Baylor University

在药物合成领域，如何高效实现含硫官能团的选择性修饰一直是研究热点。近日，贝勒大学 Liela Bayeh-Romero 团队在ACS Catalysis上发表了一项突破性成果，研究团队开发了锆催化酰胺还原磺酰胺化反应，为复杂药物分子的后期官能团化提供了温和高效的新方法。一、核心突破：温和条件下的选择性烷基化    传统的磺酰胺烷基化反应常面临两大难题：亲核性不足，磺酰胺类化合物的弱亲核性导致反应活性低；选择性困难，复杂分子中多官能团易引发副反应。而本研究利用二氯二茂锆（Cp₂ZrCl₂）的亲氧特性，通过双还原循环机制，首次实现了酰胺与磺酰胺的直接催化偶联。该反应在室温条件下即可进行，仅需10 mol% 催化剂和硅烷还原剂，产物收率最高达 94%，且对酯基、羟基、吲哚等敏感基团兼容性优异。图一、条件筛选（ACS Catal. 2025, 15, 10, 8150–8156）二、底物普适性：从简单分子到复杂药物    研究团队系统考察了反应的适用范围：芳香 / 杂环酰胺，带有吸电子或给电子基团的芳香酰胺均能高效反应，杂环酰胺如吡啶酰胺、吲哚酰胺也可兼容。各类含硫胺，磺酰胺、磺胺、亚磺酰胺、氨基磺酸酯等均能作为亲核试剂，甚至连强吸电子的三氟甲磺酰胺也能以 81% 收率得到目标产物。药物分子后期修饰，在 FDA 批准药物如氢氯噻嗪、唑尼沙胺、塞来昔布的结构中，该反应能实现位点选择性单烷基化，避免了传统方法中氨基或其他官能团的干扰。值得注意的是，使用氘代 DMF 时，还可精准引入氘标记甲基，为药物代谢研究提供了新工具。图二、底物拓展（ACS Catal. 2025, 15, 10, 8150–8156）三、机制探究：双催化循环的关键作用    通过原位监测和控制实验，团队提出了反应的可能机理：第一步还原，锆催化剂将酰胺部分还原为亚胺中间体：转胺反应，亚胺与磺酰胺发生亲核加成，生成关键中间体；第二次还原，硅烷还原剂将中间体还原为目标磺酰胺产物；实验发现，亚胺的还原速率比酰胺快 6 倍，这解释了反应的高效性。此外，交叉实验排除了可逆 β- 消除路径，证实了双催化循环的合理性。图三、机理研究（ACS Catal. 2025, 15, 10, 8150–8156）四、应用前景：开启药物合成新维度    该方法具有三大显著优势：原子经济性，直接利用酰胺作为烷基源，避免了传统方法中卤代烃的使用；温和条件，室温反应，无需手套箱操作，适合敏感分子修饰；化学空间拓展，通过化学信息学分析，该反应覆盖了市售 7 大类磺酰胺中的 6 类，显示出广泛的适用性。正如团队在文中指出，这种 “一石二鸟” 的策略不仅为磺酰胺类药物的结构优化提供了 “化学剪刀”，更有望推动锆催化在药物合成中的更多应用。研究总结    这项研究以地球丰富的锆金属为催化剂，在温和条件下实现了药物分子的精准修饰，为绿色化学和药物研发提供了新思路。未来，该方法或可进一步拓展至其他含氮杂环的选择性官能团化，值得持续关注！文献：Zirconium-Catalyzed Reductive Sulfonamidation of Amides and Its Application to Site-Selective N-Alkylation of Pharmaceuticals；ACS Catal. 2025, 15, 10, 8150–8156；https://doi.org/10.1021/acscatal.5c02265.

ARLINGTON, Texas, Sept. 26, 2024 (GLOBE NEWSWIRE) -- BioNTX is pleased to announce the finalists for the 3rd Annual Tech Transfer Showcase, set for Friday, October 4th, at the 2024 iC³ Life Science & Healthcare Innovation Summit. The Tech Transfer Showcase shines the spotlight on life science innovation that may be sitting on the shelf and strengthens the development of future leaders and entrepreneurs. This program is designed to assist academic institutions in presenting technologies available for licensing, collaboration and acquisition. The goal of the Tech Transfer Showcase is to connect Texas based academic institutions with Texas-based investors and industry executives that can help provide valuable insight into commercial readiness, market fit, business models, strategic partnerships, and commercial viability of all technologies. The 2024 competition was open to all Texas Universities. After submission, a panel of experienced judges reviews each university’s featured technology and selects the top six finalists to advance to the pitch showcase at the BioNTX annual Summit. In 2024, BioNTX has seen a 50% increase in applicants for this opportunity. A panel of knowledgeable judges have selected the top six finalists to advance to the pitch event at the iC³ Summit. The 2024 Tech Transfer Showcase finalists are: Baylor UniversityRice UniversityTexas Tech UniversityThe University of Texas at AustinThe University of Texas at DallasThe University of Texas Medical Branch “BioNTX is proud to provide a platform for university faculty and inventors to test their technology and receive expert guidance for the commercialization of their innovation,” reports Kathleen Otto, CEO, BioNTX. Each finalist will collaborate with a Tech Transfer judge to refine their pitch and will present their technology at the iC³ Life Science & Healthcare Innovation Summit for a chance to win a cash prize. “The BioNTX Tech Transfer Showcase is a perfect opportunity to get a glimpse into early-stage technologies coming out of the top universities in Texas. As a mentor and judge, it is very rewarding to see the progression and growth of the presenter and their pitches throughout the process,” said Chad Ronholdt, Co-founder, CEO of ASC Biosciences and Managing Director of NVB Ventures. Paul J. Corson, Chief Innovation and Entrepreneurship Officer for the University of Texas at Arlington, is the moderator of the Tech Transfer Office Showcase and Pitch Competition at the iC³ Life Science & Healthcare Innovation Summit on Friday, October 4, from 10 a.m. to 11 a.m. Corson states, “North Texas is a great place for life science startups, as evidenced by the amazing work I see at UT Arlington every day.” The Tech Transfer winner will be announced after the showcase and pitch competition at the Summit. To register for the 2024 iC³ Life Science & Healthcare Innovation Summit, please click here. About the 2024 iC3 Life Science SummitThe 10th Annual BioNTX iC³ Life Science & Healthcare Innovation Summit brings together the community and North Texas bioscience and healthcare innovation leaders for a two-day event from Thursday, October 3rd – Friday, October 4th. The iC³ Summit fosters collaboration between thought leaders, knowledge exchange, and explores the latest innovation, products, and services in the life sciences. We invite you to register for the 2024 iC³ Life Science & Healthcare Innovation Summit, please click here. About BioNTXBioNTX is the bioscience and healthcare innovation trade organization serving North Texas. The organization fosters innovation and community through collaborative networking events, high-level educational programming, professional development, market visibility, a purchasing consortium, and by being the voice for the North Texas biosciences and healthcare innovation community. Media Contact: Allison ChaneyCulver Public Relationsallison@culverpr.com

