Article
Chemistry, Physical
Rajarshi Nath, M. Shahar Yar, Shelly Pathania, Gourav Grover, Biplab Debnath, Md Jawaid Akhtar
Summary: A series of novel anticonvulsant compounds were designed and synthesized, with the most active compound N-(5-chlorobenzo[d]thiazol-2-yl)-2-(2,3-dioxoindolin-1-yl)acetamide (4a) showing significant anticonvulsant activity and potential pharmaceutical value. In silico studies and molecular docking were conducted to investigate the molecular interactions and drug likeness properties of the compounds.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Medicinal
Gourav Grover, Rohit Pal, Rohit Bhatia, M. Shahar Yar, Rajarshi Nath, Shamsher Singh, Khadga Raj, Bhupinder Kumar, Md Jawaid Akhtar
Summary: A series of novel clubbed aryl oxadiazole-1,2,4-triazine derivatives were designed and synthesized for potential anticonvulsant activity, with two compounds showing significant effectiveness against both generalized tonic-clonic and absence seizures. The lead compound demonstrated the highest efficacy with increased GABA concentration.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Chemistry, Physical
R. Raveesha, K. Yogesh Kumar, M. S. Raghu, S. B. Benaka Prasad, Ali Alsalme, Prakash Krishnaiah, M. K. Prashanth
Summary: Two new series of pyrazine derivatives were synthesized and evaluated for their antioxidant, anticonvulsant, and neurotoxicity properties. Compounds 2a, 2b, and 2e showed good anticonvulsant activity and minimal neurotoxicity. Computational analysis revealed strong binding interactions of these compounds in the binding pocket of a specific protein. The results suggest that compounds 2a, 2b, and 2e have potential as safer and more effective anticonvulsant drugs with neuroprotective properties.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Review
Pharmacology & Pharmacy
Rangappa S. Keri, Srinivasa Budagumpi, Sasidhar Balappa Somappa
Summary: This review aims to summarize the most relevant studies since 1990 in the field of medicinal chemistry related to coumarin-based anticonvulsant agents. It provides a panoramic view and design suggestions for biologists and medicinal chemists. These findings contribute to the rational design of more effective and safer antiepileptic drugs.
JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS
(2022)
Article
Chemistry, Multidisciplinary
Ameen A. Abu-Hashem, Mahmoud N. M. Yousif, Abdel-Rhman Barakat Ahmed El-Gazzar, Hend N. Hafez
Summary: This study synthesized a series of compounds with diverse pharmacological activities and evaluated their antimicrobial activity in vitro. These compounds may provide a new approach for future drug design.
JOURNAL OF THE CHINESE CHEMICAL SOCIETY
(2023)
Article
Medicine, General & Internal
H. Kalabharathi, Ayesha Mariam, Vidya Doddawad, S. Shivananda, C. Sanjay
Summary: This study examines the anticonvulsant properties of an ethanolic extract derived from Harpagophytum procumbens leaves. The results demonstrate that the extract has significant antiepileptic activity in both models, suggesting its potential use in managing grand mal epilepsy and absence seizures.
INTERNATIONAL JOURNAL OF ACADEMIC MEDICINE
(2023)
Article
Medicine, General & Internal
Bader Alsuwayt, Vijay Chidrawar
Summary: The study found that the essential oil of Commiphora Myrrha has significant anticonvulsant effects in the PTZ-induced epilepsy model, possibly related to modulating GABA levels. However, no protective effect was observed in the strychnine-induced model.
ANNALS OF CLINICAL AND ANALYTICAL MEDICINE
(2021)
Article
Pharmacology & Pharmacy
Albashir Tahir, Hauwau Abubakar, Aminu Umar Kura, Suleiman Yunusa, Yahaya M. Katagum
Summary: The use of plants in traditional medicine has been widely recognized for its effectiveness in treating chronic and infectious diseases. Boswellia dalzielii, a plant from the Burseraceae family, has been extensively used in African traditional medicine and has been found to have medicinal value. This study aims to evaluate the anticonvulsant potential of the methanolic stem bark extract of Boswellia dalzielii.
ADVANCES IN PHARMACOLOGY AND PHARMACY
(2023)
Article
Chemistry, Medicinal
H. L. Kalabharathi, Pragathi Balakrishna, Patali N. Snehalatha, V Ashwini, Ramith Ramu
Summary: The methanolic extract of Acorus calamus leaves exhibited significant anticonvulsant activity in mice, possibly mediated by enhancing GABA activity. Further research is needed to confirm these results and understand the mechanism of action on GABA receptor signaling.
INTERNATIONAL JOURNAL OF LIFE SCIENCE AND PHARMA RESEARCH
(2021)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)