161105-54-0Relevant articles and documents
Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain
Brand, Michael,Clayton, James,Moroglu, Mustafa,Schiedel, Matthias,Picaud, Sarah,Bluck, Joseph P.,Skwarska, Anna,Bolland, Hannah,Chan, Anthony K. N.,Laurin, Corentine M. C.,Scorah, Amy R.,See, Larissa,Rooney, Timothy P. C.,Andrews, Katrina H.,Fedorov, Oleg,Perell, Gabriella,Kalra, Prakriti,Vinh, Kayla B.,Cortopassi, Wilian A.,Heitel, Pascal,Christensen, Kirsten E.,Cooper, Richard I.,Paton, Robert S.,Pomerantz, William C. K.,Biggin, Philip C.,Hammond, Ester M.,Filippakopoulos, Panagis,Conway, Stuart J.
, p. 10102 - 10123 (2021/07/31)
CREBBP (CBP/KAT3A) and its paralogue EP300 (KAT3B) are lysine acetyltransferases (KATs) that are essential for human development. They each comprise 10 domains through which they interact with >400 proteins, making them important transcriptional co-activa
Parallel synthesis of homochiral β-amino acids
Davies, Stephen G.,Mulvaney, Andrew W.,Russell, Angela J.,Smith, Andrew D.
, p. 1554 - 1566 (2008/02/09)
The parallel asymmetric synthesis of an array of 30 β-amino acids of high enantiomeric purity using the conjugate addition of homochiral lithium N-benzyl-N-(α-methylbenzyl)amide as the key step is accomplished. The experimental simplicity and highly practical nature of the protocol is demonstrated by the efficient parallel conversion of 15 α,β-unsaturated esters to both enantiomeric series of the corresponding β-amino acids in high overall yields and selectivities with minimal purification involved in each step of the reaction protocol.
NOVEL BETA-LACTAM COMPOUNDS AND PROECSS FOR PRODUCING THE SAME
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, (2008/06/13)
1. A β-lactam compound of the formula [1]; ???wherein R1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y1 is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y2 is hydrogen, an alkyl, cyano, -C(R3)=NR4 (wherein R3 and R4 are hydrogen, an amino, an alkyl, etc., or R3 and R4 may combine each other together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has an excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.
