- Organocatalytic Synthesis of Fused Bicyclic 2,3-Dihydro-1,3,4-oxadiazoles through an Intramolecular Cascade Cyclization
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Hydrazone-carboxylic acids undergo intramolecular cyclization in the presence of pivaloyl chloride, iPr2NEt, and catalytic DABCO to form a range of substituted fused tricyclic 2,3-dihydro-1,3,4-oxadiazoles in high yields.
- Fugard, Alison J.,Thompson, Bethany K.,Slawin, Alexandra M. Z.,Taylor, James E.,Smith, Andrew D.
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supporting information
p. 5824 - 5827
(2015/12/11)
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- Design, synthesis, and biological evaluation of thiazolidine-2,4-dione conjugates as PPAR-γ agonists
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A library of synthesized conjugates of phenoxy acetic acid and thiazolidinedione 5a-m showed potent peroxisome proliferator activated receptor-γ (PPAR-γ) transactivation as well as significant blood glucose lowering effect comparable to the standard drugs pioglitazone and rosiglitazone. Most of the compounds showed higher docking scores than the standard drug rosiglitazone in the molecular docking study. Compounds 5l and 5m exhibited PPAR-γ transactivation of 54.21 and 55.41%, respectively, in comparison to the standard drugs pioglitazone and rosiglitazone, which showed 65.94 and 82.21% activation, respectively. Compounds 5l and 5m significantly lowered the blood glucose level of STZ-induced diabetic rats. Compounds 5l and 5m lowered the AST, ALT, and ALP levels more than the standard drug pioglitazone. PPAR-γ gene expression was significantly increased by compound 5m (2.00-fold) in comparison to the standard drugs pioglitazone (1.5-fold) and rosiglitazone (1.0-fold). Compounds 5l and 5m did not cause any damage to the liver and could be considered as promising candidates for the development of new antidiabetic agents.
- Nazreen, Syed,Alam, Mohammad Sarwar,Hamid, Hinna,Yar, Mohammad Shahar,Dhulap, Abhijeet,Alam, Perwez,Pasha, Mohammad Abdul Qadar,Bano, Sameena,Alam, Mohammad Mahboob,Haider, Saqlain,Kharbanda, Chetna,Ali, Yakub,Pillai, Kolakappi
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p. 421 - 432
(2015/06/08)
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- Synthesis, characterization and biological screening of some new aryloxyacetic acid analogs
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A novel series of 2-(4-bromo-2-formyl-phenoxy)acetyl amino acid and peptide analogs was synthesized by the coupling of 2-(4-bromo-2-formyl-phenoxy)acetic acid with different amino acid methyl ester hydrochlorides, dipeptide and tripeptide methyl esters using dicyclohexylcarbodiimide as the coupling agent and N-methylmorpholine as the base. Structures of all the newly synthesized compounds were elucidated on basis of IR, NMR and MS spectral data as well as elemental analysis. On pharmacological screening, some peptide derivatives were found to exhibit potent bioac-tivity against gram-negative bacterium Pseudomonas aeruginosa, pathogenic fungus Candida albicans and earthworms Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus sp. Dermatophytes were found to be moderately sensitive towards the newly synthesized analogs. Hydrolyzed peptide derivatives displayed better antimicrobial activity in comparison to corresponding esters.
- Dahiya, Rajiv,Pathak, Devender,Kaur, Ramninder
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experimental part
p. 754 - 758
(2009/12/24)
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- AZOLIDINONE-VINYL FUSED-BENZENE DERIVATIVES
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The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1 , R2 and n are as described in the description.
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- Synthesis and aldose reductase inhibitory activity of a new series of 5- [[2-(ω-carboxyalkoxy)aryl]methylene]-4-oxo-2-thioxothiazolidine derivatives
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A new series of 5-[[2-(ω-carboxyalkoxy)aryl]methylene]-4-oxo-2- thioxothiazolidine derivatives was synthesized and evaluated for their potency as aldose reductase inhibitors (ARIs). Their activities were examined in terms of their inhibitory effect on rat lens aldose reductase in vitro and in terms of the preventive effect on sorbitol accumulation in the sciatic nerve of streptozotocin (STZ)-induced diabetic rats in vivo. Of these compounds, some of the naphthylmethylene thiazolidine derivatives were comparable to Zenarestat in the inhibitory potency in vitro and in vivo. In particular, compound 30 was 1.5 times more potent than Zenarestat in the in vivo activity, and had an adequate potency for clinical development.
- Murata, Makoto,Fujitani, Buichi,Mizuta, Hiroyuki
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p. 1061 - 1070
(2007/10/03)
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- 1,4-dihydropyridine derivatives
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Compounds a formula (I) STR1 wherein the substituents and symbols have the meanings given in the specification, are new compounds with marked cardiovascular activity.
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