PubMed · 16038129
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2005. [Early sequential therapy].. https://pubmed.ncbi.nlm.nih.gov/16038129/
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Lubeluzole [(S)-9] has been synthesized by a convergent synthesis, alkylation of N-methyl-N-piperidin-4-yl-1,3-benzothiazol-2-amine (4) with (+)-(R)-1-chloro-3-(3,4-difluorophenoxy)propan-2-ol [(+)-(R)-8] being the key step. Alcohol (+)-(R)-8 was obtained from commercially available (R)-epichlorohydrin [(R)-6], while the thiazole derivative 4 was easily obtained starting from N-protected piperidin-4-one (1) in a three-step procedure. The same method was used in order to obtain both the (R)-stereoisomer of lubeluzole [(R)-9] and its racemate [(RS)-9]. Overall yields ranged from 20% to 35%. The enantiomeric excess values for (S)-9 and (R)-9 were 97% and 94% respectively, as analyzed by chiral HPLC.
Diastolic heart failure occurs when signs and symptoms of heart failure are present but left ventricular systolic function is preserved (i.e., ejection fraction greater than 45 percent). The incidence of diastolic heart failure increases with age; therefore, 50 percent of older patients with heart failure may have isolated diastolic dysfunction. With early diagnosis and proper management the prognosis of diastolic dysfunction is more favorable than that of systolic dysfunction. Distinguishing diastolic from systolic heart failure is essential because the optimal therapy for one may aggravate the other. Although diastolic heart failure is clinically and radiographically indistinguishable from systolic heart failure, normal ejection fraction and abnormal diastolic function in the presence of symptoms and signs of heart failure confirm diastolic heart failure. The pharmacologic therapies of choice for diastolic heart failure are angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, diuretics, and beta blockers.
An HPLC-DAD-ESI-MSn method was developed for simultaneous analysis of the chemical constituents in 'SHUANGDAN' granules, a newly developed drug widely used for treating cardiovascular disease. The chromatographic separation were performed on a Zorbax Stable Bond C18 column (4.6 mmx250 mm, 5 microm) with water with 0.5% acetic acid (A) and acetonitrile (B) as mobile phase. According to the characteristic UV absorption profile, the information of molecular weight and structure provided by ESI-MSn, 29 constituents which attributed to Radix Salviae Miltiorrhizae and Cortex Moutan, respectively, were detected and 28 constituents including 14 phenolic acids, 6 diterpenoid quinones, 6 monoterpenoids and 2 other components were identified, while some isomers were distinguished based on the MSn spectra. This method was rapid and reliable for identification of constituents in complex chemical system, 'SHUANGDAN' granules, and the newly fragmentation patterns proposed could be extended to the compounds elucidation with similar framework.