioxidant Evaluations.

Graphene oxide-based advanced functional materials offer an ultimate solution for wider biomedical applications. In situ thermodynamically ultrasound-assisted direct covalent functionalization of graphene oxide (GO) with sulfanilamide (SA) has synthesized f-(SA)GO. Raman spectroscopy, X-ray diffraction, high-resolution transmission electron microscopy, selected area electron diffraction pattern, scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy, ultraviolet-visible spectroscopy, thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC) have analyzed the f-(SA)GO structure for functional activities, expressed through synergistic impact of heteroatomic domains (SIHAD). The TGA of GO and f-(SA)GO demonstrates their total weight losses of 82.0 and 61.1%, respectively. Enhanced thermal stability of f-(SA)GO infers an exothermic behavior obtained with DSC. The surface-induced in situ thermodynamically controlled nonspontaneous reaction for f-(SA)GO has facilitated calculations for activation energy (E a) = - 2.65 × 103 kJ mol-1 and Gibbs free energy (ΔG) = 8.3741 kJ mol-1, energetics for biological activities with sulforhodamine B assay on MCF-7 and Vero cell lines and antioxidant potential by free radical scavenging activity with DPPH (2,2-diphenyl-1-picrylhydrazyl). Cell viabilities are >89.8% for Vero and >90.1% for MCF-7 with f-(SA)GO over 10 to 80 µg mL-1. Its cytocompatibility infers establishment of a new material. The morphological effect on MCF-7 and Vero cell lines confirm its structurally stable biocompatibility. The SIHAD of f-(SA)GO scavenges radical activity, and its heteroatomic structure causes valuable physiochemical activities. f-(SA)GO could emerge as an advanced functional biomaterial for structurally and thermally stable biocompatible nanocoatings.

Dispersion enhancing effect of sonochemically functionalized graphene oxide for catalysing antioxidant efficacy of curcumin.

The non-hazardous sonochemical approach has been developed for the functionalization of graphene oxide (GrO) with 5-Aminoindazole (5-AIND). The formation of f-(5-AIND) GrO is confirmed with 13C solid state NMR, HRXPS, XRD, Raman, TGA, DSC, FTIR etc. The >80% cell viabilities on MCF-7 and Vero cell lines have confirmed the high cytocompatibility of f-(5-AIND) GrO. Additionally, the morphological impact on Vero cell line has evidently confirmed the biocompatibility of f-(5-AIND) GrO. As compared to GrO, the f-(5-AIND) GrO has demonstrated an enhanced antioxidant efficacy of 69.4-72%, evaluated with 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radical assay. With a similar objective (0.01-0.05)mL peanut oil based curcumin micro and nanoemulsions have been prepared using ethanol and glycerol as co-solvent and co-surfactant respectively. The prepared emulsions are subsequently characterised with respect to morphological and physicochemical parameters via density, surface tension, viscosity, friccohesity measurement and DLS analysis. Henceforth, with an expectation to achieve higher dispersion, an ethanolic dispersion of f-(5-AIND) GrO has been mixed with curcumin carrying emulsions in 1:1. Notably, the radical scavenging activities (RSA) of the combined formulations are significantly enhanced to an extent of 26.6%.

In situ sonochemical reduction and direct functionalization of graphene oxide: A robust approach with thermal and biomedical applications.

The rapid, robust, scalable and non-hazardous sonochemical approach for in situ reduction and direct functionalization of graphene oxide has been developed for non-toxic biomedical applications. The graphene oxide (GrO) was directly functionalized with tryptamine (TA) without using any hazardous acylating and coupling reagents. The reaction was completed within 20min. An impact of ultrasound was inferred for a direct functionalization with other conventional methods. The evolved electronic states were confirmed with near edge X-ray absorption fine structure (NEXAFS). The direct covalent functionalization and formation of f-(TA) GrO was proven with FTIR, 13C solid state NMR, XPS, XRD, Raman' HRTEM, AFM and TGA. The total percentage weight loss in TGA confirms an enhanced thermal stability of f-(TA) GrO. The f-(TA) GrO was further explored for an investigation of in vitro antimicrobial activity to ensure the health and environmental safety. An outstanding antibacterial activity of f-(TA) GrO was found against gram positive Staphylococcus aureus at MIC 128mgmL-1. It confirms a suitability of f-(TA) GrO for thermally stable antibacterial coating. The f-(TA) GrO showed 39.14-48.9% antioxidant activities, evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical assay. The inherent cytotoxicity of f-(TA) GrO was evaluated with SRB assay to living cells, MCF-7 and Vero. The estimated cell viabilities were >80% upon addition of f-(TA) GrO over a wide concentration range of 10-80µgmL-1. The high cytocompatibility of f-(TA) GrO confirms the low toxicity and an excellent biocompatibility. The morphological effect on Vero cell line, evidently confirmed the biocompatibility of f-(TA) GrO. Therefore, f-(TA) GrO was emerged as an advanced functional biomaterial for thermal and biomedical applications.

Ultrasound assisted simultaneous reduction and direct functionalization of graphene oxide with thermal and cytotoxicity profile.

The new sonochemical approach for simultaneous reduction and direct functionalization of graphene oxide (GrO) has been developed. The GrO was functionalized with 2-Aminobenzoxazole (2-ABOZ) in twenty min with complete deletion of hazardous steps. The significance of ultrasound was exemplified with the comparative conventional methods. The newly prepared f-(2-ABOZ)GrO was extensively characterized with near edge X-ray absorption fine structure (NEXAFS) spectroscopy, 13C solid state NMR, XPS, XRD, HRTEM, SAED, AFM, Raman, UV-vis, FTIR and TGA. The thermal stability of f-(2-ABOZ)GrO was confirmed with total percentage weight loss in TGA. The biological activity of f-(2-ABOZ)GrO was explored with MCF-7 and Vero cell lines. The inherent cytotoxicity was evaluated with SRB assay at 10, 20, 40 and 80µgmL-1. The estimated cell viabilities were >78% with f-(2-ABOZ) GrO. A high cytocompatibility of f-(2-ABOZ)GrO was ensured with in vitro evaluation on living cell lines, and low toxicity of f-(2-ABOZ)GrO was confirmed its excellent biocompatibility. The morphological effect on Vero cell line evidently supports the formation of biocompatible f-(2-ABOZ)GrO. Therefore, f-(2-ABOZ)GrO was emerged as an advanced functional material for thermally stable biocompatible coatings.