Article
Chemistry, Medicinal
Monica de Gaetano, Catherine Tighe, Kevin Gahan, Andrea Zanetti, Jianmin Chen, Justine Newson, Antonino Cacace, Mariam Marai, Andrew Gaffney, Eoin Brennan, Phillip Kantharidis, Mark E. Cooper, Xavier Leroy, Mauro Perretti, Derek Gilroy, Catherine Godson, Patrick J. Guiry
Summary: The failure to resolve inflammation underlies many prevalent pathologies. Lipid mediators like lipoxins have been identified as drivers of inflammation resolution, suggesting potential therapeutic benefit. The novel quinoxaline-containing synthetic-LXA(4)-mimetic (R)-6 shows potent anti-inflammatory properties, attenuating inflammatory responses both in vitro and in vivo.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemical Research Methods
Yue Zeng, Feng Tang, Wei Shi, Qian Dong, Wei Huang
Summary: This review summarizes the recent advances in glycoengineering, including new strategies in chemoenzymatic synthesis of glycans, glycopeptides, glycoproteins, and other glycoconjugates, as well as the progresses of cell surface glyco-editing methods for gain of functions.
CURRENT OPINION IN BIOTECHNOLOGY
(2022)
Review
Chemistry, Medicinal
Seyedeh Roya Alizadeh, Mohammad Ali Ebrahimzadeh
Summary: Heterocyclic compounds, especially pyrazolotriazine derivatives, exhibit diverse biological activities with therapeutic potential. This review categorizes and explores the biological activities, synthesis procedures, structure-activity relationships, and mechanisms of action of various pyrazolotriazines. Overall, it summarizes past and current studies on the discovery of lead compounds with significant biological activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Agriculture, Multidisciplinary
Qing Zhou, Yuanxiang Zhou, Yunying Zhu, Chenyu Gong, Yongjun Wu, Wei Xue
Summary: Novel 1,4-pentadien-3-one derivatives with a sulfonamide moiety were synthesized and their activities against fungi, bacteria, and viruses were tested. These compounds exhibited potent antibacterial and antifungal effects, and some showed promising antiviral activity. The study suggests that active splicing can enhance the biological activity of natural compounds, providing potential for the development of novel pesticides.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Sadaf Fatima, Almaz Zaki, Hari Madhav, Bibi Shaguftah Khatoon, Abdur Rahman, Mohd Wasif Manhas, Nasimul Hoda, Syed Mansoor Ali
Summary: In this study, several 2-methoxy-6-((4-(6-morpholinopyrimidin-4-yl)piperazin-1-yl)(phenyl)methyl)phenol derivatives were synthesized and their anti-inflammatory activity in LPS-stimulated macrophage cells was evaluated. Among these derivatives, 2-methoxy-6-((4-methoxyphenyl)(4-(6-morpholinopyrimidin-4-yl)piperazin-1-yl)methyl)phenol (V4) and 2-((4-fluorophenyl)(4-(6-morpholinopyrimidin-4-yl)piperazin-1-yl)methyl)-6-methoxyphenol (V8) showed significant inhibition of NO production at non-cytotoxic concentrations. These compounds also reduced iNOS and COX-2 gene and protein expression, indicating their potential as a novel therapeutic strategy for inflammation-associated disorders.
Article
Chemistry, Medicinal
Wenxin Wang, Zhijun Cao, Zhongcheng Yang, Ya Chen, Huixin Yao, Danting Zhou, Peixin Ou, Wanqiu Huang, Shixuan Jiao, Siliang Chen, Lianru Chen, Yuxia Liu, Jianming Mao, Jiayi Xie, Ruojing Xiang, Yuanqian Yang, Yisi Chen, Yonghong Yang, Liyun Tan, Haolong Tang, Luyong Zhang, Zheng Li
Summary: In this study, a novel sulfonamide FXR agonist 19 was synthesized through structure-based scaffold hopping strategy and showed promising therapeutic potential for NASH treatment with acceptable safety profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Sergey N. Adamovich, Igor A. Ushakov, Elizaveta N. Oborina, Alexander V. Vashchenko
Summary: A series of sulfonamide-bridged silatranes were synthesized and characterized in this study. Computational screening showed that these compounds have drug-like features and antimicrobial properties.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2022)
Review
Oncology
Yucui Xin, Yingsheng Zhang
Summary: Tumor cells can be specifically targeted by disrupting the function of the other genes in synthetic lethality (SL) settings, while leaving normal cells unharmed. Paralogs, homologous genes that have diverged from each other, are ideal SL targets in tumor cells due to their frequent homozygous loss. However, the unclear mechanisms of targeting these gene pairs and the difficulty in finding specific inhibitors hinder further clinical development.
