Synthesis of Pyrazolesulfoximines Using α-Diazosulfoximines with Alkynes.

Sulfoximines and pyrazoles are both important motifs in medicinal compounds. Here we report the synthesis and reactivity of sulfoximine diazo compounds as new reagents for the incorporation of sulfoximines. The use of N-silyl sulfoximines enabled formation of monosubstituted diazo compounds. Their application is demonstrated in a [3 + 2] cycloaddition with alkynes to form pyrazole sulfoximines in a new combination of these important chemotypes. Further derivatization of the pyrazole sulfoximines is demonstrated, including silyl deprotection to form unprotected pyrazolesulfoximines.

The efficacy of different segments fixation for treatment thoracolumbar fractures: A Bayesian network meta-analysis.

BACKGROUND: We did this network meta-analysis to comprehensively compare the efficacy of different segments [intermediate segment (IS), short segment (SS) and long segment (LS)] in the fixation of thoracolumbar fractures. METHODS: We searched studies from inception until January 20, 2023 through PubMed, Embase, Web of Science, and the Cochrane Library. All studies comparing different segments in the fixation of thoracolumbar fractures were included in this meta-analysis. Outcomes were anterior vertebral height ratio (AVHR), sagittal Cobb angle (SCA), visual analogue scale score, and implant failure rate. This network meta-analysis was performed by R software with gemtc package. RESULTS: Finally, a total of 22 studies were finally included in this network meta-analysis. IS (WMD 2.43, 95% CrI 2.04-2.91) was more effective than SS in terms of the AVHR, and the difference was statistically significant. IS was more effective than LS in reducing SCA (WMD -2.87, 95% CrI -3.79 to -1.96) with statistically significant. Compared with SS, IS significantly reduced the SCA with statistically significant (WMD -2.52, 95% CrI -3.31 to -1.72). IS (WMD -2.87, 95% CrI -3.78 to -1.96) was more effective than LS, and the difference was statistically significant. Moreover, IS (WMD -2.52, 95% CrI -3.31 to -1.72) was more effective than SS, and the difference was statistically significant. CONCLUSION: IS was associated with a significant reduction in SCA, implant failure rate, and visual analogue scale compared to SS and LS, while having the most favorable impact on AVHR among all the treatments assessed.

The effect of lifting load on the kinematic characteristics of lumbar spinous process in vivo.

BACKGROUND: There are limited data on the in vivo natural kinematics of the lumbar spinous process. This paper intends to explore the effect of lifting load on the in vivo movement mode of the lumbar spinous process and its biomechanical changes. METHODS: Ten asymptomatic subjects between the ages of 25 and 39 underwent CT scans of the lumbar spine in the supine position, and 3D models of L3-L5 were constructed. Using a Dual Fluoroscopy Imaging System (DFIS), instantaneous orthogonal fluoroscopic images of each subject's flexion-extension, left-right bending, and left-right rotational movements were taken under different loads (0 kg, 5 kg, 10 kg). The supine CT model was matched, using computer software, to the bony contours of the images from the two orthogonal views, so that the instantaneous 3D vertebral position at each location could be quantified. A Cartesian coordinate system was ultimately constructed at the tip of the spinous process to obtain the 6DOF kinematic data of the spinous process. RESULTS: In different postural movements of the trunk, there was no significant difference in the rotation angle and translation range of the lumbar spinous process under different loads (P > 0.05). In flexion to extension motion, spinous processes mainly rotate < 4° along the medial and lateral axes and translate < 4 mm along the craniocaudal direction. In the left-right bending motion, spinous processes mainly rotate < 5° along the anterior and posterior axes, and the translation is mainly coupling < 2 mm. In the rotational motion, the spinous process is mainly coupled motion, the rotation range is less than 3°, and the translation range is less than 2 mm. The distance between spinous processes measured in the supine position was 6.66 ± 2.29 mm at L3/4 and 5.08 ± 1.57 mm at L4/5. CONCLUSION: The in vivo kinematics of the lumbar spinous process will not change significantly with increasing low load. In complex motion, the spinous process is dominated by coupling motion.

Non-coding RNAs as potential biomarkers in osteosarcoma.

Osteosarcoma (OS) is a primary solid malignant tumor that occurs most frequently in the metaphysis of long bones. More likely to happen to children and adolescents. OS has high mortality and disability rate. However, the etiology and pathogenesis of OS have not been fully understood till now. Due to the lack of effective biomarkers, OS cannot be precisely detected in the early stage. With the application of next-generation and high-throughput sequencing, more and more abnormally expressed non-coding RNAs(ncRNAs) have been identified in OS. Growing evidences have suggested the ncRNAs, such as microRNAs (miRNAs), long non-coding RNAs (lncRNAs), circular RNAs (circRNAs), have played an important role in the tumorigenesis and progression of OS. Thus, they can be served as novel biomarkers for diagnosis, treatment and prognosis. This review summarized the application of ncRNA as biomarkers in OS in detail, and discussed the limitation and future improvement of the potential biomarkers.

Synthesis of Sulfoximine Propargyl Carbamates under Improved Conditions for Rhodium Catalyzed Carbamate Transfer to Sulfoxides.

Sulfoximines provide aza-analogues of sulfones, with potentially improved properties for medicinal chemistry. The sulfoximine nitrogen also provides an additional vector for the inclusion of other functionality. Here, we report improved conditions for rhodium catalyzed synthesis of sulfoximine (and sulfilimine) carbamates, especially for previously low-yielding carbamates containing π-functionality. Notably we report the preparation of propargyl sulfoximine carbamates to provide an alkyne as a potential click handle. Using Rh2(esp)2 as catalyst and a DOE optimization approach provided considerably increased yields.