- SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
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- BIOFILM FORMATION INHIBITOR
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PROBLEM TO BE SOLVED: To provide a substance that can effectively inhibit biofilm formation. SOLUTION: A biofilm formation inhibitor has a compound represented by the following formula (I) as an active ingredient (where R1, R2, Rsup
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Paragraph 0054
(2019/01/06)
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- Lewis Base Catalyzed Intramolecular Reduction of Salicylaldehydes by Pinacol-Derived Chlorohydrosilane
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A newly developed stable chlorohydrosilane derived from pinacol is herein described. This was successfully used in the reduction of salicylaldehydes in reasonable to excellent yields (51–97 %). The ability of the hydrosilane to react as a reducing agent is increased upon the in situ formation of a trialkoxyhydrosilane and activation with a Lewis base, as further indicated by density functional theory studies. 1,3-Dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone (DMPU) was identified to be a suitable catalyst for this metal-free reduction, promoting the regio- and chemoselective reduction of aldehydes in ortho-position to phenols, despite the presence of vicinal ketones. The performance of pinacol-derived chlorohydrosilane in the reduction of salicylaldehydes was further observed to be superior to that of well-established commercially available chlorohydrosilanes.
- Assoah, Benedicta,Vale, Jo?o R.,Kalenius, Elina,Veiros, Luis F.,Candeias, Nuno R.
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supporting information
p. 2910 - 2917
(2018/06/27)
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- Enantioselective synthesis of (R)-salmeterol employing an asymmetric Henry reaction as the key step
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A practical synthesis of (R)-salmeterol has been accomplished from 3-bromo salicylaldehyde, which involved a Cu(II)-sparteine complex catalyzed asymmetric Henry reaction as the key step. (R)-Salmeterol can be obtained in 39% overall yield and 95% ee.
- Guo, Zong-Liang,Deng, Yan-Qiu,Zhong, Shi,Lu, Gui
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scheme or table
p. 1395 - 1399
(2011/11/06)
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- Enzymatically activated cycloSal-d4T-monophosphates: The third generation of cycloSal-pronucleotides
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The third generation of cycloSal-pronucleotides, 5-diacetoxymethyl- cycloSal-d4T-monophosphates (5-di-AM-cycloSal-d4TMPs), is reported as a new class of "lock-in"-modified cycloSal-pronucleotides. These compounds bear an esterase-cleavable geminal dicarboxylate (acylal) attached to the aromatic ring of the saligenyl unit. The conversion into a strong acceptor group (aldehyde) leads to a strong decrease in hydrolytic stability. As a consequence, a fast release of a nucleoside monophosphate (i.e., d4TMP) follows. The concept of this enzymatic activation is proven by hydrolysis studies in phosphate buffer, cell extracts, and human serum. These investigations showed the conversion of the acylal group into a polar aldehyde by enzymatic cleavage. Besides, antiviral activities against HIV are presented.
- Gisch, Nicolas,Balzarini, Jan,Meier, Chris
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p. 1658 - 1667
(2008/01/27)
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- 5-Diacetoxymethyl-cycloSal-d4TMP - A prototype of enzymatically activated cyclosal-pronucleotides
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A new class of "lock-in"-modified cycloSal-pronucleotides has been synthesized. On the example of 5-diacetoxymethyl-cycloSal-d4T-monophosphate (5-di-AM-cycloSal-d4TMP), the concept of enzymatically activated cycloSal-pronucleotides is elucidated. Synthesis, hydrolysis studies, and antiviral activities against HIV are presented. Copyright Taylor & Francis Group, LLC.
- Gisch,Balzarini,Meier
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p. 861 - 864
(2008/09/17)
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- A short stereoselective synthesis of (R)-salmeterol
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A short, highly stereoselective oxy-Michael approach to the total synthesis of the β2-agonist, (R)-salmeterol is described. Georg Thieme Verlag Stuttgart.
- Buchanan, David J.,Dixon, Darren J.,Looker, Brian E.
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p. 1948 - 1950
(2007/10/03)
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