67044-05-7Relevant academic research and scientific papers
Lipase-catalyzed aza-michael reaction on acrylate derivatives
Steunenberg, Peter,Sijm, Maarten,Zuilhof, Han,Sanders, Johan P. M.,Scott, Elinor L.,Franssen, Maurice C. R.
, p. 3802 - 3813 (2013/06/05)
A methodology has been developed for an efficient and selective lipase-catalyzed aza-Michael reaction of various amines (primary and secondary) with a series of acrylates and alkylacrylates. Reaction parameters were tuned, and under the optimal conditions it was found that Pseudomonas stutzeri lipase and Chromobacterium viscosum lipase showed the highest selectivity for the aza-Michael addition to substituted alkyl acrylates. For the first time also, some CLEAs were examined that showed a comparable or higher selectivity and yield than the free enzymes and other formulations.
Aurora kinase A inhibitors: Identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold
Coumar, Mohane Selvaraj,Wu, Jian-Sung,Leou, Jiun-Shyang,Tan, Uan-Kang,Chang, Chung-Yu,Chang, Teng-Yuan,Lin, Wen-Hsing,Hsu, John T.-A.,Chao, Yu-Sheng,Wu, Su-Ying,Hsieh, Hsing-Pang
, p. 1623 - 1627 (2008/12/21)
Tricyclic 6,7-dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione was identified as a novel scaffold for Aurora kinase A inhibition through virtual screening. SAR exploration coupled with molecular modeling of 8a reveals the minimum pharmacophore requirements for Aurora kinase A inhibition.
Substituted β-alanines
-
Page column 97, (2010/01/30)
The invention is directed to physiologically active compounds of general formula (I): wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group —L1—(CH2)n—C(=O)—N(R4)—CH2—CH2—Y; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (à4β1).
6,7-dihydropyrrol[3,4-c]pyrido[2,3-d]pyrimidine derivatives
-
, (2008/06/13)
The present invention concerns compounds of the formula: STR1 wherein R is a lower alkyl group, an aryl group or an alkylaryl group and X and Y are the same or different, and each is OH, NH2, or SH. The aryl group or the aryl moiety of the alkylaryl group may be unsubstituted, monosubstituted, disubstituted or trisubstituted. If substituted, each substituent may independently be an alkyl group, an alkyloxy group or a halogen. The present invention also provides methods for synthesizing the compounds described above.
