172695-25-9Relevant academic research and scientific papers
Development of Chiral Organosuperbase Catalysts Consisting of Two Different Organobase Functionalities
Kondoh, Azusa,Oishi, Masafumi,Terada, Masahiro,Tezuka, Hikaru
supporting information, p. 7472 - 7477 (2020/03/19)
In the field of chiral Br?nsted base catalysis, a new generation of chiral catalysts has been highly anticipated to overcome the intrinsic limitation of pronucleophiles that are applicable to the enantioselective reactions. Herein, we reveal conceptually new chiral Br?nsted base catalysts consisting of two different organobase functionalities, one of which functions as an organosuperbase and the other as the substrate recognition site. Their prominent activity, which stems from the distinctive cooperative function by the two organobases in a single catalyst molecule, was demonstrated in the unprecedented enantioselective direct Mannich-type reaction of α-phenylthioacetate as a less acidic pronucleophile. The present achievement would provide a new guiding principle for the design and development of chiral Br?nsted base catalysts and significantly broaden the utility of Br?nsted base catalysis in asymmetric organic synthesis.
A Modular Synthesis of Conformationally Preorganised Extended β-Strand Peptidomimetics
Yamashita, Tohru,Knipe, Peter C.,Busschaert, Nathalie,Thompson, Sam,Hamilton, Andrew D.
supporting information, p. 14699 - 14702 (2015/10/20)
A promising strategy for mediating protein-protein interactions is the use of non-peptidic mimics of secondary structural protein elements, such as the α-helix. Recent work has expanded the scope of this approach by providing proof-of-principle scaffolds that are conformationally biased to mimic the projection of side-chains from one face of another common secondary structural element - the β-strand. Herein, we present a synthetic route that has key advantages over previous work: monomers bearing an amino acid side-chain were pre-formed before rapid assembly to peptidomimetics through a modular, iterative strategy. The resultant oligomers of alternating pyridyl and six-membered cyclic ureas accurately reproduce a recognition domain of several amino acid residues of a β-strand, demonstrated herein by mimicry of the i, i+2, i+4 and i+6 residues.
METHODS FOR INHIBITING DRUG DEGRADATION
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Paragraph 0244; 0246, (2015/11/02)
Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters
A multifaceted secondary structure mimic based on piperidine-piperidinones
Xin, Dongyue,Perez, Lisa M.,Ioerger, Thomas R.,Burgess, Kevin
, p. 3594 - 3598 (2014/04/17)
Minimalist secondary structure mimics are typically made to resemble one interface in a protein-protein interaction (PPI), and thus perturb it. We recently proposed suitable chemotypes can be matched with interface regions directly, without regard for secondary structures. Here we describe a modular synthesis of a new chemotype 1, simulation of its solution-state conformational ensemble, and correlation of that with ideal secondary structures and real interface regions in PPIs. Scaffold 1 presents amino acid side-chains that are quite separated from each other, in orientations that closely resemble ideal sheet or helical structures, similar non-ideal structures at PPI interfaces, and regions of other PPI interfaces where the mimic conformation does not resemble any secondary structure. 68 different PPIs where conformations of 1 matched well were identified. A new method is also presented to determine the relevance of a minimalist mimic crystal structure to its solution conformations. Thus dld-1-faf crystallized in a conformation that is estimated to be 0.91 kcal-mol-1 above the minimum energy solution state. Do we know, when designing a new peptidomimetic scaffold like the one shown, how it can resemble secondary structures? Design and modular synthesis of this elongated mimic is reported, and the structure is related to ideal and real structures at PPI interfaces.
Diastereoselective synthesis of a core fragment of ritonavir and lopinavir
Roy, Arnab,Reddy, Lekkala Amarnath,Dwivedi, Namrata,Naram, Jyothirmayi,Swapna, Rodda,Malakondaiah, Golla China,Ravikumar, Mylavarpu,Bhalerao, Dinesh,Pratap, Taduri Bhanu,Reddy, Padi Pratap,Bhattacharya, Apurba,Bandichhor, Rakeshwar
, p. 6968 - 6970 (2012/02/13)
A novel approach to the synthesis of Boc-core, a key starting material for ritonavir and lopinavir involving an unprecedented diastereoselective nitroaldol reaction on β-amino aldehyde is disclosed.
4-ARYL-BUTANE-1,3-DIAMIDES
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Page/Page column 73-74, (2011/07/07)
The invention relates to compound of the formula (I): in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
4-ARYL-BUTANE-1,3-DIAMIDES
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Page/Page column 40, (2010/08/09)
The invention relates to compound of the formula (1) in which the substituents are as defined in the specification; m free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
Entropy-controlled catalytic asymmetric 1,4-type Friedel-crafts reaction of phenols using conformationally flexible guanidine/bisthiourea organocatalyst
Sohtome, Yoshihiro,Shin, Bongki,Horitsugi, Natsuko,Takagi, Rika,Noguchi, Keiichi,Nagasawa, Kazuo
supporting information; experimental part, p. 7299 - 7303 (2010/11/04)
Soft and weak cooperation: Conformationally flexible organic compounds were found to promote the title transformation. These "soft" organocatalysts, which are able to control processes through the differential activation entropies (ΔΔS*S-R) of
HIV PROTEASE INHIBITOR AND CYTOCHROME P450 INHIBITOR COMBINATIONS
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Page/Page column 42-43, (2009/10/18)
Compositions and methods of treating viral infections are provided. More particularly, compositions including a combination of protease inhibitors and cytochrome p450 enzyme inhibitors are provided. Methods of using the compositions for treatment of disea
COMPOSITIONS AND METHODS FOR INHIBITING CYTOCHROME P450
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Page/Page column 45-46, (2008/06/13)
Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters
