27893-05-6Relevant academic research and scientific papers
Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication
Stachulski, Andrew V.,Pidathala, Chandrakala,Row, Eleanor C.,Sharma, Raman,Berry, Neil G.,Iqbal, Mazhar,Bentley, Joanne,Allman, Sarah A.,Edwards, Geoffrey,Helm, Alison,Hellier, Jennifer,Korba, Brent E.,Semple, J. Edward,Rossignol, Jean-Francois
experimental part, p. 4119 - 4132 (2011/08/05)
We report the syntheses and activities of a wide range of thiazolides [viz., 2-hydroxyaroyl-N-(thiazol-2-yl)amides] against hepatitis B virus replication, with QSAR analysis of our results. The prototypical thiazolide, nitazoxanide [2-hydroxybenzoyl-N-(5-
N-ACYL ANTHRANILIC ACID DERIVATIVE OR SALT THEREOF
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Page/Page column 75, (2011/11/13)
An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.)
N-ACYL ANTHRANILIC ACID DERIVATIVE OR SALT THEREOF
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Page/Page column 94-95, (2011/11/13)
An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or th
Synthesis of novel thiopyrimidines: An investigation of anti-tubercular and antimicrobial activity
Haveliwala, Dhaval D.,Kamdar, Nimesh R.,Mistry, Prashant T.,Patel, Saurabh K.
experimental part, p. 451 - 462 (2012/06/30)
A variety of novel sulfur-containing tricyclic pyrimidine derivatives have been synthesized via the reaction of 2-amino-4-oxo-4H-chromene-3-carbonitriles 3(a-f) with different reagents and characterized by IR, 1H NMR, 13C NMR, mass spectrometry and elemen
Amide-containing diketoacids as HIV-1 integrase inhibitors: Synthesis, structure-activity relationship analysis, and biological activity
Li, Hongcai,Wang, Chao,Sanchez, Tino,Tan, Yanmei,Jiang, Chunying,Neamati, Nouri,Zhao, Guisen
experimental part, p. 2913 - 2919 (2009/09/06)
HIV-1 integrase, which catalyzes the integration of the viral genome into the cellular chromosome, is an essential enzyme for retroviral replication, and represents an attractive and validated target in the development of therapeutics against AIDS. In this paper, 17 amide-containing novel diketoacids were designed and synthesized, and their ability to inhibit HIV-1 integrase was tested. The structure-activity relationships were also analyzed.
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors
Spencer, Jeffrey R,McGee, Danny,Allen, Darin,Katz, Bradley A,Luong, Christine,Sendzik, Martin,Squires, Neil,Mackman, Richard L
, p. 2023 - 2026 (2007/10/03)
The structure-based design of potent and selective urokinase-type plasminogen activator (uPA) inhibitors with 4-aminoarylamidine or 4-aminoarylguanidine S1 binding groups, is described.
A highly practical route to 2-methylchromones from 2-acetoxybenzoic acids
Jung,Min,Park
, p. 1837 - 1845 (2007/10/03)
2-Methylchromones were accessed via a keto ester condensation on 2-acetoxybenzoyl chloride, followed by cyclization and decarboxylation. No column chromatography was required in the process.
Novel quinolizidine salicylamide influenza fusion inhibitors
Yu, Kuo-Long,Ruediger, Edward,Luo, Guangxiang,Cianci, Christopher,Danetz, Stephanie,Tiley, Laurence,Trehan, Ashok K.,Monkovic, Ivo,Pearce, Bradley,Martel, Alain,Krystal, Mark,Meanwell, Nicholas A.
, p. 2177 - 2180 (2007/10/03)
A novel series of quinolizidine salicylamides was synthesized as specific inhibitors of the H1 subtype of influenza A viruses. These inhibitors inhibit the pH-induced fusion process, thereby blocking viral entry into host cells. Compound 16 was the most active inhibitor in this series with an EC50 of 0.25 μg/mL in plaque reduction assay. The synthesis and the SAR of these compounds are discussed.
H-bonded oxyhemoglobin models with substituted picket-fence porphyrins: The model compound equivalent of site-directed mutagenesis
Wuenschell, Gerald E.,Tetreau, Catherine,Lavalette, Daniel,Reed, Christopher A.
, p. 3346 - 3355 (2007/10/02)
Iron(II) complexes of picket-fence-type porphyrins having one of the four pivalamide pickets replaced by a substituent capable of H-bonding have been synthesized as models for oxyhemoglobin. This synthetic approach is analogous to site-directed mutagenesis of the distal residues in oxygen-binding hemoproteins. Rate and equilibrium data for dioxygen binding have been determined to evaluate the effect of the H-bonding substituent and to make comparisons with more passive substituents. The effect of H-bonding on the dioxygen affinity under standard conditions (25 °C, toluene solvent, 1,2-dimethylimidazole as axial ligand) is best illustrated by the ca. 10-fold increase observed when one pivalamide substituent of picket-fence porphyrin is replaced by a phenylurea substituent. Other substituents influence dioxygen adduct stability in a variety of ways to reveal that even with an apparently straightforward systematic approach, there can be considerable difficulty in partitioning the various factors that influence O2 affinity. This applies to both model compounds and mutant proteins.
SYNTHESIS OF 4-CHLOROSUBSTITUTED SPIROPYRANES OF THE INDOLE SERIES
Przhiyalgovskaya, N. M.,Kon'kov, L. I.,Kurkovskaya, L. N.,Mandzhikov, V. F.
, p. 1078 - 1081 (2007/10/02)
Enaminohydroxyketones, formed from 1,3,3-trimethyl-2-methyleneindoline and ortho-acetoxyaromatic acid chlorides, are converted by heating with phosphorus oxychloride in dichloroethane and subsequent treatment with alkali to 4-chlorosubstituted spiropyrane
