78357-63-8Relevant academic research and scientific papers
INHIBITORS TO TARGET HIV-1 NEF-CD80/CD86 INTERACTIONS FOR THERAPEUTIC INTERVENTION
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Paragraph 000169, (2020/03/05)
The compounds of Formula I, II, and III along with their stereoisomers, pharmaceutically acceptable salts, polymorphs, solvates and hydrates thereof are described in the present disclosure. The said compounds restore immune activation in case of infections or a disease associated with an HIV infection in a subject in need thereof.
Structure-based design, synthesis and evaluation of 2,4-diaminopyrimidine derivatives as novel caspase-1 inhibitors
Patel, Shivani,Modi, Palmi,Ranjan, Vishal,Chhabria, Mahesh
, p. 258 - 268 (2018/04/05)
Interleukin-1β converting enzyme contributes in various inflammatory and autoimmune diseases by maturing pro-inflammatory cytokines IL-1β, IL-18 and IL-33. Therefore, inhibition caspase-1 may provide a potential therapeutic strategy for the treatment of chronic inflammatory diseases. Here we have reported structure-based design, synthesis and biological evaluation of 2,4-diaminopyrimidine derivatives (6a-6w) as potential caspase-1 inhibitors. Six compounds 6m, 6n, 6o, 6p, 6q and 6r showed significant enzymatic inhibition with IC5 0 ranging from 0.022 to 0.078 μM. These compounds also displayed excellent cellular potency at sub-micromolar concentration. Moreover, molecular docking studies provided the useful binding insights specific for caspase-1 inhibition. All these results indicated that compounds 6m, 6n and 6o could be potential leads for the development of newer caspase-1 inhibitors as anti-inflammatory agents.
Privileged 1,2,4-oxadiazoles in anticancer drug design: Novel 5-aryloxymethyl-1,2,4-oxadiazole leads for prostate cancer therapy
Lukin, Alexey,Karapetian, Ruben,Ivanenkov, Yan,Krasavin, Mikhail
, p. 198 - 204 (2016/03/15)
Based on the structure of the previously identified leads, new series of compounds containing 1,2,4-oxadiazole core was designed. A small, diverse library of 51 compounds including both 2-(acylamino)ethyl and 2-ureidoethyl side chains was synthesized using parallel chemistry and tested for antiproliferative activity against prostate cancer DU-145 cell line. Four hit compounds - all belonging to 2-ureidoethyl series - were identified and three compounds were confirmed as 10-20 μM inhibitors. The similarity in compounds' periphery and the data obtained previously suggest a similar mode of action for these compounds which was postulated as tubulin inhibition and was confirmed by in silico docking. These data provide further evidence for the privileged character of 1,2,4-oxadiazoles in antiproliferative compound design.
Photoassisted Synthesis of Complex Molecular Architectures: Dearomatization of Benzenoid Arenes with Aza-o-xylylenes via an Unprecedented [2+4] Reaction Topology
Kuznetsov, Dmitry M.,Mukhina, Olga A.,Kutateladze, Andrei G.
supporting information, p. 6988 - 6991 (2016/06/13)
A new method was developed for the photoinduced dearomatization of arenes through an intramolecular cycloaddition with aza-o-xylylenes generated by excited-state intramolecular proton transfer (ESIPT) in the readily available photoprecursors. The [2+4] topology of this cycloaddition is unprecedented for photo-dearomatizations of benzenoid aromatic carbocycles. It provides rapid access to novel heterocycles, cyclohexadieno-oxazolidino-quinolinols, as valuable synthons for a broad range of post-photochemical transformations. I'm so excited: Photoinduced dearomatization of arenes was achieved through intramolecular cycloaddition with aza-o-xylylenes generated by excited-state intramolecular proton transfer in the readily available photoprecursors. The [2+4] topology of this cycloaddition is unprecedented for photo-dearomatizations of benzenoid aromatic carbocycles and produces the novel heterocycles cyclohexadieno-oxazolidino-quinolinols.
1-arylsulfonyl-2-(Pyridylmethylsulfinyl) benzimidazoles as new proton pump inhibitor prodrugs
Shin, Jai Moo,Sachs, George,Cho, Young-Moon,Garst, Michael
experimental part, p. 5247 - 5280 (2010/03/30)
New arylsulfonyl proton pump inhibitor (PPI) prodrug forms were synthesized. These prodrugs provided longer residence time of an effective PPI plasma concentration, resulting in better gastric acid inhibition.
PRODRUGS OF PROTON PUMP INHIBITORS
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Page 64-65; 88, (2010/02/06)
Prodrugs of proton pump inhibitors of Formulas 1 through 4, (I-IV), where the symbols are as defined in the specification, and the R group includes at least one acidic group or its pharmaceutically acceptable salt, have improved aqueous solubility and bioavailability.
Method for treating glaucoma IIB
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, (2008/06/13)
Provided is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing amount or ocular accommodation improving amount of a compound of the formula I or IA, wherein J is oxygen, sulfur, or N—Rd.
