Microwave-assisted green synthesis of new imidazo[2,1-b]thiazole derivatives and their antimicrobial, antimalarial, and antitubercular activities

Vekariya, Rajesh H.; Patel, Hitesh; Vekariya, Mayur K.; Prajapati, Neelam P.; Rajani, Dhanji P.; Rajani, Smita D.

doi:10.1007/s11164-017-2985-5

Cited by 22 publications

(12 citation statements)

References 62 publications

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“…Antimicrobial assay was performed at Microcare Laboratory and TRC, Surat, India according to revealed method as reported earlier . All compounds were also assessed for their antibacterial and antifungal efficacy and results obtained were shown in Table .…”

Section: Resultsmentioning

confidence: 99%

Pyrimidine‐Pyrazole Hybrids as Morpholinopyrimidine‐Based Pyrazole Carboxamides: Synthesis, Characterisation, Docking, ADMET Study and Biological Evaluation

Vekariya

Vekariya²,

Patel

et al. 2018

ChemistrySelect

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With the utilization of molecular hybridization, a series of novel morpholinopyrimidine based distinctive pyrazole carboxamides were designed and synthesized in an attempt to develop newer antimicrobial agents against the increasing bacterial resistance. Structure of final targeted compounds were confirmed by spectral analysis i. e. 1H‐NMR, 13C‐NMR and Mass spectra. The newly synthesized compounds were screened for their preliminary in‐vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi, antituberculosis activity against Mycobacterium tuberculosis H37Rv and antimalarial activity against Plasmodium falciparum. In addition to this, In‐silico molecular docking study and ADME properties were likewise studied for the targeted compounds. It was inferred that from the series, Fluorinated anilide derivatives of morpholinopyrimidine clubbed with pyrazole carboxylate emerged out as potential antimicrobial candidates from the in‐vitro antimicrobial assay.

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Section: Resultsmentioning

confidence: 99%

Pyrimidine‐Pyrazole Hybrids as Morpholinopyrimidine‐Based Pyrazole Carboxamides: Synthesis, Characterisation, Docking, ADMET Study and Biological Evaluation

Vekariya

Vekariya²,

Patel

et al. 2018

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“…Shi and co-workers developed a method for imidazo [ struction of imidazo[2,1-b]thiazole with phenylacetylene. [34] The reaction was carried out under very mild condition in the presence of potassium tert-butoxide (t-BuOK). Imidazo They reported a reaction using phenylacetylene (188) as a reactant because it is more active and, reacts with 6-phenyl-imidazo [2,1-b] [1,3,4]thiadiazole (187), to form 3,6-diphenylimidazo[2,1-b]thiazole (188).…”

Section: Miscellaneous Reactionsmentioning

confidence: 99%

“…Imidazothiazoles and its derivatives are synthesized by a plethora of reactions involving multicomponent reactions (MCRs), [24][25] biosynthesis of staphyloxanthin produced by staphylococcus aurease in the presence of dehydrosqualene synthase enzyme, [27] transition metal catalysed reactions, [28] visible light synthesis, [29] regioselective reaction, [30] Groebke-Blackburn-Bienayme-Reaction (GBBR) mechanism, [24,31] oxidative cyclisation, [32] Claisen-Schmidt condensation, [33] microwave assisted green synthesis [34] and ring-opening and ring-closing reconstruction reactions. [35] Multi-component reactions are reactions involving a combination of three or more substrates, which are carried out in a one-pot system to obtain the desired product.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Applications of Imidazothiazoles: An Overview

et al. 2020

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Imidazothiazoles and its derivatives have vital role in medicinal chemistry as they exhibit biological activities such as anti‐tumor, anti‐cancer, anti‐inflammatory, antibacterial, analgesic etc. This review summarises the various methodologies used to synthesise imidazothiazoles, its derivatives and applications covering literature upto 2020 and it emphasizes the synthesis of imidazothiazoles from 2‐aminothiazole, mercaptoimidazole and imidazothiadiazole.

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“…Recently, microwave irradiation has been considered as a green energy source for various organic reactions. [48,49] The main global health challenges in the field of medicinal chemistry are microbial resistance. Bacteria, fungi, viruses, and parasites are continues responsible to invalidate the effectiveness of various existing antimicrobial drugs.…”

Section: Introductionmentioning

confidence: 99%

“…Recently, microwave irradiation has been considered as a green energy source for various organic reactions. [ 48,49 ]…”

Section: Introductionmentioning

confidence: 99%

Microwave assisted synthesis, biological activities, and in silico investigation of some benzimidazole derivatives

Bhavsar

Acharya

Jethava

et al. 2020

Journal of Heterocyclic Chem

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Some derivatives of 2-substituted benzimidazole were prepared via coupling of N-methyl-o-phenylenediamine or o-phenylenediamine with different aromatic aldehydes catalyzed by Ni(OAc) 2 in the presence of chloroform under microwave-assisted conditions. Structural confirmation of all synthesized molecules was investigated by FT-IR, 13 C NMR, 1 H NMR, ESI-MS, and Elemental analysis. All prepared molecules were examined for in-vitro pharmaceutical activities like antibacterial, antifungal, antimalarial, antituberculosis, and antioxidant. Additionally, in silico study was also carried out. We also evaluated the steadiness and molecular interaction of docked complex, that is, complex of molecule (7s) with PDB: 5ZNI and complex of derivative (7l) with PDB: 3VLN, we have established a molecular dynamics model on the best dock molecules. All newly prepared molecules were authenticated to have excellent pharmacokinetics stuffs via calculated ADME-Tox descriptors, which signifying that these derivatives could be utilized as hit for the expansion of the some innovative active compounds.

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Microwave-assisted green synthesis of new imidazo[2,1-b]thiazole derivatives and their antimicrobial, antimalarial, and antitubercular activities

Cited by 22 publications

References 62 publications

Pyrimidine‐Pyrazole Hybrids as Morpholinopyrimidine‐Based Pyrazole Carboxamides: Synthesis, Characterisation, Docking, ADMET Study and Biological Evaluation

Pyrimidine‐Pyrazole Hybrids as Morpholinopyrimidine‐Based Pyrazole Carboxamides: Synthesis, Characterisation, Docking, ADMET Study and Biological Evaluation

Synthesis and Applications of Imidazothiazoles: An Overview

Microwave assisted synthesis, biological activities, and in silico investigation of some benzimidazole derivatives

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