CsF-Catalyzed Transannulation Reaction of Oxazolones: Diastereoselective Synthesis of Diversified trans- N-(6-Oxo-1,4,5,6-tetrahydropyrimidin-5-yl)benzamides with Arylidene Azlactones and Amidines [0.03%]
CsF催化的噁唑酮并环化反应：芳醛与脒类化合物参与合成多样化反式-N-(6-氧代-1,4,5,6-四氢嘧啶-5-基)苯胺类衍生物的研究
Golnaz Parhizkar,Ahmad Reza Khosropour,Iraj Mohammadpoor-Baltork et al.
Golnaz Parhizkar et al.
A versatile and straightforward synthetic strategy for the construction of new tetrasubstituted 1,3-diazinones is described. The procedure is based on CsF-catalyzed, microwave-assisted, ring transformation reaction of arylidene azlactones w...
Yun Ding,Jing Chai,Paolo A Centrella et al.
Yun Ding et al.
Encoded library technology (ELT) is an effective approach to the discovery of novel small-molecule ligands for biological targets. A key factor for the success of the technology is the chemical diversity of the libraries. Here we report the...
Acid-Promoted One-Pot Synthesis of Substituted Furan and 6-Methylpyrazin-2(1 H)-one Derivatives via Allene Intermediate Formed in Situ [0.03%]
通过原位形成的全烯亚Intermediate合成取代的呋喃和6-甲基吡嗪-2(1h)-one衍生物的一锅酸促合成法
Jie Lei,Zhi-Gang Xu,Dian-Yong Tang et al.
Jie Lei et al.
Under the acidic conditions, substituted furans were constructed from γ-alkynyl ketones through corresponding allene intermediates in one-pot. The methodology was also tailored to a series of the Ugi reaction products for the synthesis of ...
A Parallel Approach to 7-(Hetero)arylpyrazolo[1,5- a]pyrimidin-5-ones [0.03%]
7-（杂）芳基吡唑并[1,5-a]嘧啶-5-酮的并行合成方法研究
Daniel C Schmitt,Nootaree Niljianskul,Neal W Sach et al.
Daniel C Schmitt et al.
A modular, two-pot assembly of 7-arylpyrazolo[1,5- a]pyrimidones from aryl/heteroaryl halides and aminopyrazoles in library format was developed. Sonogashira coupling of aryl bromides with triethyl orthopropiolate, followed by in situ ortho...
Automated High-Throughput Synthesis of Protein-Loaded Polyanhydride Nanoparticle Libraries [0.03%]
自动化高通量合成负载蛋白质的聚酐纳米颗粒库
Jonathan T Goodman,Adam S Mullis,Lucas Dunshee et al.
Jonathan T Goodman et al.
The development of high-throughput techniques and combinatorial libraries can facilitate rapid synthesis and screening of biomaterial-based nanocarriers for drug and vaccine delivery. This study describes a high-throughput method using an a...
Solid-Phase Synthesis of β-Hydroxy Ketones Via DNA-Compatible Organocatalytic Aldol Reactions [0.03%]
基于DNA相容的有机催化aldol反应固相合成β-羟基酮
Keitou Shu,Thomas Kodadek
Keitou Shu
One-bead one-compound (OBOC) libraries constructed by solid-phase split-and-pool synthesis are a valuable source of protein ligands. Most OBOC libraries are composed of oligoamides, particularly peptides, peptoids, and peptoid-inspired mole...
Construction of Druglike 2-Amido Benzo[ d]imidazole Analogues via Desulfurative Cyclization of Thiourea Intermediate Resin on Solid-Phase [0.03%]
基于固相树脂中硫脲中间体去硫环化反应构建苯并咪唑类药物库研究
Hyun-Jeong Ryu,Seung-Ju Yang,Gee-Hyung Lee et al.
Hyun-Jeong Ryu et al.
A 2-amido benzo[ d]imidazole library has been constructed by solid-phase synthesis. The key step of this solid-phase synthesis involves the preparation of polymer-bound 2-amino benzo[ d]imidazole resin through desulfurative cyclization of t...
Development and Application of a Sensitive Peptide Reporter to Discover 20S Proteasome Stimulators [0.03%]
一种敏感肽探针的开发及应用以发现20S蛋白酶体激活剂
Rachel A Coleman,Darci J Trader
Rachel A Coleman
To attenuate an overabundance of cellular protein, it has been hypothesized that the 20S core particle (20S CP) of the proteasome can be chemically stimulated to degrade proteins into nontoxic peptides more quickly. Screening for small mole...
Woo-Ri Shin,Simranjeet Singh Sekhon,Sung-Keun Rhee et al.
Woo-Ri Shin et al.
Aptamer-based paper strip sensor for detecting Vibrio fischeri was developed. Our method was based on the aptamer sandwich assay between whole live cells, V. fischeri and DNA aptamer probes. Following 9 rounds of Cell-SELEX and one of the n...
A General Small-Angle X-ray Scattering-Based Screening Protocol Validated for Protein-RNA Interactions [0.03%]
基于小角度X射线散射的蛋白质-核酸相互作用通用筛选方法及验证结果
Po-Chia Chen,Pawel Masiewicz,Vladimir Rybin et al.
Po-Chia Chen et al.
We present a screening protocol utilizing small-angle X-ray scattering (SAXS) to obtain structural information on biomolecular interactions independent of prior knowledge, so as to complement affinity-based screening and provide leads for f...