Department of Chemistry

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    Synthesis, Antibacterial Evaluation, and Computational Studies of a Diverse Set of Linezolid Conjugates
    (MDPI, 2022) Sakhuja, Rajeev
    The development of new antibiotics to treat multidrug-resistant (MDR) bacteria or possess broad-spectrum activity is one of the challenging tasks. Unfortunately, there are not many new antibiotics in clinical trials. So, the molecular hybridization approach could be an effective strategy to develop potential drug candidates using the known scaffolds. We synthesized a total of 31 diverse linezolid conjugates 3, 5, 7, 9, 11, 13, and 15 using our established benzotriazole chemistry with good yield and purity. Some of the synthesized conjugates exhibited promising antibacterial properties against different strains of bacteria. Among all the synthesized compounds, 5d is the most promising antibacterial agent with MIC 4.5 µM against S. aureus and 2.25 µM against B. subtilis. Using our experimental data pool, we developed a robust QSAR (R2 = 0.926, 0.935; R2cvOO = 0.898, 0.915; R2cvMO = 0.903, 0.916 for the S. aureus and B. subtilis models, respectively) and 3D-pharmacophore models. We have also determined the drug-like properties of the synthesized conjugates using computational tools. Our findings provide valuable insight into the possible linezolid-based antibiotic drug candidates.
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    Design and synthesis of spiro[indole-thiazolidine]spiro[indole-pyrans] as antimicrobial agents
    (Elsiever, 2011-09-15) Sakhuja, Rajeev
    A series of novel spiro[indole-thiazolidine]spiro[indole-pyran] derivatives were synthesized from N-(bromoalkyl)indol-2,3-diones via monospiro-bisindole intermediates; the two indole nuclei being connected via N–(CH2)n–N linker. Synthesized compounds were evaluated for their antimicrobial activities in vitro against three Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis, and Staphylococcus epidermis), four Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi, and Klebsiella pneumonia) as well as four fungi (Aspergillus niger, Aspergillus fumigatus, Aspergillus flavus, and Candida albicans) using Cup plate method. Bis spiro-indoles exhibited stronger antibacterial and antifungal efficiency than their corresponding mono spiro-indoles. Compound 10e, the most active derivative was shown to inhibit the growth of all bacterial strains and two fungal strains (A. niger and C. albicans)
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    2-(3'-Indolyl)-N-arylthiazole-4-carboxamides: Synthesis and evaluation of antibacterial and anticancer activities
    (Elsiever, 2015-10) Kumar, Dalip; Kumar, Anil
    A new series of 2-(3′-indolyl)-N-arylthiazole-4-carboxamides 17a–p has been designed and synthesized. Initial reaction of readily available thioamides 15 with bromopyruvic acid under refluxing conditions produced different thiazole carboxylic acids 16 which upon coupling with arylamines by using EDCI·HCl and HOBt afforded diverse arylthiazole-4-carboxamides 17a–p in 78–87% yields. Antibacterial activity evaluation against Gram-positive and Gram-negative bacterial strains led to compounds 17i–k and 17o as potent and selectively (Gram-negative) antibacterial agents. The cytotoxicity of thiazole carboxamides 17a–p was also evaluated on a panel of human cancer cell lines. Among the tested derivatives, compounds 17i (IC50 = 8.64 μM; HEK293T) and 17l (IC50 = 3.41 μM; HeLa) were identified as the most potent analogues of the series. Preliminary mechanism of action studies of thiazole carboxamide 17i suggested that its cytotoxicity against HeLa cells involves the induction of cell death by apoptosis.
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    Synthesis, characterization and microbiocidal studies of novel ionic liquid tagged Schiff bases
    (Elsiever, 2012-08) Khungar, Bharti; Kumar, Anil; Panwar, Jitendra
    The synthesis of novel imidazolium ionic liquid, tagged Schiff, has been described. The synthesis was achieved in three steps from 2,4-dihydroxybenzaldehyde by selective alkylation with 1,3-dibromopropane, followed by reaction with 1-methylimidazole and Schiff base formation with aromatic amines. The compounds were evaluated for antibacterial and antifungal activities. The ionic liquid tagged Schiff base 4a showed the inhibition of both Gram positive and Gram negative bacteria. It also showed broad spectrum antifungal activity against all four tested fungi; however, 4f showed highest antifungal activity against A. niger.
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    Silver triflate catalyzed synthesis of 3-aminoalkylated indoles and evaluation of their antibacterial activities
    (Springer, 2011-09-27) Kumar, Anil; Panwar, Jitendra
    An efficient, one-pot synthesis was developed for 3-aminoalkylated indoles by three-component coupling reaction of aldehydes, N-methylanilines, and indoles using AgOTf as a catalyst. A series of twenty 3-aminoalkylated indoles was evaluated for their antibacterial activities against both Gram negative and Gram positive bacteria. Compounds 4b and 4r showed good antibacterial activity against both Gram positive and Gram negative strains. However, inversing the property of substituent (from 4r to 4q) resulted in the significant fall in the magnitude of antibacterial activity against Escherichia coli.