- Synthesis of novel triazole based benzoxazolinones: Their TNF-α based molecular docking with in-vivo anti-inflammatory, antinociceptive activities and ulcerogenic risk evaluation
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A library of novel bis-heterocycles containing benzoxazolinone based 1,2,3-triazoles has been synthesized using click chemistry approach. The compound 3f exhibited potent selective COX-2 inhibition of 59.48% in comparison to standard drug celecoxib (66.36% inhibition). The compound 3i showed significant (p 0.001, 50.95%), TNF-α inhibitory activity as compared to indomethacin (p 0.001, 64.01%). The results of the carrageenan induced hind paw oedema showed that compounds 3a, 3f, 3i, 3o, and 3e exhibited potent anti-inflammatory activity in comparison to Indomethacin. The molecular docking studies revealed that 3i exhibits strong inhibitory effect due to the extra stability of the complex because of an extra π-π bond. The histopathology report showed that none of the compounds caused gastric ulceration.
- Haider, Saqlain,Alam, M. Sarwar,Hamid, Hinna,Shafi, Syed,Nargotra, Amit,Mahajan, Priya,Nazreen, Syed,Kalle, Arunasree M.,Kharbanda, Chetna,Ali, Yakub,Alam, Aftab,Panda, Amulya K.
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- Trapping Reactions of Benzynes Initiated by Intramolecular Nucleophilic Addition of a Carbonyl Oxygen to the Electrophilic Aryne
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We describe here reactions in which a carbonyl oxygen atom initiates cascade reactions by nucleophilic attack on a covalently attached benzyne. The benzynes are produced by thermal cyclization of triynes via hexadehydro-Diels-Alder reaction. The initially produced oxocarbenium/aryl carbanionic zwitterion is protonated in situ by an external protic nucleophile (NuH) of appropriate acidity. The resulting ion pair (oxocarbenium+/Nu-) collapses through several different mechanistic manifolds, adding to the diversity of structural classes that can be generated.
- Chinta, Bhavani Shankar,Arora, Sahil,Hoye, Thomas R.
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supporting information
p. 425 - 429
(2022/01/12)
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- Benzimidazolidinone derivatives as muscarinic agents
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Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
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- Benzimidazolidinone derivatives as muscarinic agents
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Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
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Page/Page column 39
(2010/02/06)
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