Yazar "Sriram, Dharmarajan" seçeneğine göre listele

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    Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors
    (Elsevier France-Editions Scientifiques Medicales Elsevier, 2020) Dogan, Hilal; Dogan, Sengul Dilem; Gunduz, Miyase Gozde; Krishna, Vagolu Siva; Lherbet, Christian; Sriram, Dharmarajan; Sahin, Onur
    Tuberculosis, caused by Mycobacterium tuberculosis, is a serious infectious disease and remains a global health problem. There is an increasing need for the discovery of novel therapeutic agents for its treatment due to the emerging multi-drug resistance. Herein, we present the rational design and the synthesis of eighteen new thiadiazolylhidrazones (TDHs) which were synthesized by intramolecular oxidative N-S bond formation reaction of 2-benzylidene-N-(phenylcarbamothioyl)hydrazine-lcarboximidamide derivatives by phenyliodine(III) bis(trifluoroacetate) (PIFA) under mild conditions. The compounds were characterized by various spectral techniques including FTIR, H-1 NMR, C-13 NMR and HRMS. Furthermore, the proposed structure of TDH12 was resolved by single-crystal X-ray analysis. The compounds were evaluated for their in vitro antitubercular activity against M. tuberculosis H37Rv. Among them, some compounds exhibited remarkable antimycobacterial activity, MIC = 0.78-6.25 mu g/mL, with low cytotoxicity. Additionally, the most active compounds were screened for their biological activities against M. tuberculosis in the nutrient starvation model. Enzyme inhibition assays and molecular docking studies revealed enoyl acyl carrier protein reductase (InhA) as the possible target enzyme of the compounds to show their antitubercular activities. (C) 2020 Elsevier Masson SAS. All rights reserved.
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    S-alkylated thiosemicarbazone derivatives: Synthesis, crystal structure determination, antimicrobial activity evaluation and molecular docking studies
    (Elsevier, 2021) Gunduz, Miyase Gozde; Kaya, Busra; Ozkul, Ceren; Sahin, Onur; Rekha, Estharla Madhu; Sriram, Dharmarajan; Ulkuseven, Bahri
    Increasing antimicrobial resistance is one of the most serious threats to human health worldwide. Therefore, there is an urgent need for the discovery of novel antimicrobial agents. Herein, we presented the synthesis of ten thiosemicarbazone derivatives (T1-T10) obtained by the reaction of S-alkylthiosemicarbazide with various dicarbonyl derivatives. The compounds were characterized by IR, H-1 NMR, ESI-MS and X-ray crystallography. Reaction with the dicarbonyl compound bearing the 4-fluorobenzoyl group unexpectedly gave a pyrazole derivative (T8) containing the entire S-methylthiosemicarbazone backbone. We extensively screened these derivatives for their antimicrobial activities against Mycobacterium tuberculosis and various bacterial and Candida strains. Additionally, the biofilm inhibition capacity of T8 was evaluated on Staphylococcus epidermidis and Pseudomonas aeruginosa biofilm positive strains. To find out the potential mechanism of anti-biofilm activity against PAO1, the docking studies of T8 were carried out into the binding site of LasR, which is the main regulator of bacterial cell-to-cell communication system known as quorum sensing. (C) 2021 Elsevier B.V. All rights reserved.