Category: 167938-56-9

Markert, Christian; Thoma, Gebhard; Srinivas, Honnappa; Bollbuck, Birgit; Luond, Rainer M.; Miltz, Wolfgang; Walchli, Rudolf; Wolf, Romain; Hinrichs, Jurgen; Bergsdorf, Christian; Azzaoui, Kamal; Penno, Carlos A.; Klein, Kai; Wack, Nathalie; Jager, Petra; Hasler, Franziska; Beerli, Christian; Loetscher, Pius; Dawson, Janet; Wieczorek, Grazyna; Numao, Shin; Littlewood-Evans, Amanda; Rohn, Till A. published the artcile< Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A4 Hydrolase>, HPLC of Formula: 167938-56-9, the main research area is tetrazole derivative LYS 006 preparation LTA4H inhibitor antiinflammatory activity.

The cytosolic metalloenzyme leukotriene A4 hydrolase (LTA4H) is the final and rate-limiting enzyme in the biosynthesis of pro-inflammatory leukotriene B4 (LTB4). Preclin. studies have validated this enzyme as an attractive drug target in chronic inflammatory diseases. Despite several attempts, no LTA4H inhibitor has reached the market, yet. Herein, we disclose the discovery and preclin. profile of LYS006 (I), a highly potent and selective LTA4H inhibitor. A focused fragment screen identified hits that could be cocrystd. with LTA4H and inspired a fragment merging. Further optimization led to chiral amino acids and ultimately to LYS006, a picomolar LTA4H inhibitor with exquisite whole blood potency and long-lasting pharmacodynamic effects. Due to its high selectivity and its ability to fully suppress LTB4 generation at low exposures in vivo, LYS006 has the potential for a best-in-class LTA4H inhibitor and is currently investigated in phase II clin. trials in inflammatory acne, hidradenitis suppurativa, ulcerative colitis, and NASH.

Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 167938-56-9 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H17NO3, HPLC of Formula: 167938-56-9.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Fan, Yiqing; Zhang, Yongjie; Liu, Yan; Jiang, Hongyu; Zhou, Ying; Tang, Chunlei; Fan, Weizheng published the artcile< Pyrazolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: design, synthesis and biological evaluation>, Synthetic Route of 167938-56-9, the main research area is pyrazolopyrimidine macrocyclic preparation tropomyosin receptor kinase inhibition docking; Antitumor; Design and synthesis; High selectivity; The next-generation Trk inhibitor; Tropomyosin receptor kinase.

A series of pyrazolo[1,5-a]pyrimidine derivatives I [R = H, F, Cl; X1 = (CH2)2, CH2CMe2, (R)-CHMeCH2, (S)-CHMeCH2; X2 = (CH2)2, (CH2)3, (R)-CHMeCH2, (S)-CHMeCH2, (S)-CH2CHMe, (R)-CH2CHMe] was synthesized and evaluated the their biol. activity as the second-generation Trk inhibitors. The best compounds I [R = F; X1 = CH2CMe2; X2 = (R)-CHMeCH2] (IC50 = 1.40 and 1.80 nM, against TrkA, TrkAG595R, resp.) and I [R = F; X1 = (S)-CHMeCH2; X2 = (R)-CHMeCH2] (IC50 = 0.86, 6.92 nM, against TrkA, TrkAG595R, resp.) showed a kinase activity comparable to TPX-0005, and I [R = F; X1 = (S)-CHMeCH2; X2 = (R)-CHMeCH2] (IC50 = 350 nM against ALK) had a higher selectivity of Trk inhibition than TPX-0005, which was of great significance for reducing toxicity.

Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 167938-56-9 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H17NO3, Synthetic Route of 167938-56-9.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Cai, Aijie; Yan, Wenhao; Wang, Chao; Liu, Wei published the artcile< Copper-Catalyzed Difluoromethylation of Alkyl Iodides Enabled by Aryl Radical Activation of Carbon-Iodine Bonds>, Quality Control of 167938-56-9, the main research area is alkyl iodide copper catalyst difluoromethylation; alkyldifluoromethane preparation; copper; cross-coupling; difluoromethylation; radicals; reaction mechanisms.

A novel strategy that leveraged the halogen abstraction ability of aryl radicals, thereby engaging a diverse range of alkyl iodides in copper-catalyzed Negishi-type cross-coupling reactions at room temperature Specifically, aryl radicals generated via copper catalysis efficiently initiate the cleavage of the carbon-iodide bonds of alkyl iodides. The alkyl radicals thus generated enter the copper catalytic cycles to couple with a difluoromethyl zinc reagent, thus furnished the alkyl difluoromethane products. This unprecedented Negishi-type difluoromethylation approach was applied to the late-stage modification of densely functionalized pharmaceutical agents and natural products.

Angewandte Chemie, International Edition published new progress about Aralkyl halides, iodides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 167938-56-9 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H17NO3, Quality Control of 167938-56-9.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ota, Eisuke; Wang, Huaiju; Frye, Nils Lennart; Knowles, Robert R. published the artcile< A Redox Strategy for Light-Driven, Out-of-Equilibrium Isomerizations and Application to Catalytic C-C Bond Cleavage Reactions>, Synthetic Route of 167938-56-9, the main research area is light driven redox neutral isomerization cyclic aliphatic alc; linear carbonyl compound preparation out of equilibrium isomerization.

We report a general protocol for the light-driven isomerization of cyclic aliphatic alcs. to linear carbonyl compounds These reactions proceed via proton-coupled electron-transfer activation of alc. O-H bonds followed by subsequent C-C β-scission of the resulting alkoxy radical intermediates. In many cases, these redox-neutral isomerizations proceed in opposition to a significant energetic gradient, yielding products that are less thermodynamically stable than the starting materials. A mechanism is presented to rationalize this out-of-equilibrium behavior that may serve as a model for the design of other contrathermodynamic transformations driven by excited-state redox events.

Journal of the American Chemical Society published new progress about C-C bond cleavage (photo-). 167938-56-9 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H17NO3, Synthetic Route of 167938-56-9.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts