149602-63-1Relevant academic research and scientific papers
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 337, (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)
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.
MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO
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Paragraph 0427; 0428, (2017/09/02)
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, compositions containing such molecules, and processes of using such molecules and compositions against such pests. These molecules and compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
Double Heck Route to a Dibenzoxepine and Convergent Suzuki Cross-Coupling Strategy for the Synthesis of an MR Antagonist
Hansen, Marvin M.,Kallman, Neil J.,Koenig, Thomas M.,Linder, Ryan J.,Richey, Rachel N.,Rizzo, John R.,Ward, Jeffrey A.,Yu, Hannah,Zhang, Tony Y.,Mitchell, David
, p. 208 - 217 (2017/02/26)
A practical pilot plant convergent synthesis of MR antagonist LY2623091 was established. For synthesis convergence, a vinyl bromide geometric isomer and chiral alaninol derivative were required building blocks. Key to the synthesis route development is a stereoselective synthesis of the E-vinyl bromide via a sequential double Heck reaction, Suzuki-Miyaura cross-coupling of the vinyl bromide, a selective nitro reduction, and a highly sensitive cyanamide hydrolysis to the urea. Improvements in yield and processing were accomplished by two sets of telescoping methods which decreased the manufacturing time and provided purity enhancements.
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
