2289-03-4Relevant academic research and scientific papers
Crystal Photodimerization Reactions of Spatially Engineered Isocoumarin Assemblies
Weerasinghe, Mihiri S.,Karlson, Steven T.,Lu, Yuhua,Wheeler, Kraig A.
, p. 1781 - 1785 (2016)
We report the single-crystal-to-single-crystal (SCSC) photodimerization of a sulfonamide isocoumarin. When recrystallized, this material forms centrosymmetrically related supramolecular dimers that assemble via the complementary features of molecular shap
Design, Synthesis, and Structural Analysis of Cladosporin-Based Inhibitors of Malaria Parasites
Babbar, Palak,Das, Pronay,Manickam, Yogavel,Mankad, Yash,Yadav, Swati,Parvez, Suhel,Sharma, Amit,Reddy, D. Srinivasa
, p. 1777 - 1794 (2021/05/10)
Here we have described a systematic structure activity relationship (SAR) of a set of compounds inspired from cladosporin, a tool compound that targets parasite (Plasmodium falciparum) lysyl tRNA synthetase (KRS). Four sets of analogues, synthesized based on point changes in the chemical scaffold of cladosporin and other logical modifications and hybridizations, were assessed using high throughput enzymatic and parasitic assays along with in vitro pharmacokinetics. Co-crystallization of the most potent compound in our series (CL-2) with PfKRS revealed its structural basis of enzymatic binding and potency. Further, we report that CL-2 has performed better than cladosporin in terms of metabolic stability. It thus represents a new lead for further optimization toward the development of antimalarial drugs. Collectively, along with a lead compound, the series offers insights on how even the slightest chemical modification might play an important role in enhancing or decreasing the potency of a chemical scaffold.
2-Hydroxy-1-oxo-1,2-dihydroisoquinoline-3-carboxylic Acid with Inbuilt β-NHydroxy-γ-keto-Acid pharmacophore as HCV NS5B polymerase inhibitors
Deore,Chen,Chen,Chang,Chuang,Chern,Wang,Chern
experimental part, p. 613 - 624 (2012/07/28)
The inbuilt 2-N-hydroxy-1-oxo-3-carboxylic acid of isoquinolone was designed as pyrophosphate mimic for hepatitis C NS5B polymerase. Various 2-hydroxy-1-oxo-1,2-dihydroisoquinoline-3-carboxylic acid derivatives 11a-p were synthesized and evaluated as HCV NS5B polymerase inhibitors. Compound 11c exhibited moderate inhibitory potency based on the inorganic pyrophosphate generation (IC50 = 9.5 μM) and based on NTP incorporation by NS5B enzyme (IC50 = 5.9 μM). Compound 11c demonstrated antiviral activity (EC50 = 15.7 μM) and good selectivity in HCV genotype 1b replicon Ava.5 cells. Compound 11c reduced the interaction of NTP to NS5B polymerase. Docking model showed that 11c situated in similar orientation to the bound uridine triphosphate in the active site of NS5B polymerase. As a result, 2-hydroxy-1-oxo-1,2-dihydroisoquinoline-3-carboxylic acid was disclosed as a novel inbuilt β-Nhydroxy-γ-keto-acid pharmacophore for HCV NS5B polymerase inhibitors.
COSMETIC OR DERMATOLOGICAL COMPOSITION COMPRISING A POLYMER BEARING JUNCTION GROUPS, AND COSMETIC TREATMENT PROCESS
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, (2010/10/03)
The present patent application relates to a cosmetic or dermatological composition comprising, in a cosmetically or dermatologically acceptable medium, a polymer comprising: (a) a polymer backbone that may be obtained by reaction: of a polyol comprising 3 to 6 hydroxyl groups;of a monocarboxylic acid containing 6 to 32 carbon atoms;of a polycarboxylic acid comprising at least two carboxylic groups COOH, and/or of a cyclic anhydride such as a polycarboxylic acid and/or of a lactone comprising at least one carboxylic group COOH; and(b) at least one junction group linked to the said polymer backbone and capable of establishing H bonds with one or more partner junction groups, each pairing of a junction group involving at least three H (hydrogen) bonds. The patent application also concerns a cosmetic treatment process using the said composition.
TRISUBSTITUTED AMINE COMPOUND
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Page/Page column 146-147, (2008/06/13)
The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
Vinyl Azides in Heterocyclic Synthesis. Part 6. Synthesis of Isoquinolines by Intramolecular Aza-Wittig Reaction
Hickey, Deirdre M. B.,MacKenzie, A. Roderick,Moody, Christopher J.,Rees, Charles W.
, p. 921 - 926 (2007/10/02)
Azidocinnamates containing ortho-carbonyl substituents are versatile intermediates for heterocyclic synthesis.Isoquinolines (8) and (9) are formed under mild neutral conditions by intramolecular aza-Wittig reactions of iminophosphoranes, readily derived f
Anti-allergic-3-carboxy-isocoumarin compositions and methods of use
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, (2008/06/13)
3-Carboxyisocoumarins, 2-thiaisocoumarins and related isocarbostyrils are useful anti-allergic agents. Several of these compounds are novel, and a process for their preparation is provided.
Method of treatment using 1-oxo-1H-2-benzopyran-3-carboxylic acid derivatives
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, (2008/06/13)
The method comprises administering to an animal an amount of substituted-1-oxo-1H-2-benzopyran-3-carboxylic acid effective to inhibit antigen-antibody reaction in said animal. Representative of the compounds that can be used in the method is sodium 1-oxo-
