- Carbazole-based semicarbazones and hydrazones as multifunctional anti-Alzheimer agents
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With the aim to combat a multi-faceted neurodegenerative Alzheimer’s disease (AD), a series of carbazole-based semicarbazide and hydrazide derivatives were designed, synthesized and assessed for their cholinesterase (ChE) inhibitory, antioxidant and biometal chelating activity. Among them, (E)-2-((9-ethyl-9H-carbazol-3-yl)methylene)-N-(pyridin-2-yl)hydrazinecarbothioamide (62) and (E)-2-((9-ethyl-9H-carbazol-3-yl)methylene)-N-(5-chloropyridin-2-yl)hydrazinecarbothioamide (63) emerged as the premier candidates with good ChE inhibitory activities (IC50 values of 1.37 μM and 1.18 μM for hAChE, IC50 values of 2.69 μM and 3.31 μM for EqBuChE, respectively). All the test compounds displayed excellent antioxidant activity (reduction percentage of DPPH values for compounds (62) and (63) were 85.67% and 84.49%, respectively at 100 μM concentration). Compounds (62) and (63) conferred specific copper ion chelating property in metal chelation study. Molecular docking studies of compounds (62) and (63) indicate strong interactions within the active sites of both the ChE enzymes. Besides that, these compounds also exhibited significant in silico drug-like pharmacokinetic properties. Thus, taken together, they can serve as a starting point in the designing of multifunctional ligands in pursuit of potential anti-AD agents that might further prevent the progression of ADs. Communicated by Ramaswamy H. Sarma.
- Chaudhary, Bharat N.,Gandhi, Bhumi,Kanhed, Ashish M.,Patel, Dushyant V.,Patel, Kirti V.,Patel, Kishan B.,Patel, Nirav R.,Prajapati, Navnit K.,Shah, Bhavik S.,Teli, Divya M.,Yadav, Mange Ram
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- Synthesis, crystal structure, molecular docking studies and bio-evaluation of some N4-benzyl-substituted isatin-3-thiosemicarbazones as urease and glycation inhibitors
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Fifteen N4-benzyl-substituted isatin-3-thiosemicarbazones 5a-o were synthesized and evaluated for their urease and glycation inhibitory potential. Lemna aequinocitalis growth and Artemia salina assays were also done to determine their phytotoxi
- Pervez, Humayun,Khan, Nazia,Iqbal, Jamshed,Zaib, Sumera,Yaqub, Muhammad,Tahir, Muhammad Nawaz,Naseer, Muhammad Moazzam
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- Synthesis and in vitro bio-activity evaluation of N4-benzyl substituted 5-chloroisatin- 3-thiosemicarbazones as urease and glycation inhibitors
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A series of fifteen N4-benzyl substituted 5-chloroisatin-3-thiosemicarbazones 5a-o were synthesized and screened mainly for their antiurease and antiglycation effects. Lemna aequinocitalis growth and Artemia salina assays were carried out to de
- Pervez, Humayun,Khan, Nazia,Iqbal, Jamshed,Zaib, Sumera,Yaqub, Muhammad,Naseer, Muhammad Moazzam
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p. 108 - 118
(2018/03/29)
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- Synthesis, X-ray molecular structure, biological evaluation and molecular docking studies of some N4-benzyl substituted 5-nitroisatin-3-thiosemicarbazones
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A series of fifteen N4-benzyl substituted 5-nitroisatin-3-thiosemicarbazones 5a–o was synthesized and evaluated for urease inhibitory, phytotoxic and cytotoxic influences. All the compounds proved to be highly potent inhibitors of the enzyme, s
- Pervez, Humayun,Khan, Nazia,Zaib, Sumera,Yaqub, Muhammad,Naseer, Muhammad Moazzam,Tahir, Muhammad Nawaz,Iqbal, Jamshed
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p. 1022 - 1029
(2017/02/05)
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- Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors
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A series of thiadiazole derivatives has been designed as potential allosteric, substrate competitive inhibitors of the protein kinase JNK. We report on the synthesis, characterization and evaluation of a series of compounds that resulted in the identifica
- De, Surya K.,Chen, Vida,Stebbins, John L.,Chen, Li-Hsing,Cellitti, Jason F.,Machleidt, Thomas,Barile, Elisa,Riel-Mehan, Megan,Dahl, Russell,Yang, Li,Emdadi, Aras,Murphy, Ria,Pellecchia, Maurizio
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scheme or table
p. 590 - 596
(2010/05/02)
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