FRONTIERS IN ONCOLOGY
(2023)
Article
Agriculture, Multidisciplinary
Zihui Yang, Xuebao Sun, Yigui Qiu, Daojun Jin, Yiming Zheng, Jia Li, Wen Gu
Summary: In this study, a series of novel fungicides were designed and synthesized. Compound 4b showed potent antifungal activity against Botryosphaeria dothidea and displayed significant protective and curative effects on apple fruits infected by B. dothidea. The primary antifungal mechanism of 4b was found to be enhancing cell membrane permeability, disrupting mycelial surface morphology and cell ultrastructure.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Agriculture, Multidisciplinary
Qing Zhou, Yuanxiang Zhou, Yunying Zhu, Chenyu Gong, Yongjun Wu, Wei Xue
Summary: Novel 1,4-pentadien-3-one derivatives containing a sulfonamide moiety were synthesized and found to exhibit strong antifungal, antibacterial, and antiviral activities. These compounds showed superior activity against bacteria and fungi compared to commercial agents. The results suggest that active splicing can enhance the biological activity of natural compounds and contribute to the development of novel pesticides.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Review
Pharmacology & Pharmacy
Zachary S. Clauss, Jessica R. Kramer
Summary: Carbohydrates play essential roles in living organisms, while glycopolymers serve as biomimetic analogs for studying carbohydrate-dependent processes. Glycopolypeptides, as closer structural mimics of natural glycoproteins, show promise as carriers for biologically active carbohydrates in biomedical applications such as therapeutic delivery and tissue engineering.
ADVANCED DRUG DELIVERY REVIEWS
(2021)
Article
Acoustics
Przemyslaw Zareba, Anna K. Drabczyk, Artur Wnorowski, Edyta Pindelska, Gniewomir Latacz, Jolanta Jaskowska
Summary: This paper presents a new synthesis pathway for the production of arylsulfonamide derivatives with valuable biological activities. The method is environmentally friendly and efficient, utilizing ultrasound-assisted or microwave synthesis. The synthesized compounds showed cytotoxic activity and potential usefulness in pharmacotherapy.
ULTRASONICS SONOCHEMISTRY
(2022)
Article
Chemistry, Medicinal
John E. Philo, Jenna D. Caudle, Reema N. Moussa, Patrick M. Kampmeyer, Tasfia R. Hasin, David K. Seo, Robert J. Sheaff, Angus A. Lamar
Summary: A library of 34 lipophilic sulfonamides based on the memantine core was synthesized to find potential drug candidates for crossing the blood-brain barrier and targeting glioblastoma. The library was tested against 4 mammalian cell lines, including U-87 (glioblastoma). Further synthetic variation of the active compounds confirmed the importance of specific regions of the pharmacophore, with the sulfonamide functionality and S-aryl unit having the most significant impact. In silico investigations suggest that the active compounds might target DDR1 or RET proteins. The study has identified several compounds for further development and lead optimization.
Article
Chemistry, Multidisciplinary
Haiyang Dong, Lu Lu, Xueting Song, Youkang Li, Jinguang Zhou, Yungen Xu, Yahong Zhang, Jianguo Qi, Tingting Liang, Jianhong Wang
Summary: Colchicine binding site inhibitors (CBSIs) are potential microtubule targeting agents (MTAs) that can overcome multidrug resistance and reduce toxicity. In this study, tetrahydroquinoxaline sulfonamide derivatives were synthesized and evaluated for their antiproliferative activities. Compound I-7 showed the most inhibitory activity against HT-29 cell line, inhibited tubulin polymerization, and arrested cell cycle at G2/M phase. Additionally, it was found that I-7 targeted the colchicine binding site through hydrogen and hydrophobic interactions.
Article
Biochemistry & Molecular Biology
Mostafa M. Ghorab, Aiten M. Soliman, Gharieb S. El-Sayyad, Maged S. Abdel-Kader, Ahmed I. El-Batal
Summary: A series of 4-((7-methoxyquinolin-4-yl) amino)-N-(substituted) benzenesulfonamide 3(a-s) compounds were synthesized by reacting 4-chloro-7-methoxyquinoline 1 with different sulfa drugs. The structures of the synthesized compounds were confirmed by spectroscopic data analysis. The antimicrobial activity of the compounds against Gram-positive bacteria, Gram-negative bacteria, and unicellular fungi was evaluated. Compound 3l exhibited the highest activity against most tested bacterial and fungal strains. It also showed antibiofilm activity against different pathogenic microbes, with high percentages of biofilm extension observed.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Organic
Fuying Zhu, Yamei Lin
Summary: In this study, a low-metal iron-supported catalyst (Fe20/NC-Mg) was reported for the efficient synthesis of quinoxaline compounds, using water as a solvent and without additional bases. The synergistic effect of FeNx site and Mg (OH)2 nanorods in the catalyst played a key role in achieving high yields (82-91%) in 16 examples. The gram-level synthesis and reusability of the catalysts after four cycles demonstrated its industrial application potential.
Article
Chemistry, Organic
Mikhail Kozlov, Alexey Tyurin, Andrey Dmitrenok, Vyacheslav Rusak, Aleksander Fedorov, Igor Zavarzin, Yulia Volkova
Summary: This study presents a novel and practical synthesis method for phosphorus-substituted 1,3,4-thiadiazolines using phosphorylthioformic acid hydrazides and ketones. The protocol demonstrates operational simplicity, availability of reagents, and tolerance towards different functional groups.
Article
Chemistry, Organic
Jisna Jose, Thomas Mathew
Summary: 2-Cyclopentenone and its derivatives are highly esteemed synthetic intermediates with exceptional utility in organic synthesis. They are favored structural motifs in numerous pharmaceutical drugs and natural products, highlighting their significance. The review discusses the various methods used to synthesize cyclopentenones from 2016 to 2023.
