- Synthesis, pharmacological activities and molecular docking studies of pyrazolyltriazoles as anti-bacterial and anti-inflammatory agents
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A series of novel pyrazolyl alcohols (5a-h), pyrazolyl azides (6a-h), and pyrazolyltriazoles (8a-h, 10a-p and 12a-l) were prepared and evaluated for their bioactivity (anti-bacterial and anti-inflammatory) profile. The compound 5c displayed the potent anti-bacterial activity against Micrococcus luteus (MIC 3.9 and MBC 7.81 μg/mL). In vitro anti-inflammatory activity data denoted that compound 8b is effective among the tested compounds against IL-6 (IC50 6.23 μM). Docking analysis of compounds 5f, 8a-b, 8e-f and 8h displayed high binding energies for the compounds 8a-b and 8h towards TNF-α dimer (2AZ5 protein) and IL-6 (1ALU protein). In vivo anti-inflammatory activity of compounds 8b and 8h with respect to LPS induced mice model indicated that compound 8h showed significant reduction in TNF-α.
- Dayakar, Cherupally,Kumar, Buddana Sudheer,Sneha, Galande,Sagarika, Gudem,Meghana, Koneru,Ramakrishna, Sistla,Prakasham, Reddy Shetty,China Raju, Bhimapaka
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p. 5678 - 5691
(2017/10/09)
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- 4-Functionally-substituted 3-heterylpyrazoles: XV. 3-Aryl(heteryl)-1- phenyl-4-pyrazolylmethylamines and heterocumulenes obtained therefrom
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By reduction of 3-aryl(heteryl)-1-phenyl-4-azidomethyl-pyrazoles in the presence of Raney nickel or by hydrazinolysis of N-[3-aryl(heteryl)-1-phenyl-4- pyrazolylmethyl]phthalimides 4-pyrazolylmethylamines were obtained that in reaction with bis(trichloromethyl) carbonate afforded 3-aryl-(heteryl)-1-phenyl- 4-pyrazolylmethyl isocyanates, and with carbon disulfide furnished 3-aryl-(heteryl)-1-phenyl-4-pyrazolylmethyl isothiocyanates. 2005 Pleiades Publishing, Inc.
- Bratenko,Panimarchuk,Mel'nichenko,Vovk
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p. 238 - 242
(2007/10/03)
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