Adults who continuously played organized sports through their youth have fewer symptoms of anxiety and depression than those who never played or those who dropped out, a new study finds. And those who dropped out of sports had poorer mental health than those who never played at all. Adults who continuously played organized sports through their youth have fewer symptoms of anxiety and depression than those who never played or those who dropped out, a new study finds. And those who dropped out of sports had poorer mental health than those who never played at all. But many more people drop out of youth sports than play continuously until they are 18, said Chris Knoester, senior author of the study and professor of sociology at The Ohio State University. "If you play and stick with sports, it's a positive for your mental health, but if you play and drop out it seems to be negative -- and most kids drop out," Knoester said. The study, published in the Sociology of Sport Journal, showed that most people dropped out of sports because they weren't having fun or felt they weren't good enough. That suggests ways youth sports can be improved to help kids, said study lead author Laura Upenieks, assistant professor of sociology at Baylor University. "Our findings about why kids drop out of organized sports suggests that the current environment is less than ideal for everyone, and that the barriers to participation need to be given greater attention," Upenieks said. The study used data from the National Sports and Society Survey, conducted in 2018 and 2019 by Ohio State. It included a sample of 3,931 adults from across the country who answered questions about their sports participation as children and their current anxiety and depression symptoms. Results showed 35% of the participants did not play organized sports at all, 41% participated and dropped out and 24% participated continuously until age 18. Those who participated in organized sports continuously while growing up reported lower depressive symptoms and symptoms of anxiety than others. Those who dropped out had the worst mental health profile, with those who never played in the middle. Knoester emphasized that most participants didn't have clinical levels of depression or anxiety, and the differences between the three groups were relatively modest. But the differences still mattered. By far the most common reason cited for dropping out was "not having fun," which nearly half of respondents (45%) identified. The next most common reason was feeling like they were not a good player (31%). Other reasons for dropping out were wanting to focus on grades (16%), having a health problem or injury (16%), not being able to afford sports (16%), having an issue with team members (15%) and having an interest in other clubs and activities (14%). Notably, 8% said they dropped out because they had been abused by a coach. While dropping out of sports was associated with poorer mental health, "not all reasons for dropping out had the same effects," Upenieks said. Interpersonal reasons for dropping out -- including not having fun, not getting along with team members and being abused by a coach -- were associated with adult depressive and anxiety symptoms. Those who couldn't afford sports and sporting equipment also showed poorer mental health. But those who dropped out in order to focus on grades actually showed lower depressive symptoms, the study found. "Prioritizing education predicts better mental health as an adult," Knoester said. Many previous studies have focused on the impact of playing sports -- or not playing -- on adult outcomes. But this study is one of the first to look at what happens when youth quit sports, Knoester said, and it shows that persistence in playing is an important issue. "Unfortunately, it is not a simple story of playing sports is good for kids," he said. "It is complicated by whether kids stick to playing sports and the reasons why they do stick to it or quit." It is easy to see why sports can be good for those who are able to continue with it to adulthood, Upenieks said. "The longer that youth are exposed to a positive and encouraging sporting environment, the more likely they are to develop habits that are conducive to long-term mental well-being, such as a commitment to regular exercise and collaborating with others as part of a team," she said. The fact that so many kids quit shows that organized sports often don't provide a positive environment. But there are steps adults can take to improve that environment. For one, sports should be safe for kids. The fact that 8% said they were abused by coaches is particularly alarming, the researchers said. And the finding that nearly half of kids quit because they weren't having fun and about a third dropped out because they felt they weren't good enough should also be a wake-up call, Knoester said. "We need to improve youth sports so that it supports positive experiences for everyone and makes it more enjoyable," he said. While winning is part of sports, it may be that adults overemphasize that aspect and ruin the experience for many young people. "Most kids are looking to have fun with their friends and support and encourage each other," Upenieks said. "It doesn't have to be all serious." Knoester added: "Our results suggest that by taking away the fun and making kids feel they aren't good enough, there could be cascading effects in terms of hurting self-esteem and confidence that could reverberate through to adulthood."