126301-16-4Relevant articles and documents
Urea based foldamers
Yoo, Sung Hyun,Li, Bo,Dolain, Christel,Pasco, Morgane,Guichard, Gilles
, p. 59 - 92 (2021/06/25)
N,N′-linked oligoureas are a class of enantiopure, sequence-defined peptidomimetic oligomers without amino acids that form well-defined and predictable helical structures akin to the peptide α-helix. Oligourea-based foldamers combine a number of features—such as synthetic accessibility, sequence modularity, and folding fidelity—that bode well for their use in a range of applications from medicinal chemistry to catalysis. Moreover, it was recently recognized that this synthetic helical backbone can be combined with regular peptides to generate helically folded peptide-oligourea hybrids that display additional features in terms of helix mimicry and protein-surface recognition properties. Here we provide detailed protocols for the preparation of requested monomers and for the synthesis and purification of homo-oligoureas and peptide-oligourea hybrids.
Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington's Disease
Stott, Andrew J.,Maillard, Michel C.,Beaumont, Vahri,Allcock, David,Aziz, Omar,Borchers, Alexander H.,Blackaby, Wesley,Breccia, Perla,Creighton-Gutteridge, Gillian,Haughan, Alan F.,Jarvis, Rebecca E.,Luckhurst, Christopher A.,Matthews, Kim L.,McAllister, George,Pollack, Scott,Saville-Stones, Elizabeth,Van De Po?l, Amanda J.,Vater, Huw D.,Vann, Julie,Williams, Rachel,Yates, Dawn,Mu?oz-Sanjuán, Ignacio,Dominguez, Celia
supporting information, p. 380 - 388 (2021/03/03)
Using an iterative structure-activity relationship driven approach, we identified a CNS-penetrant 5-(trifluoromethyl)-1,2,4-oxadiazole (TFMO, 12) with a pharmacokinetic profile suitable for probing class IIa histone deacetylase (HDAC) inhibition in vivo.
HETEROCYCLIC COMPOUNDS
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, (2020/12/29)
Provided herein are compounds of formula (I) which comprise a thiomorpholine 1,1-dioxide or 1-imino-thiomorpholine 1-oxide moiety, or pharmaceutically acceptable salts of any of the foregoing, pharmaceutical compositions that include a compound described herein (including salts of the compound) and methods of synthesizing the same. Also provided are methods of treating Hepatitis B viral (HBV) infections using a compound of formula (I), or pharmaceutically acceptable salts thereof.
PYRAZINE COMPOUNDS AND USES THEREOF
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Page/Page column 335, (2020/03/05)
The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
SULFUR-CONTAINING POLYCYCLIC-HYDROXYPYRIDONE CARBOXAMIDE ANALOG AGAINST HIV
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Paragraph 0077; 0079-0080, (2020/12/05)
The disclosure discloses a sulfur-containing polycyclic-hydroxypyridone carboxamide analog against HIV and an application thereof. The sulfur-containing polycyclic-hydroxypyridone carboxamide analog has a compound represented by the following formula (I)
TRICYCLIC 2-QUINOLINONES AS ANTIBACTERIALS
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Paragraph 00310; 00311, (2018/11/26)
This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof that are useful as antibacterial agents. The compounds are useful as inhibitors of bacterial gyrase activity and of bacterial infections, and have the structure of Formula (I): as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 001031, (2018/09/12)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
16-METHYL-OXACYCLOHEXADECAN-2-ONE AND 16-METHYL-AZACYCLOHEXADECAN-2-ONE DERIVATIVES AS ANTIMICROBIAL AGENTS
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Paragraph 00267, (2018/10/19)
16-membered macrolide compounds inhibit growth of various microbial species and have utility in the treatment of systemic or topical microbial infections, including methicillin-resistant strains (Formula I).
PIPERIDINE DERIVATIVES AS INHIBITORS OF UBIQUITIN SPECIFIC PROTEASE 7
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, (2018/05/16)
The present invention concerns the identification of inhibitors of ubiquitin specific protease 7 (USP7), and methods of use thereof.
Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide
Futamura, Aya,Nozawa, Dai,Araki, Yuko,Tamura, Yunoshin,Tokura, Seiken,Kawamoto, Hiroshi,Tokumaru, Yuichi,Kakihara, Sora,Aoki, Takeshi,Ohtake, Norikazu
, p. 5203 - 5215 (2017/10/06)
The design, synthesis, and structure activity relationships of the novel class of pyrazolylethylbenzamide orexin receptor 1-selective antagonists are described. Further derivatization of the prototype dual orexin receptor 1/2 antagonist lead (1) by instal