Design, Synthesis and Biological Evaluation of Novel Ketamine Derivatives as NMDAR Antagonists.

Depression is a chronic, severe, and often life-threatening neurological disorder. It not only causes depression in patients and affects daily life but, in severe cases, may lead to suicidal behavior and have adverse effects on families and society. In recent years, it has been found that sub-anesthetic doses of ketamine have a rapid antidepressant effect on patients with treatment-resistant depression and can significantly reduce the suicidal tendencies of patients with major depressive disorder. Current studies suggest that ketamine may exert antidepressant effects by blocking NMDAR ion channels, but its anesthetic and psychotomimetic side effects limit its application. Here, we report efforts to design and synthesize a novel series of ketamine derivatives of NMDAR antagonists, among which compounds 23 and 24 have improved activity compared with ketamine, introducing a new direction for the development of rapid-acting antidepressant drugs.

Complete genome sequence of a novel fusarivirus from the phytopathogenic fungus Fusarium sp.

Fusarium diseases include wilts, blights, rots, and cankers of many horticultural, field, ornamental, and forest crops in both agricultural and natural ecosystems, and they significantly hinder food plant production. Here, we describe a novel mycovirus, tentatively designated as "Fusarium fusarivirus 1" (FuFV1), which was discovered in an isolate of the phytopathogenic fungus Fusarium sp. FuFV1 has a positive-sense single-stranded RNA (+ssRNA) genome of 6,391 nucleotides (nt) containing three open reading frames (ORFs). ORF1 encodes a large polypeptide of 1,501 amino acids (aa) with conserved RNA-dependent RNA polymerase (RdRp) and helicase (Hel) domains. ORF2, overlapping ORF1 by 122 nucleotides, encodes a polypeptide with a conserved Smc domain. The third and smaller ORF (ORF3) encodes a polypeptide with an unknown function. BLASTp analysis of the ORF1-encoded polypeptide revealed that FuFV1 shares the highest aa sequence similarity (68.5% identity, E-value 0.0) with Fusarium poae fusarivirus 1 (FpFV1, genus Alphafusarivirus). Phylogenetic analysis of the RdRp and helicase (Hel) sequences indicated that FuFV1 clustered closely with FpFV1 in a separate branch within the clade containing members of the genus Alphafusarivirus. Based on these results, we propose that FuFV1 should be considered a novel mycovirus belonging to the genus Alphafusarivirus of the family Fusariviridae.

Copper-Catalyzed Aerobic Oxidative Dehydrogenative Coupling to Access Benzo[c]cinnolines.

In this paper, a highly efficient copper-catalyzed oxidative dehydrogenative coupling to obtain benzo[c]cinnolines (up to 100% yield) was developed. It was found that DMAP was a highly efficient ligand for copper-catalyzed oxidation, and molecular oxygen was a green oxidizing agent. In this simple process, various functional groups were tolerated under mild reaction conditions, and the practicality of the process was demonstrated by the preparation of benzo[c]cinnolines on a gram scale and later derivatization.

Controllable Selective Oxidation of Anilines to Azoxybenzenes and Nitrobenzenes by Regulating the Base.

The importance of selectively oxidizing aniline into value-added chemicals azoxybenzene and nitrobenzene is well-recognized in organic synthesis. However, the lack of control over selectivity and the complex synthesis of costly catalysts significantly hinder these reactions' industrial applications. In this work, an environmentally friendly approach was developed for the selective oxidization of substituted anilines. This method involves adjusting the strength of alkalinity with peroxide as the oxidant, without the addition of any metals or additives. A mild base (NaF) facilitated azoxybenzene formation, while a stronger base (NaOMe) enabled the synthesis of nitroaromatics. These protocols are user-friendly and scalable, accommodating various substitution patterns and functional groups, yielding products with high to excellent yields. The findings of this work present a framework for investigating base catalysis in organic synthesis and provide a viable and effective approach for selectively oxidizing aniline.

Human-computer interactive physical education teaching method based on speech recognition engine technology.

With the advent of the era of artificial intelligence, speech recognition engine technology has a profound impact on social production, life, education, and other fields. Voice interaction is the most basic and practical type of human-computer interaction. To build an intelligent and automatic physical education teaching mode, this paper combines human-computer interaction based on speech recognition technology with physical education teaching. Students input through voice signals, and the system receives signals, analyzes signals, recognizes signals, and feeds back information to students in multiple forms. For the system to process the external speech signal, this paper uses the Mel cepstral coefficient algorithm to extract the speech information. By comparing the speech recognition rate and antinoise rate of Hidden Markov Model, Probabilistic Statistics Neural Network, and Hybrid Model (Hidden Markov and Rate Statistical Neural Network combination), the speech recognition engine uses the hybrid model, and its speech recognition rate is 98.3%, and the average antinoise rate can reach 85%. By comparing the human-computer interaction physical education teaching method with the traditional teaching method, the human-computer interaction method is superior to the traditional teaching method in the acquisition of physical knowledge, the acquisition of physical skills, the satisfaction of physical education courses and the ability of active learning. It effectively solves the drawbacks of traditional physical education and rationally uses human-computer interaction technology. On the basis of not violating physical education, realize the diversification of physical education, improve the quality of teaching, improve students' individual development and students' autonomous learning ability. Therefore, the combination of human-computer interaction and physical education based on recognition engine technology is the trend of today's physical education development.

