201005-58-5Relevant academic research and scientific papers
Anticonvulsant Activity of Enantiomeric N-trans-Cinnamoyl Derivatives of 2-Aminopropan-1-ols and 2-Aminobutan-1-ols
Gunia-Krzyzak, Agnieszka,Zes?awska, Ewa,Nitek, Wojciech,Popió?, Justyna,Marona, Henryk
, p. 482 - 488 (2016/06/08)
Epilepsy, one of the most frequent neurological disorders, is still insufficiently treated in about 30% of patients. As a consequence, identification of novel anticonvulsant agents is an important issue in medicinal chemistry. In the present article we re
Synthesis and in vitro antimycobacterial activity of compounds derived from (R)- and (S)-2-amino-1-butanol - The crucial role of the configuration
Dobrikov, Georgi M.,Valcheva, Violeta,Stoilova-Disheva, Margarita,Momekov, Georgi,Tzvetkova, Pavleta,Chimov, Angel,Dimitrov, Vladimir
supporting information; experimental part, p. 45 - 56 (2012/03/26)
The synthesis of 47 structurally diverse compounds incorporating the (R)-2-amino-1-butanol motif has been realized. Ten of these compounds were found to exhibit in vitro specific activity against Mycobacterium tuberculosis H37Rv in a MIC range of 0.65 μM-14.03 μM. Five of the most active compounds 11, 22, 23, 31 and 42 (5.7-11.1 fold more active than ethambutol) can be outlined with very low cytotoxicity towards human embryonal kidney non-tumour cells (SI ranging from 91.2 to 375.4). For the purpose of comparison the (S)-enantiomers of these most active compounds have been synthesized and evaluated towards M. tuberculosis H37Rv showing no activity even at 20-32 fold higher concentrations.
Asymmetric hetero-Diels-Alder reactions of alkenyldihydrooxazoles. Synthesis of oxazolo[3,2-c]pyrimidines and related compounds
Elliott, Mark C.,Kruisvvijk, Elbertus
, p. 3157 - 3166 (2007/10/03)
Alkenyldihydrooxazoles undergo a highly diastereoselective formal aza-Diels-Alder reaction with aryl and arenesulfonyl isocyanates to give oxazolo[3,2-c]pyrimidines. Depending on the substitution pattern of the alkenyldihydrooxazole, these compounds may then undergo addition of a second equivalent of the isocyanate to give either tetrahydrooxazoIo[3,2-c]pyrimidine-8-carboxamides or octahydroazeto[2,3-7]oxazolo[3,2c]pyrimidines. The second addition is sensitive to steric and electronic factors, and can be prevented in some cases. The Royal Society of Chemistry 1999.
Highly diastereoselective hetero-Diels-Alder reactions of alkenyldihydrooxazoles as an approach to novel pyrimidine derivatives
Elliott, Mark C.,Kruiswijk, Elbertus
, p. 2311 - 2312 (2007/10/03)
Chiral 2-alkenyldihydrooxazoIes react with two equivalents of aryl and arylsulfonyl isocyanates to give chiral non-racemic dihydropyrimidone derivatives in high yield and with complete diastereocontrol.
