145790-51-8Relevant articles and documents
Tataricins A and B, two novel cyclotetrapeptides from Aster tataricus, and their absolute configuration assignment
Xu, Hui-Min,Yi, Hua,Zhou, Wen-Bing,He, Wen-Jun,Zeng, Gang-Zhi,Xu, Wen-Yan,Tan, Ning-Hua
, p. 1380 - 1383 (2013/04/23)
Two novel cyclotetrapeptides, tataricins A and B, with a unique cyclopeptide backbone and aδ 2,4Pro side chain, were isolated from the traditional Chinese medicine Aster tataricus. Their structures and absolute configurations were determined using a combination of spectroscopic data, the advanced Marfey's method, and a total synthesis. Copyright
Design, Synthesis, and invitro Antibacterial Activity of Fluoroquinolone Derivatives Containing a Chiral 3-(Alkoxyimino)-2-(aminomethyl)azetidine Moiety
Lv, Kai,Sun, Yexin,Sun, Lanyin,Wei, Zengquan,Guo, Huiyuan,Wu, Jinwei,Liu, Mingliang
experimental part, p. 1230 - 1236 (2012/08/08)
A series of novel (R)/(S)-7-(3-alkoxyimino-2-aminomethyl-1-azetidinyl)fluoroquinolone derivatives were synthesized and evaluated for their invitro antibacterial activity against representative strains. Our results reveal that 12 of the target compounds generally show better activity (MIC: -1) against the tested Gram-positive strains including MRSA and MRSE than levofloxacin (LVFX, MIC: 0.125-8μgmL-1). Their activity is similar to that of gemifloxacin (GMFX, MIC: -1). However, they are generally less active than the two reference drugs against Gram-negative strains. Moreover, against clinical strains of S.aureus including MRSA and S.epidermidis including MRSE, the MIC50 values (0.06-16μgmL-1) and MIC90 values (0.5-32μgmL-1) of compounds 16w, y, and z are 2-8- and 2-16-fold less than LVFX, respectively, and 16w (MIC90 range: 0.5-4μgmL-1) was also found to be more active than GMFX (MIC90 range: 1-8μgmL-1).
Novel orally active morpholine N-arylsulfonamides γ-secretase inhibitors with low CYP 3A4 liability
Josien, Hubert,Bara, Thomas,Rajagopalan, Murali,Clader, John W.,Greenlee, William J.,Favreau, Leonard,Hyde, Lynn A.,Nomeir, Amin A.,Parker, Eric M.,Song, Lixin,Zhang, Lili,Zhang, Qi
scheme or table, p. 6032 - 6037 (2010/05/18)
A new class of 2,6-disubstituted morpholine N-arylsulfonamide γ-secretase inhibitors was designed based on the introduction of a morpholine core in lieu or piperidine in our lead series. This resulted in compounds with improved CYP 3A4 profiles. Several a
Concise total synthesis of the thiazolyl peptide antibiotic GE2270 A
Delgado, Oscar,Martin Mueller,Bach, Thorsten
supporting information; experimental part, p. 2322 - 2339 (2009/04/10)
The potent antibiotic thiazolylpeptide GE2270 A was synthesized starting from N-tert-butyloxycarbonyl protected valine in a longest linear sequence of 20 steps and with an overall yield of 4.8 %. Key strategy was the assembly of the 2,3,6-trisubstituted p
SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS
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Page/Page column 66, (2010/02/15)
This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected f
Asymmetric synthesis of cis-2,4-disubstituted azetidin-3-ones from metal carbene chemistry
Burtoloso, Antonio Carlos B.,Correia, Carlos Roque D.
, p. 5636 - 5646 (2007/10/03)
Several chiral cis-2,4-disubstituted azetidin-3-ones were prepared as single diastereoisomers from N-protected amino acids, employing a highly stereoselective copper carbenoid N-H insertion reaction of diazoketones. These azetidin-3-ones were then convert
Chirality transfer in the aza-[2,3]-Wittig sigmatropic rearrangement
Anderson, James C.,Gair Ford,Whiting, Matthew
, p. 3734 - 3748 (2007/10/03)
The aza-[2,3]-Wittig sigmatropic rearrangements of substrates derived from enantiomerically pure alanine, valine and serine with phenyl and ester anion stabilising groups were investigated for their efficiency in chirality transfer. It was found that a me
Metal carbene N-H insertion of chiral α, α′-dialkyl α-diazoketones. A novel and concise method for the stereocontrolled synthesis of fully substituted azetidines
Burtoloso, Antonio Carlos B.,Correia, Carlos Roque D.
, p. 3355 - 3358 (2007/10/03)
The syntheses of all cis substituted azetidines were accomplished in few steps from L-serine in modest to high yields. The key step was based on a rhodium or copper carbenoid N-H insertion of α,α′- dialkyl-α-diazoketones to furnish cis-2,4-dial
Protection of Hydroxy Groups by Silylation: Use in Peptide Synthesis and as Lipophilicity Modifiers for Peptides
Davies, John S.,Higginbotham, Clement L.,Tremeer, E. John,Brown, Charles,Treadgold, Richard C.
, p. 3043 - 3048 (2007/10/02)
A survey of a series of organosilyl derivatives of serine and tyrosine has shown that they have a satisfactory stability profile for use in peptide synthesis.Only when alkaline conditions were used did side-reactions appear.A range of stability profiles have been determined from a study of organosilyl derivatised dipetides under different conditions, giving t1/2 values for hydrolysis ranging from 41 to 465 min in acid conditions, yet giving long-term stability at pH-values near to neutrality.
