326799-92-2Relevant academic research and scientific papers
The first total synthesis of potent antitumoral (±)-mafaicheenamine A, unnatural 6-fluoromafaicheenamine A and expedient synthesis of clausine e
Abbas, Yasir,Mansha, Muhammad,Ullah, Nisar
, p. 26104 - 26110 (2016)
The first total synthesis of potent antitumoral mafaicheenamine A (1) and its unnatural analogue, 6-fluoromafaicheenamine A (2) have been accomplished. An expedient synthesis of clausine E, a key intermediate in the course of synthesis of 1 and 2, was ach
Discovery of a novel series of guanidinebenzoates as gut-restricted enteropeptidase and trypsin dual inhibitors for the treatment of metabolic syndrome
Zhang, Xuqing,Zhu, Bin,Sun, Weimei,Wang, Mina,Albarazanji, Kamal,Ghosh, Brahma,Cummings, Maxwell,Lenhard, James,Leonard, James,Macielag, Mark,Lanter, James
supporting information, (2021/03/22)
A novel series of guanidinebenzoate enteropeptidase and trypsin dual inhibitors has been discovered and SAR studies were conducted. Optimization was focused on improving properties for gut restriction, including increased aqueous solubility, lower cellular permeability, and reduced oral bioavailability. Lead compounds were identified with efficacy in a mouse fecal protein excretion study.
5,8-DISUBSTITUTED-[1,2,4]TRIAZOLO[1,5-A]PYRIDINYL AND 5,8-DISUBSTITUTED-IMIDAZO[1,2-A]PYRIDINE DERIVATIVES USEFUL AS INHIBITORS OF ENTEROPEPTIDASE
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Page/Page column 120, (2021/01/29)
The present invention is directed to 5,8-disubstituted-[1,2,4]triazolo[1,5- a]pyridinyl and 5,8-disubstituted-imidazo[1,2-a]pyridine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the enteropeptidase enzyme.
An expeditious synthetic route to proteomimetic foldamers
Karekar, Vaibhav V.,Bhoge, Bapurao A.,Saraogi, Ishu
, p. 556 - 560 (2019/01/10)
α-Helix proteomimetics such as oligobenzamides have been shown to successfully inhibit a broad array of protein-protein interactions (PPIs) mediated by α-helices. Here we report the synthesis of a protected oligobenzamide intermediate, which can be selectively deprotected and alkylated with desired side chains to rapidly afford a library of α-helix proteomimetics.
Synthesis of highly functionalized oligobenzamide proteomimetic foldamers by late stage introduction of sensitive groups
Burslem, George M.,Kyle, Hannah F.,Prabhakaran, Panchami,Breeze, Alexander L.,Edwards, Thomas A.,Warriner, Stuart L.,Nelson, Adam,Wilson, Andrew J.
supporting information, p. 3782 - 3786 (2016/05/09)
α-Helix proteomimetics represent an emerging class of ligands that can be used to inhibit an array of helix mediated protein-protein interactions. Within this class of inhibitor, aromatic oligobenzamide foldamers have been widely and successfully used. This manuscript describes alternative syntheses of these compounds that can be used to access mimetics that are challenging to synthesize using previously described methodologies, permitting access to compounds functionalized with multiple sensitive side chains and accelerated library assembly through late stage derivatisation.
Efficient synthesis of fused bicyclic ethers and their application in herbicide chemistry
Schaetzer, Jürgen,Edmunds, Andrew J.F.,Gaus, Katharina,Rendine, Stefano,De Mesmaeker, Alain,Rueegg, Willy
, p. 4643 - 4649 (2015/01/08)
A series of triketones 2 and 3 featuring novel fused bicyclic aryl ethers have been prepared. The syntheses utilized ring-closing olefin metathesis (compounds 2), or oxidative cyclization of allylphenols as the key steps. The herbicidal activity of the ta
DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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, (2012/07/28)
Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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, (2012/08/08)
Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
IMIDAZOLINYLMETHYL ARALKYLSULFONAMIDES
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Page 19-20, (2010/02/06)
Compounds of the Formula: where R1-R6 are those defined herein and methods for producing the same. Also provided are pharmaceutical compositions comprising a Compound of Formula I and methods for their use as therapeutic agents.
A mild deprotection strategy for allyl-protecting groups and its implications in sequence specific dendrimer synthesis
Vutukuri, Dharma Rao,Bharathi, Pandi,Yu, Zhouying,Rajasekaran, Karthik,Tran, My-Huyen,Thayumanavan
, p. 1146 - 1149 (2007/10/03)
A mild deprotection strategy for allyl ethers under basic conditions in the presence of a palladium catalyst is described. Under these conditions, aryl allyl ethers can be cleaved selectively in the presence of alkyl allyl ethers. These conditions are also effective in the deprotection of allyloxycarbonyl groups. The utility of the current methodology in sequence specific dendrimer synthesis is demonstrated.
