Synthesis and anti-leishmanial activity of TRIS-glycine-β-alanine dipeptidic triazole dendron coated with nonameric mannoside glycocluster

Pawar, Sushil V.; Upadhyay, Puspesh K.; Burade, Sachin S.; Kumbhar, Navanath; Patil, Rajendra; Dhavale, Dilip D.

doi:10.1016/j.carres.2019.107815

Cited by 11 publications

(1 citation statement)

References 65 publications

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“…Triazole derivatives have a very wide biological effect confirmed by research. They have antimicrobial activity [ 5 ], fungicidal activity [ 6 , 7 ], antiviral activity [ 8 ], anti-proliferative activity [ 9 , 10 ], cytotoxic and antitumor activity [ 11 ], antioxidant activity [ 12 ], anti-leishmanial activity [ 13 ], antitubercular activity [ 14 ], anti-inflammatory and analgesic activity [ 15 ], anticonvulsant activity [ 16 ], anti-obesitic activity [ 17 ], and antimalarial activity [ 18 ]. Studies on triazoles as inhibitors of Alzheimer’s disease have also given promising results [ 19 ].…”

Section: Introductionmentioning

confidence: 99%

New Application of 1,2,4-Triazole Derivatives as Antitubercular Agents. Structure, In Vitro Screening and Docking Studies

et al. 2020

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A series of 1,2,4-triazole derivatives were synthesized and assigned as potential anti-tuberculosis substances. The molecular and crystal structures for the model compounds C1, C12, and C13 were determined using X-ray analysis. The X-ray investigation confirmed the synthesis pathway and the assumed molecular structures for analyzed 1,2,4-triazol-5-thione derivatives. The conformational preferences resulting from rotational degrees of freedom of the 1,2,4-triazole ring substituents were characterized. The lipophilicity (logP) and electronic parameters as the energy of frontier orbitals, dipole moments, NBO net charge distribution on the atoms, and electrostatic potential distribution for all structures were calculated at AM1 and DFT/B3LYP/6-311++G(d,p) level. The in vitro test was done against M. tuberculosis H37Ra, M. phlei, M. smegmatis, and M. timereck. The obtained results clearly confirmed the antituberculosis potential of compound C4, which turned out to be the most active against Mycobacterium H37Ra (MIC = 0.976 μg/mL), Mycobaterium pheli (MIC = 7.81 μg/mL) and Mycobacerium timereck (62.6 μg/mL). Satisfactory results were obtained with compounds C8, C11, C14 versus Myc. H37Ra, Myc. pheli, Myc. timereck (MIC = 31.25−62.5 μg/mL). The molecular docking studies were carried out for all investigated compounds using the Mycobacterium tuberculosis cytochrome P450 CYP121 enzyme as molecular a target connected with antimycobacterial activity.

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Section: Introductionmentioning

confidence: 99%

New Application of 1,2,4-Triazole Derivatives as Antitubercular Agents. Structure, In Vitro Screening and Docking Studies

et al. 2020

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Synthesis, biological evaluation and molecular docking studies of quinoline‐conjugated 1,2,3‐triazole derivatives as antileishmanial agents

Tapkir

Patil

Galave

et al. 2021

Journal of Heterocyclic Chem

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In the present work, we have synthesized novel quinoline-conjugated 1,2,3-triazole derivatives 6a-l starting from substituted acetanilides in five steps. The synthesized compounds were screened for their antileishmanial activity. Quinoline-conjugated 1,2,3-triazole compounds 6c (IC 50 = 15.1 μg/ml), 6d (IC 50 = 14.6 μg/ml) and 6e (IC 50 = 14.3 μg/ml) displayed potent antileishmanial activity when compared with standard sodium stibogluconate (IC 50 = 14.3 ± 1.5 μg/ml). A molecular docking study against Leishmania major pteridine reductase (Lm-PTR1) suggests that these compounds have the potential to become lead molecules in antileishmanial drug discovery.

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Analysis of carbohydrates and glycoconjugates by matrix‐assisted laser desorption/ionization mass spectrometry: An update for 2019–2020

Harvey

2023

Mass Spectrometry Reviews

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This review is the tenth update of the original article published in 1999 on the application of matrix‐assisted laser desorption/ionization (MALDI) mass spectrometry to the analysis of carbohydrates and glycoconjugates and brings coverage of the literature to the end of 2020. Also included are papers that describe methods appropriate to analysis by MALDI, such as sample preparation techniques, even though the ionization method is not MALDI. The review is basically divided into three sections: (1) general aspects such as theory of the MALDI process, matrices, derivatization, MALDI imaging, fragmentation, quantification and the use of arrays. (2) Applications to various structural types such as oligo‐ and polysaccharides, glycoproteins, glycolipids, glycosides and biopharmaceuticals, and (3) other areas such as medicine, industrial processes and glycan synthesis where MALDI is extensively used. Much of the material relating to applications is presented in tabular form. The reported work shows increasing use of incorporation of new techniques such as ion mobility and the enormous impact that MALDI imaging is having. MALDI, although invented nearly 40 years ago is still an ideal technique for carbohydrate analysis and advancements in the technique and range of applications show little sign of diminishing.

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Synthesis and anti-leishmanial activity of TRIS-glycine-β-alanine dipeptidic triazole dendron coated with nonameric mannoside glycocluster

Cited by 11 publications

References 65 publications

New Application of 1,2,4-Triazole Derivatives as Antitubercular Agents. Structure, In Vitro Screening and Docking Studies

New Application of 1,2,4-Triazole Derivatives as Antitubercular Agents. Structure, In Vitro Screening and Docking Studies

Synthesis, biological evaluation and molecular docking studies of quinoline‐conjugated 1,2,3‐triazole derivatives as antileishmanial agents

Analysis of carbohydrates and glycoconjugates by matrix‐assisted laser desorption/ionization mass spectrometry: An update for 2019–2020

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