54030-33-0Relevant academic research and scientific papers
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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, (2019/11/12)
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.
Novel and selective detection of Tabun mimics
Jang, Yoon Jeong,Tsay, Olga G.,Murale, Dhiraj P.,Jeong, Jeong A.,Segev, Aviv,Churchill, David G.
, p. 7531 - 7534 (2014/07/07)
Detection of nerve agent-related molecules based on BODIPY-salicylaldehyde oxime conjugation was studied. Fluorescence intensity of the B-SAL-OXIME species increases in the presence of DECP, whereas it decreases in the presence of DCP and DEMP (limit of detection = 997 nM). Benzonitrile formation in the novel fluorescent B-SAL-OXIME system was elucidated using model substrates. the Partner Organisations 2014.
Enantioselective synthesis of (R)-salmeterol employing an asymmetric Henry reaction as the key step
Guo, Zong-Liang,Deng, Yan-Qiu,Zhong, Shi,Lu, Gui
, p. 1395 - 1399 (2011/11/06)
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.
Enzymatically activated cycloSal-d4T-monophosphates: The third generation of cycloSal-pronucleotides
Gisch, Nicolas,Balzarini, Jan,Meier, Chris
, p. 1658 - 1667 (2008/01/27)
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.
5-Diacetoxymethyl-cycloSal-d4TMP - A prototype of enzymatically activated cyclosal-pronucleotides
Gisch,Balzarini,Meier
, p. 861 - 864 (2008/09/17)
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.
Vitamin D analogues
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Page column 27, (2010/02/05)
The invention concerns novel bi-aromatic compounds having the formula: which are analogs of vitamin D, the process of preparing them, as well as their use in pharmaceutical compositions in human or veterinary medicine, particularly in dermatology, cancer treatment, treatment of auto-immune diseases, and in organ or tissue transplants. Cosmetic compositions and methods of use are also included.
