ABSTRACT
Aliphatic strained rings have been increasingly applied in medicinal chemistry due to their beneficial physicochemical and pharmacokinetic properties. However, the divergent synthesis of enantioenriched cyclobutane derivatives with various structural patterns continues to be a significant challenge. Here, we disclose a palladium-catalyzed enantioselective desymmetrization of cyclobutenes, resulting in a series of hydroarylation and 1,2- and 1,3-diarylation products via the interceptions of a common Heck intermediate. Mechanistic investigations provide valuable insights into understanding the catalytic mode of the palladium catalysts and the observed variations in the deuterium-responsive behavior during reactions. Furthermore, the synthetic utility is demonstrated in the syntheses of deuterated drug candidate belaperidone skeletons and pseudosymmetrical truxinic acid-type derivatives.
ABSTRACT
Two convenient and practical methods for the synthesis of axially chiral biaryls bearing the trifluoromethylthio group are reported. A Cu-catalyzed enantioselective ring-opening reaction of cyclic diaryliodoniums with CsSCF3 enables the direct synthesis of trifluoromethylthiolated biaryl atropisomers in high yields and enantioselectivity. For unsymmetric cyclic diaryliodoniums bearing an adjacent group to the C-I bond, a two-step procedure is required to achieve good regio- and enantioselectivity.
ABSTRACT
The objective of the present study was to evaluate the anti-inflammatory effects of Bifidobacterium animalis subsp. lactis strain BB12 in stimulated Caco-2 cells and to characterize the factors responsible for these anti-inflammatory effects. Characterization and purification studies indicate that BB12's anti-inflammatory factors might include a 50-kDa proteinaceous compound that is stable under a variety of heat and pH conditions.
Subject(s)
Anti-Inflammatory Agents/metabolism , Bifidobacterium/metabolism , Gene Expression/drug effects , Interleukin-8/antagonists & inhibitors , NF-kappa B/antagonists & inhibitors , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Bacterial Proteins/chemistry , Bacterial Proteins/isolation & purification , Bacterial Proteins/metabolism , Caco-2 Cells , Humans , Hydrogen-Ion Concentration , Molecular Weight , Protein Stability , TemperatureABSTRACT
PURPOSE: To compare the effects of analgesic therapies on odontalgia caused by pulpitis in molars by three different methods. METHODS: 173 molars were diagnosed as irreversible pulpitis, and randomized block designed in three groups. Under block or local anesthesia: 46 cases of the first group, leaving teeth on open drainage, after 1 day, sealing devitalized material (arsenic), arranged next appointment 2 weeks later. 52 molars of the second group, enlarging exposure site, drainage several minutes only, sealed devitalized material, re-examined 2 weeks later. 75 cases of the third group, removing roof of pulp chamber, undergoing pulpectomy directly, re-examined 1 week later. Adopting VAS(vital analogue scale) to analyze the pulp receptivity of three different methods and to evaluate the analgesic effects by complete analgesia, effective analgesia, and no response. The data was analysed using chi-square test. RESULTS: The rate of complete analgesia was 50.0%, 63.46% and 76.0%, respectively. There was a significant difference in complete analgesia among the three methods. The analgesic effect of the third group (pulpectomy) was significantly higher than that of the first group (P<0.01).Pulpectomy group had impossibility of adverse effects caused by using devitalizing material (arsenic). CONCLUSIONS: It is worthy to adopt pulpectomy extensively to relieve the pain of molars caused by pulpitis clinically. The course of treatment of the third group was significantly shorter than other groups, and the simultaneous symptoms occurred rarely.
Subject(s)
Pulpectomy , Pulpitis/physiopathology , Toothache/therapy , Adult , Aged , Aged, 80 and over , Female , Humans , Male , Middle Aged , MolarABSTRACT
OBJECTIVE: To study the indication and contraindication of opening pulp chamber therapy for patients with a history of remote myocardial infarction. METHODS: Blood pressure (BP), heart beat rate and electrocardiographic examination were determined during opening pulp chamber therapy in patients with acute and chronic pulpititis and a history of remote myocardial infarction. RESULTS: High blood pressure and quick heart beat were found during local anaesthetic injection and opening of pulp chamber (during local anaesthetic injection BP increased by 12.52/8.04 mmHg, heart rate by 4.02 times/min;during opening of pulp chamber BP and heart rate increased by 15.43/8.0 mmHg, 6.37 times/min respectively). Electrocardiogram showed myocardial ischemic pattern deteriorated in some patients with the history of coronary insufficiency. CONCLUSIONS: Most patients can bear it. Comprehensive physical examinations, evaluations of the patients' cardial status, mental state and indispensible equipment are necessary. The therapy is recommended to be operated under the monitor electrocardiography for the safety of the patients.
