An efficient synthesis of structurally diverse 2-methyl-N-[(3-phenylamino)oxetan-3-yl]-2-propanesulfinamide derivatives under catalyst free conditions

Ugale, Sandip R.; Gholap, Somnath S.

doi:10.1007/s11696-017-0237-1

Cited by 4 publications

(1 citation statement)

References 29 publications

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“…In continuation to our ongoing research on the synthesis of biologically active oxadiazole derivatives, herein, we have reported the synthesis of novel structurally diverse 1,3,4‐oxadiazole possessing 2,2‐dimethyl‐2,3‐dihydrobenzofuran core ( 12a–j ) (Table ) and evaluated their biological potential. The structure of the synthesized compounds was confirmed by their characterization data obtained by IR, NMR, and mass spectral analysis study.…”

Section: Resultsmentioning

confidence: 99%

Design, synthesis, and pharmacological evaluation of fluorinated azoles as anti‐tubercular agents

Gholap¹,

Tambe²,

Nawale

et al. 2018

Archiv der Pharmazie

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Design, synthesis, and biological screening of 2,2-dimethyl-2,3-dihydrobenzofuran tethered 1,3,4-oxadiazole derivatives as anti-tubercular agents were described. The synthesis of the target compounds was conducted by a series of reaction schemes. All the synthesized compounds were characterized by IR, H NMR, C NMR, and mass spectrometry. The therapeutic potential of the synthesized compounds was confirmed by molecular docking studies. Among the synthesized compounds, 12a, 12c, 12d, 12e, 12g, and 12j were found to be more active against non-replicating than against replicating cultures of Mycobacterium tuberculosis H37Ra ex vivo and in vitro. These compounds exhibit minimum inhibitory concentration (MIC) values in the range of 2.31-23.91 μg/mL. The cytotoxicity study was conducted against the cell lines THP-1, A549 and PANC-1, and the compounds were observed to be non-toxic to host cells. Molecular docking was conducted with InhA (FabI/ENR) and suggested the antimycobacterial potential of the synthesized compounds. The investigation presented here was found to be adventitious for the development of new therapeutic agents against Mycobacterium infection.

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Section: Resultsmentioning

confidence: 99%

Design, synthesis, and pharmacological evaluation of fluorinated azoles as anti‐tubercular agents

Gholap¹,

Tambe²,

Nawale

et al. 2018

Archiv der Pharmazie

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Design, Synthesis and Biological Screening of Novel 1,3,4‐Oxadiazoles as Antitubercular Agents

Tambe¹,

Choudhari

Sarkar

et al. 2018

ChemistrySelect

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A series of novel 2,5‐disubstitued 1,3,4‐oxadiazole derivatives bearing 2,2‐dimethyl‐2,3‐dihydrobenzofuran scaffold has been synthesized and screened for antitubercular activity. All the synthesized compounds were characterized by IR, 1H NMR, 13C‐NMR and Mass spectral study. The in vitro antitubercular activity of the synthesized compounds was evaluated against Mycobacterium tuberculosis H37Ra(ATCC 25177) strain. Among the synthesized compounds, four compound displayed good antitubercular activity IC50 values in low micro‐gram range (<10 μg/mL). The antitubercular data suggested that growth inhibition MTB can be imparted by the introduction of a 4‐ trifluoromethyl phenyl acetylene substituent. Specificity of these compounds was checked by screening them for their anti‐bacterial activity against four bacterial strains (Gram‐negative strains: E. coli, S. aureus; Gram‐positive strains: P. aeruginosa and B. subtilis). None of the compound displayed antibacterial activity against any of the seleted strain. Molecular docking studies were carried out on InhA (FabI/ENR) which shows that the synthesized compounds bind at the catalytic site in a most favourable manner suggesting their potential as anti‐mycobacterial agents. The research presented here was found to be adventitious for the development of new therapeutic agents against Mycobacterium infection.

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Natural surfactants assisted an efficient synthesis of tetrahydro-β-carbolines

Gholap

Kadu²

2021

Results in Chemistry

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An efficient synthesis of structurally diverse 2-methyl-N-[(3-phenylamino)oxetan-3-yl]-2-propanesulfinamide derivatives under catalyst free conditions

Cited by 4 publications

References 29 publications

Design, synthesis, and pharmacological evaluation of fluorinated azoles as anti‐tubercular agents

Design, synthesis, and pharmacological evaluation of fluorinated azoles as anti‐tubercular agents

Design, Synthesis and Biological Screening of Novel 1,3,4‐Oxadiazoles as Antitubercular Agents

Natural surfactants assisted an efficient synthesis of tetrahydro-β-carbolines

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