The Development Strategy of Home-Based Exercise in China Based on the SWOT-AHP Model.

In view of the increasing importance of sports to people and the impact of COVID-19 on people's lives, home-based exercise has become a popular choice for people to keep fit due to its unique advantages and its popularity is expected to keep growing in the future. Therefore, it is necessary to determine the development direction of home-based exercise and put in the corresponding efforts. However, there is currently a lack of research on all aspects of home-based exercise. The purpose of this research was to investigate the effective sustainable development strategy of home-based exercise in China through a SWOT (Strengths, Weaknesses, Opportunities and Threats) and AHP (Analytic Hierarchy Process) hybrid model. Thirteen factors corresponding to the SWOT analysis were identified through a literature review and expert opinions. The results show that in China the advantages and potential outweigh the weaknesses and threats of home-based exercise. Home-based exercise should grasp the external development opportunities and choose the SO development strategic type that combines internal strengths and external opportunities. As the core for the development of home-based exercise, this strategy should be given priority. To sum up, home-based exercise is believed to have a bright future.

[Early surgical outcomes of coronary heart disease with severe ischemic mitral regurgitation].

OBJECTIVE: To summarize the experience with surgical treatment of coronary artery disease with severe ischemic mitral valve regurgitation (IMR). METHODS: From January 2006 to December 2009, 45 patients (35 males, 10 females aged 32-74 years) with the diagnosis of coronary artery disease complicated by IMR underwent coronary artery bypass grafting (CABG) combined with mitral valve plasty (MVP, 24 cases) or mitral valve replacement (MVR, 21 cases). RESULTS: Perioperative deaths occurred in 2 cases due to multiple organ failure (MOF). Echocardiography showed a significant reduction of the mitral regurgitation area (from 11.80∓2.45 cm(2) to 2.83∓0.98 cm(2), t=22.80, P=0.00) after CABG combined with mitral valve surgery, with also significantly reduced postoperative left ventricular end diastolic diameter (LVEDD) (from 57.61∓10.06 mm to 51.84∓8.98 mm, t=2.85, P=0.005). No significant difference was detected in the left ventricular ejection fraction after the operation [(52.7∓15.4)% vs (53.2∓13.2)%, t=0.16, P=0.87)]. CONCLUSIONS: CABG combined with mitral valve surgery can improve early postoperative left ventricular function in patients with ischemic coronary heart disease complicated by severe mitral regurgitation, but further follow-up study is still needed for evaluation of the long-term results.

[Early and mid-term results after 17 mm St Jude Regent mechanical valve replacement in 44 patients with small aortic root].

OBJECTIVE: To analyze the changes in the cardiac function after St. Jude Regent mechanical valve replacement and assess the prosthesis-patient matching. METHODS: From October 2007 to March 2009, 44 patients received implantation of 17 mm St. Jude aortic prostheses in our hospital. The patients were followed up for clinical symptoms, signs, electrocardiogram (ECG), echocardiogram and cardiac functions, and the results were compared with those of randomly selected 44 patients receiving 21 mm St. Jude aortic prostheses. RESULTS: In 17 mm St Jude Medica Regent valve group, 8 patients presented with ECG ST segment changes, 3 complained of chest tightness, 3 had occasional chest pain and discomfort, and 8 had grade II and 4 grade III cardiac function. In 21 mm St Jude Medical Regent valve group, 6 patients had ECG ST segment changes, 2 complained of chest tightness, 2 reported occasional chest pain and discomfort, 11 had grade II and 2 grade III cardiac function. No significant differences were found in these indices between the two groups (P=0.32). Compared with those before operation, the two groups showed significant improvements in the left ventricular end-diastolic diameter, left ventricular posterior wall thickness, left ventricular mass index, and aortic pressure gradient (P<0.05). A significant increase in the left ventricular ejection fraction occurred 6-12 months after operation, but without statistical difference between the two groups (P>0.05). CONCLUSION: For underweight patients (<60 kg) and those with small body surface area (<1.6 cm(2)), 17 mm St. Jude Medical Regent valve prosthesis may produce good therapeutic effect, and some indices are even close to those after placement of 21 mm St. Jude Medical Regent valve prosthesis. No obvious prosthesis-patient mismatch occurs after the placement of the 17 mm valve prosthesis and aortic valve ring expansion is not necessary.