Publications by authors named "Vikas Kumar Aamate"

5 Publications

  • Page 1 of 1

Indole-fused spirochromenes as potential anti-tubercular agents: design, synthesis and in vitro evaluation.

Mol Divers 2021 Nov 30;25(4):2137-2148. Epub 2020 May 30.

Department of Chemistry, Satavahana University, Karimnagar, Telangana State, 505001, India.

As part of an ongoing effort to develop new anti-tubercular agents, a series of novel indole-fused spirochromene hybrids (7a-l) were efficiently synthesized in excellent yields by the popular 'Fisher-Indole synthesis' approach. The structure elucidation of the target compounds was carried out by different spectral techniques including H-NMR, C-NMR, ESI Mass, and FTIR analysis. Additionally, the proposed structure of 7i was proved by single-crystal X-ray analysis. These compounds (7a-l) were screened for in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain. The results showed that most of the targets exhibited promising antimycobacterial activity with MICs of 1.56-6.25 μg/mL and weak cytotoxicity (19.93-32.16% at 50 μg/mL). Among them, compound 7l was found to be the most active compound (MIC of 1.56 μg/mL) with a good safety profile (32.16% at 50 μg/mL).
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http://dx.doi.org/10.1007/s11030-020-10108-zDOI Listing
November 2021

Conventional and microwave-assisted synthesis of new indole-tethered benzimidazole-based 1,2,3-triazoles and evaluation of their antimycobacterial, antioxidant and antimicrobial activities.

Mol Divers 2018 Nov 18;22(4):769-778. Epub 2018 Apr 18.

Department of Chemistry, Green and Medicinal Chemistry Laboratory, Osmania University, Hyderabad, Telangana, 500007, India.

A new series of triheterocycles containing indole-benzimidazole-based 1,2,3-triazole hybrids have been synthesized in good yields via a microwave-assisted click reaction. All the compounds were characterized by IR, [Formula: see text] NMR, [Formula: see text] NMR and mass spectroscopy and were evaluated for their in vitro antitubercular activity against the Mycobacterium tuberculosis H37Rv strain. Compounds 4b, 4h and 4i displayed highly potent antitubercular activity with MIC 3.125-6.25 [Formula: see text]. The antioxidant potential was evaluated using 2,2-diphenyl-1-picryl hydrazine and [Formula: see text] radical scavenging activity, and compounds 4e,4f and 4g showed excellent radical scavenging activity with [Formula: see text] values in the range of 08.50-10.05 [Formula: see text]. Furthermore, the compounds were evaluated for antimicrobial activity against numerous bacterial and fungal strains, and compounds 4b, 4c and 4h were found to be the most promising potential antimicrobial molecules with MIC 3.125-6.25 [Formula: see text].
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http://dx.doi.org/10.1007/s11030-018-9828-1DOI Listing
November 2018

Microwave-assisted synthesis, antioxidant and antimicrobial evaluation of 2-indolinone-based bis-1,2,3-triazole derivatives.

Mol Divers 2018 Feb 7;22(1):57-70. Epub 2017 Nov 7.

Green and Medicinal Chemistry Laboratory, Department of Chemistry, Osmania University, Hyderabad, 500007, India.

A series of 2-indolinone-based bis-1,2,3-triazole derivatives have been synthesized in excellent yields via microwave-assisted, copper-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC) reaction of O-, N-propargylated indolinone derivatives with in situ generated organic azides. The antioxidant activity of the synthesized compounds was evaluated by DPPH, NO and [Formula: see text] radical scavenging methods. Among the compounds screened for antioxidant activity, compounds 5e, 5f and 5o showed excellent radical scavenging activity more than the standard drugs ascorbic acid and BHT. The synthesized compounds were evaluated for their antimicrobial activity against gram-positive and gram-negative bacterial and fungal strains. Compounds 5g, 5h, 5n, 5q and 5r were found to be the most promising microbial growth inhibitory molecules.
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http://dx.doi.org/10.1007/s11030-017-9791-2DOI Listing
February 2018

Bis-spirochromanones as potent inhibitors of Mycobacterium tuberculosis: synthesis and biological evaluation.

Mol Divers 2017 Nov 24;21(4):999-1010. Epub 2017 Aug 24.

X-ray Crystallography Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, Telangana State, 500 007, India.

On the basis of reported antimycobacterial property of chroman-4-one pharmacophore, a series of chemically modified bis-spirochromanones were synthesized starting from 2-hydroxyacetophenone and 1,4-dioxaspiro[4.5] decan-8-one using a Kabbe condensation approach. The synthesized bis-spirochromanones were established based on their spectral data and X-ray crystal structure of 6e. All synthesized compounds were evaluated against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain, finding that some products exhibited good antimycobacterial activity with minimum inhibitory concentration as low as [Formula: see text]. Docking studies were carried out to identify the binding interactions of compounds II, 6a and 6n with FtsZ. Compounds exhibiting good in vitro potency in the MTB MIC assay were further evaluated for toxicity using the HEK cell line.
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http://dx.doi.org/10.1007/s11030-017-9779-yDOI Listing
November 2017

Synthesis, antimicrobial activity and molecular docking of novel tetracyclic scaffolds incorporating a flavonoid framework with medium sized oxygen heterocycles.

Bioorg Med Chem Lett 2015 Feb 30;25(4):898-903. Epub 2014 Dec 30.

Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.

A convenient approach for the synthesis of novel tetracyclic scaffolds incorporating a flavonoid framework with medium sized heterocyclic rings (eight-, nine-, ten- and eleven-membered rings) containing two oxygen atoms from flavonols through alkylation using different dibromoalkanes was described. The synthesized compounds were established based on the spectral data and X-ray crystal structure for 6c. The synthesized compounds were evaluated for their in vitro antimicrobial activity. Docking studies were carried out for most active two compounds 6f and 6i.
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http://dx.doi.org/10.1016/j.bmcl.2014.12.066DOI Listing
February 2015
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