Article
Biochemistry & Molecular Biology
Jiafeng Wang, Jiale Wu, Yinglong Han, Jie Zhang, Yu Lin, Haijun Wang, Jing Wang, Jicheng Liu, Ming Bu
Summary: Two new series of betulin derivatives with semicarbazone or thiosemicarbazone groups at the C-28 position were synthesized and evaluated for cytotoxicity against various cancer cell lines. Compound 8f demonstrated the most potent cytotoxicity against MCF-7 cells. Mechanism studies indicated that compound 8f may induce mitochondrial-mediated apoptosis pathway in MCF-7 cells.
Article
Biochemistry & Molecular Biology
Arshia, Sharmeen Fayyaz, Muniza Shaikh, Khalid Mohammed Khan, M. Iqbal Choudhary
Summary: The study identified benzophenone thio- and semicarbazone as novel DPP-IV inhibitors with moderate to good enzyme inhibitory activity. Pharmacophore studies indicated that substitution of aryl group at C-4'' of benzene ring with a lipophilic substituent and addition of a hydroxyl at C-4' strongly influenced the inhibitory activity.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Organic
Gulsah Karakaya, Aysun Ozdemir, Asli Ture, Berrin Ozcelik, Mutlu Aytemir
Summary: Dermatophytes are pathogenic fungi that cause superficial fungal infections. Current antifungal drugs have drawbacks, leading to the need for new antidermatophyte agents.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Ali Almasirad, Maryam Ghadimi, Saeideh Mirahmadi, Pouya Ahmadian Kodakan, Reza Jahani, Maryam Nazari, Elham Rezaee, Homa Azizian, Parmida Rabizadeh, Sayyed Abbas Tabatabai, Mehrdad Faizi
Summary: Thiazolidinones have been hybridized with benzodiazepine receptor-binding scaffolds to create novel compounds with extensive anticonvulsant effects. The newly designed derivatives exhibit potent anticonvulsant activity and show promise as potential oral agents. The involvement of benzodiazepine receptors in the pharmacological effects of these compounds has been confirmed.
MOLECULAR DIVERSITY
(2022)
Article
Chemistry, Multidisciplinary
Mirna Jabbour, Mohammad Ammar Al-Khayat
Summary: In this study, we have developed promising drug candidates with multiple activities, including antimicrobial, antioxidant, antileishmanial, and anticancer effects. The synthesized compounds exhibited free radical scavenging activity, with compound 1 being the most effective. They showed antibacterial activity comparable to the standard drug and were highly effective against Leishmania tropica. The compounds also demonstrated good antiproliferative activity against cancer cells.
JOURNAL OF CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Qingfei Meng, Xue Ren, Rui Wang, Yu Han, Xiufen Li, Qin Zhang, Zhenpeng Li, Yuexing Wang, Longjiang Huang, Haibo Yu
Summary: A series of 3(1,2,3,6-tetrahydropyridine)-7-azaindole derivatives were synthesized and evaluated for their anticonvulsant activities and neurotoxicity. Compounds 4i, 4p, and 5k showed significant anticonvulsant activities in the PTZ-induced epilepsy model, but not in the MES model. These compounds also exhibited lower neurotoxicity. The presence of a N-atom at the 7-position of the 7-azaindole and a double-bond in the 1,2,3,6-tetrahydropyridine skeleton were found to be essential for the antiepileptic activities.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Abdulrahman G. Alhamzani, Tarek A. Yousef, Mortaga M. Abou-Krisha, M. S. Raghu, K. Yogesh Kumar, M. K. Prashanth, Byong-Hun Jeon
Summary: This study designed and synthesized triazine-linked triazole compounds and evaluated their anticonvulsant abilities. The results showed that some of these compounds exhibited significant anticonvulsant activity and could serve as potential novel anticonvulsant agents. Computational analysis also supported the pharmacophoric characteristics of these compounds. Therefore, these triazine-linked triazole analogues may contribute to future research and development.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Chemistry, Multidisciplinary
Mingxia Song, Wennan Zhao, Yangnv Zhu, Wenli Liu, Xianqing Deng, Yushan Huang
Summary: This study discovered a new triazolopyrimidine compound (6d) with good antiepileptic activity and a high protection index. The compound showed significant anticonvulsant effects in multiple epilepsy models and exerted its action through interaction with GABA receptors.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Muhammad Khalid, Rifat Jawaria, Muhammad Usman Khan, Ataualpa Albert Carmo Braga, Zahid Shafiq, Muhammad Imran, Hafiz Muhammad Ahmad Zafar, Ahmad Irfan
Summary: In this study, seven derivatives of salicylaldehyde thiosemicarbazones were synthesized and analyzed using spectral techniques and quantum chemical studies, showing excellent agreement between experimental and computational findings. The investigation revealed the significance of nonbonding transitions for the stability of prepared molecules and the presence of a promising charge transfer phenomenon. Furthermore, the global reactivity parameters indicated that the synthesized compounds were less reactive and more stable, with potential significance for high-tech NLO applications.
