cas 89336-46-9, (2-TERT-BUTOXYCARBONYLAMINO-THIAZOL-4-YL)-ACETIC ACID

Articles about 89336-46-9Total 10 be found

A Novel Minor Groove Binder as a Potential Therapeutic Agent for Myotonic Dystrophy Type 1
Myotonic dystrophy type 1 (DM1) is a multisystemic neuromuscular disorder that is inherited in an autosomal dominant manner. DM1 originates in a (CTG?CAG) repeat expansion in the 3’-UTR of the dystrophia myotonic protein kinase (DMPK) gene on chromosome 19. One of the transcripts, r(CUG)exp, is toxic in various ways. Herein we report a rationally designed small molecule with a thiazole peptidomimetic unit that can serve as a minor groove binder for the nucleic acid targets. This peptide unit linked to two triaminotriazine recognition units selectively binds to d(CTG)exp to inhibit the transcription process, and also targets r(CUG)exp selectively to improve representative DM1 pathological molecular features, including foci formation and pre-mRNA splicing defects in DM1 model cells. As such, it represents a new structure type that might serve as a lead compound for future structure-activity optimization.
Li, Ke,Krueger, Sarah B.,Zimmerman, Steven C.
p. 2638 - 2644
(2021/06/14)

Mirabegron impurity compound, and preparation method and application thereof
The invention discloses a mirabegron impurity compound, and a preparation method and application thereof. The mirabegron impurity compound disclosed by the invention is relatively high in purity and can be used as a reference substance for effectively identifying impurities generated in mirabegron synthesis, so that the drug quality of mirabegron is controlled.
-
Paragraph 0106-0111

(2020/09/23)

Target-Directed Azide-Alkyne Cycloaddition for Assembling HIV-1 TAR RNA Binding Ligands
The highly conserved HIV-1 transactivation response element (TAR) binds to the trans-activator protein Tat and facilitates viral replication in its latent state. The inhibition of Tat–TAR interactions by selectively targeting TAR RNA has been used as a strategy to develop potent antiviral agents. Therefore, HIV-1 TAR RNA represents a paradigmatic system for therapeutic intervention. Herein, we have employed biotin-tagged TAR RNA to assemble its own ligands from a pool of reactive azide and alkyne building blocks. To identify the binding sites and selectivity of the ligands, the in situ cycloaddition has been further performed using control nucleotide (TAR DNA and TAR RNA without bulge) templates. The hit triazole-linked thiazole peptidomimetic products have been isolated from the biotin-tagged target templates using streptavidin beads. The major triazole lead generated by the TAR RNA presumably binds in the bulge region, shows specificity for TAR RNA over TAR DNA, and inhibits Tat–TAR interactions.
Dash, Jyotirmayee,Dutta, Debasish,Paul, Raj,Paul, Rakesh
p. 12407 - 12411
(2020/06/01)

Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein
Small molecule inhibitors of the HIV-1 nucleocapsid protein (NC) are considered as promising agents in the treatment of HIV/AIDS. In an effort to exploit the privileged 2-amino-4-phenylthiazole moiety in NC inhibition, here we conceived, synthesized, and tested in vitro 18 NC inhibitors (NCIs) bearing a double functionalization. In these NCIs, one part of the molecule is deputed to interact noncovalently with the NC hydrophobic pocket, while the second portion is designed to interact with the N-terminal domain of NC. This binding hypothesis was verified by molecular dynamics simulations, while the linkage between these two pharmacophores was found to enhance antiretroviral activity both on the wild-type virus and on HIV-1 strains with resistance to currently licensed drugs. The two most interesting compounds 6 and 13 showed no cytotoxicity, thus becoming valuable leads for further investigations.
Mori, Mattia,Dasso Lang, Maria Chiara,Saladini, Francesco,Palombi, Nastasja,Kovalenko, Lesia,De Forni, Davide,Poddesu, Barbara,Friggeri, Laura,Giannini, Alessia,Malancona, Savina,Summa, Vincenzo,Zazzi, Maurizio,Mely, Yves,Botta, Maurizio
p. 463 - 468
(2019/04/25)

Synthesizing method of {2-[2-(2-amino-4-thiazolyl)-amino acetyl]-4-thiazolyl}-acetic acid
The invention discloses a synthesizing method of {2-[2-(2-amino-4-thiazolyl)-amino acetyl]-4-thiazolyl}-acetic acid, belongs to the technical field of medicine synthesis, and provides a new synthesizing method of {2-[2-(2-amino-4-thiazolyl)-amino acetyl]-4-thiazolyl}-acetic acid. The synthesizing method comprises the following synthesizing steps of (1) esterification reaction: reacting (2-Aminothiazole-4-yl)acetic acid and ethanol into ester, so as to obtain an intermediate product A; (2) amino protection: reacting (2-Aminothiazole-4-yl)acetic acid and t-butyloxycarboryl, so as to generate an intermediate product B; (3) amide condensation reaction: condensing the intermediate product A and the intermediate product B by a condensing agent, so as to generate an intermediate product C; (4) deprotection reaction: removing ester and t-butyloxycarboryl from the intermediate product C by trifluoroacetic acid, so as to obtain a target product. The synthesizing method has the advantages that the cost is low, the yield rate of the product is high, and the synthesizing method is suitable for large-scale industrial production.
-
Paragraph 0018; 0019; 0022; 0023; 0026; 0027

(2017/07/20)

COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES AS GLUTAMINASE INHIBITORS FOR TREATING CANCERS THEREOF
Provided are compounds of formula (I), wherein X, Y, Z, W, m, n, o, p, R1, R2 and R6 are defined as in the description. Pharmaceutical compositions and uses as glutaminase inhibitors for treating cancers thereof are also provided.
-
Page/Page column 187

(2014/06/11)

COMPOUNDS AND THEIR METHODS OF USE
Provided are compounds of formula (I), which can inhibit glutaminase. Pharmaceutical compositions comprising these compounds and uses as glutaminase inhibitors for treating cancers thereof are also provided.
-
Page/Page column 207; 208

(2014/06/11)

COSMETIC USES AND METHODS FOR INDOLINE GRANZYME B INHIBITOR COMPOSITIONS
Cosmetic uses and methods for indoline granzyme B inhibitor compounds in compositions with a cosmetically acceptable carrier. Uses and methods for treating, reducing or inhibiting the appearance of ageing in the skin are provided. Also provided are compositions and formulation for cosmetic uses and methods of maintaining a youthful appearance, reducing an appearance of ageing, inhibiting an appearance of ageing, reducing a rate of an appearance of ageing, reducing a skin inelasticity, reducing a rate of increasing skin inelasticity, maintaining a skin elasticity, and increasing the density of hair follicles of a skin of a subjecl. The uses and methods comprise applying/administering an indoline granzyme B inhibitor to a skin, or a portion of a skin of the subject.
-
(2014/10/15)

Heteroarylacetamide inhibitors of factor Xa
The invention is concerned with novel heteroarylacetamides of formula (I) [in-line-formulae]Rd—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb) ??(I) [/in-line-formulae] wherein Ra to Re /
-
Page/Page column 23

(2008/06/13)

Cyclic compounds linked by a heterocyclic ring useful as inhibitors of platelet glycoprotein IIB/IIIA
This invention relates to novel cyclic compounds linked by a heterocyclic ring system, which are useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, and to methods of using these compounds for the inhibition of platelet aggregation. A representative compound of the invention is cyclo-(D-Val-N(Me)Arg-Gly-Asp-?5-aminomethyl!-2-furoate).
-
(2008/06/13)