244132-27-2Relevant academic research and scientific papers
Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors
Flagstad, Thomas,Pedersen, Mette T.,Jakobsen, Tim H.,Felding, Jakob,Tolker-Nielsen, Tim,Givskov, Michael,Qvortrup, Katrine,Nielsen, Thomas E.
supporting information, (2021/12/24)
There is an emerging global need for new and more effective antibiotics against multi-resistant bacteria. This situation has led to massive industrial investigations on novel bacterial topoisomerase inhibitors (NBTIs) that target the vital bacterial enzym
Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions
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Page/Page column 1092; 1093, (2016/05/09)
The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Heterocyclic core analogs of a direct thrombin inhibitor
Blizzard, Timothy A.,Singh, Sanjay,Patil, Basanagoud,Chidurala, Naresh,Komanduri, Venukrishnan,Debnath, Samarpita,Belyakov, Sergei,Crespo, Alejandro,Struck, Alice,Kurtz, Marc,Wiltsie, Judyann,Shen, Xun,Sonatore, Lisa,Arocho, Marta,Lewis, Dale,Ogletree, Martin,Biftu, Tesfaye
, p. 1111 - 1115 (2014/03/21)
Thrombin is a serine protease that plays a key role in blood clotting. Pyrrolidine 1 is a potent thrombin inhibitor discovered at Merck several years ago. Seven analogs (2-8) of 1 in which the pyrrolidine core was replaced with various heterocycles were p
THROMBIN INHIBITORS
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Page/Page column 26, (2013/10/21)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2
A traceless, solid-supported synthesis ofβ-turn mimetics based on the hexahydropyrazino[1,2-α ]pyrazine-1,2-dione scaffold
Mieczkowski, Adam,Kozminski, Wiktor,Jurczak, Janusz
experimental part, p. 221 - 232 (2010/04/02)
The solid-supported synthesis of a library of-turn mimetics based on the three-component Petasis condensation and 2,5-diketopiperazine formation is reported. The eight-step sequence starts from optically pure (S)-piperazine-2-carboxylic acid dihydrochloride, which is first converted into an orthogonally protected, resin-bound amino derivative. The subsequent transformations lead to compounds having the common hexahydropyrazino[1,2-a] pyrazine-1,2-dione core and diverse side chains, which mimic the-turn structure. This synthetic route includes protection of the initial amino acid with two different protecting groups, followed by attachment to the Wang resin using the Mitsunobu reaction, deprotection of the-nitrogen atom, then Petasis reaction, amidation, deprotection of the-nitrogen atom, coupling with a Boc-protected-amino acid, cleavage of the Boc group, and the cyclizative cleavage from the resin, resulting in the requested bicyclic products obtained in good yields and having good to moderate purities. Six different boronic acids, four amines, and nine-amino acids were applied to this synthetic route, to explore the efficiency and limitations of the described method. Georg Thieme Verlag Stuttgart.
A traceless solid-supported synthesis of novel pyrazinediazepinedione derivatives
Mieczkowski, Adam,Jurczak, Janusz
experimental part, p. 2514 - 2519 (2010/05/18)
A simple, convenient, six-step synthesis of novel, tricyclic pyrazinebenzodiazepinedione derivatives has been described. The strategy is based on the use of the orthogonally-protected, optically pure, (S)-piperazine-2-carboxylic acid, in a Petasis reaction, followed by coupling with anthranilic acid and finally cyclizing cleavage. The investigated method was applied for the synthesis of novel bicyclic pyrazinediazepinedione derivatives. This traceless, solid-supported approach allows the preparation of a wide variety of compounds in moderate yields from commercially available or easily obtainable reagents.
COMPOUNDS AND METHODS FOR TREATMENT OF HCV
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Page/Page column 73-74, (2008/12/05)
Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.