Article
Chemistry, Physical
R. Raveesha, K. Yogesh Kumar, M. S. Raghu, S. B. Benaka Prasad, Ali Alsalme, Prakash Krishnaiah, M. K. Prashanth
Summary: In this study, a multistep reaction sequence was explored to obtain novel anticonvulsant compounds with greater selectivity and reduced toxicity. These compounds exhibited promising antimicrobial and antioxidant activities.
CHEMICAL PHYSICS LETTERS
(2022)
Review
Chemistry, Physical
Irtiqa Ashraf Mir, Qurat Ul Ain, Tanzeela Qadir, Azad Qayoom Malik, Saima Jan, Sakineh Shahverdi, Syed Ayaz Nabi
Summary: Semicarbazones are versatile compounds formed by the condensation reaction of imines with aldehydes or ketones. Transition metal complexes containing imine ligands have shown potential in various fields such as pharmacology, nanotechnology, and biological composite oxidation. These compounds have demonstrated promising results in antifungal, antiviral, and catalytic applications. Spectroscopic data such as IR and NMR have been analyzed, and different types of semicarbazone complexes have been discussed.
JOURNAL OF MOLECULAR STRUCTURE
(2024)
Review
Biochemistry & Molecular Biology
Jessica E. Mendieta-Wejebe, Martha C. Rosales-Hernandez, Itzia I. Padilla-Martinez, Efren V. Garcia-Baez, Alejandro Cruz
Summary: (T)Us and BTs have shown diverse biological activities. When combined, (T)UBTs are formed, which have improved physicochemical and biological properties, making them interesting for medicinal chemistry.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Xiang Huang, Shiyang Dong, Hua Liu, Pingnan Wan, Tiantian Wang, Hexiu Quan, Zengcai Wang, Zengtao Wang
Summary: In this study, a series of novel benzo[d]isoxazole derivatives were designed and synthesized as anticonvulsants. The most potent compound, Z-6b, displayed high protection against seizures induced by MES, and selectively inhibited the Na(V)1.1 sodium channel.
ACS CHEMICAL NEUROSCIENCE
(2022)
Article
Chemistry, Physical
Fekadu Muleta, Tegene Desalegn, Taye B. Demissie, Rajalakshmanan Eswaramoorthy, H. C. Ananda Murthy, Kah-Yoong Chan, Bianca L. Davids, Kennedy J. Ngwira
Summary: In this study, novel heteroleptic Cu(II) and Zn(II) complexes were synthesized using two semicarbazone-based derivative ligands. The complexes were characterized by various methods, and their potential for scavenging free radicals and antibacterial effects were examined. The results show that the complexes exhibit good antibacterial and antioxidant activities, with [Zn(L1)(L2)] complex showing the highest binding potential. This study highlights the significance of multi-semicarbazone ligands and their complexes for enhancing the biological activities of metal complexes.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
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)
