ChemInform Abstract: Microwave Assisted Organic Synthesis: A Green Chemical Approach

Ameta, Chetna; Ameta, Aarti; Ameta, Rakshit; Punjabi, P. B.; Ameta, Suresh C.

doi:10.1002/chin.201219227

Cited by 16 publications

(16 citation statements)

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“…Since the first reported microwave utilization techniques in organic synthesis in 1986, microwave techniques have become a recognized laboratory system and they have an important synthetic approach in the field of chemistry [58]. Moreover, these methodologies are therefore being used as an important synthetic tool [59][60][61][62][63]. For these reasons, our group has been interested in using microwave approaches to achieve our synthetic goals [64][65][66][67] in the last few years.…”

Section: Introductionmentioning

confidence: 99%

Innovative Three-Step Microwave-Promoted Synthesis of N-Propargyltetrahydroquinoline and 1,2,3-Triazole Derivatives as a Potential Factor Xa (FXa) Inhibitors: Drug Design, Synthesis, and Biological Evaluation

et al. 2020

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The coagulation cascade is the process of the conversion of soluble fibrinogen to insoluble fibrin that terminates in production of a clot. Factor Xa (FXa) is a serine protease involved in the blood coagulation cascade. Moreover, FXa plays a vital role in the enzymatic sequence which ends with the thrombus production. Thrombosis is a common causal pathology for three widespread cardiovascular syndromes: acute coronary syndrome (ACS), venous thromboembolism (VTE), and strokes. In this research a series of N-propargyltetrahydroquinoline and 1,2,3-triazole derivatives as a potential factor Xa (FXa) inhibitor were designed, synthesized, and evaluated for their FXa inhibitor activity, cytotoxicity activity and coagulation parameters. Rational design for the desired novel molecules was performed through protein-ligand complexes selection and ligand clustering. The microwave-assisted synthetic strategy of selected compounds was carried out by using Ullmann-Goldberg, N-propargylation, Mannich addition, Friedel-Crafts, and 1,3-dipolar cycloaddition type reactions under microwave irradiation. The microwave methodology proved to be an efficient way to obtain all novel compounds in high yields (73–93%). Furthermore, a thermochemical analysis, optimization and reactivity indexes such as electronic chemical potential (µ), chemical hardness (η), and electrophilicity (ω) were performed to understand the relationship between the structure and the energetic behavior of all the series. Then, in vitro analysis showed that compounds 27, 29–31, and 34 exhibited inhibitory activity against FXa and the corresponding half maximal inhibitory concentration (IC50) values were calculated. Next, a cell viability assay in HEK293 and HepG2 cell lines, and coagulation parameters (anti FXa, Prothrombin time (PT), activated Partial Thromboplastin Time (aPTT)) of the most active novel molecules were performed to determine the corresponding cytotoxicity and possible action on clotting pathways. The obtained results suggest that compounds 27 and 29 inhibited FXa targeting through coagulation factors in the intrinsic and extrinsic pathways. However, compound 34 may target coagulation FXa mainly by the extrinsic and common pathway. Interestingly, the most active compounds in relation to the inhibition activity against FXa and coagulation parameters did not show toxicity at the performed coagulation assay concentrations. Finally, docking studies confirmed the preferential binding mode of N-propargyltetrahydroquinoline and 1,2,3-triazole derivatives inside the active site of FXa.

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Section: Introductionmentioning

confidence: 99%

Innovative Three-Step Microwave-Promoted Synthesis of N-Propargyltetrahydroquinoline and 1,2,3-Triazole Derivatives as a Potential Factor Xa (FXa) Inhibitors: Drug Design, Synthesis, and Biological Evaluation

et al. 2020

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“…Many surveys have shown that rapid heating and enhancements of chemical yields are achieved with microwaves [12][13][14][15]. In solid chemistry and in heterogeneous solid-liquid systems, many experiments led to significant differences in reaction rates obtained between conventional and microwave heating.…”

Section: About Energy and Heatingmentioning

confidence: 99%

Continuous flow-microwave reactor: Where are we?

Estel

Poux

Benamara

et al. 2017

Chemical Engineering and Processing: Process Intensification

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This article presents the different microwave continuous reactors existing, which are reported in literature to carry out chemical synthesis with a more efficient way. It shows how the methods and tools of chemical engineering can be useful and necessary to define, characterize and optimize the microwave reactors. This review scans continuous microwave reactors, by describing the different types of microwave technologies used (multimode, single-mode, coaxial or guided transmission. . .). It then focuses on the various existing reactor geometries and on the control of the electromagnetic field homogeneity. The problem of temperature measurement and overall instrumentation is also addressed (input power, reflected power, continuous adaptation. . .). This review scans the most efficient microwave continuous flow reactors existing in the literature and highlights how the microwave technology is used as well as chemical engineering tools. It points out the reactors geometries, the control of the electromagnetic field and the measurement of the physical parameters (Temperature, microwave power, etc.). Finally, the scale-up of continuous-flow microwave reactors is examined through the existing lab-scale and semi industrial pilot plants described in literature.

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“…During the microwave heating, polar molecules such as water molecules try to orientate with the rapidly changing alternating electric field; thus, heat is generated by the rotation, friction, and collision of molecules (dipolar polarization mechanism). This makes it an ideal choice for heating polar solutions (Ameta et al 2015).…”

Section: Dipolar Polarizationmentioning

confidence: 99%

Microwave-Assisted Sol–Gel Synthesis Of Metal Oxide Nanomaterials

Garadkar

Kadam

Park

2016

Handbook of Sol-Gel Science and Technology

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The main goal of this chapter is to fill the gap in contemporary literature on the basic scientific aspects of microwave-assisted sol-gel technique. In this chapter, we shall briefly consider the microwave-assisted sol-gel method adopted for the preparation of metal oxide nanoparticles with controlled particle size, morphology, and crystal structure. Now a days researchers are motivated by an advantages

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ChemInform Abstract: Microwave Assisted Organic Synthesis: A Green Chemical Approach

Abstract: Review: [265 refs.]

Cited by 16 publications

References 0 publications

Innovative Three-Step Microwave-Promoted Synthesis of N-Propargyltetrahydroquinoline and 1,2,3-Triazole Derivatives as a Potential Factor Xa (FXa) Inhibitors: Drug Design, Synthesis, and Biological Evaluation

Innovative Three-Step Microwave-Promoted Synthesis of N-Propargyltetrahydroquinoline and 1,2,3-Triazole Derivatives as a Potential Factor Xa (FXa) Inhibitors: Drug Design, Synthesis, and Biological Evaluation

Continuous flow-microwave reactor: Where are we?

Microwave-Assisted Sol–Gel Synthesis Of Metal Oxide Nanomaterials

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