Article
Chemistry, Organic
Mateus Mittersteiner, Genilson S. Pereira, Yuri Silva, Ludger A. Wessjohann, Helio G. Bonacorso, Marcos A. P. Martins, Nilo Zanatta
Summary: Selective N- or O-alkylation of 4-(trihalomethyl)-pyrimidin-2(1H)-ones using 5-bromo enones/enaminones as alkylating agents is reported. The selectivity towards the N- or O-regioisomer is determined by the substituent at the 6-position of the pyrimidine ring, allowing the preparation of each isomer as the sole product in yields of 60-95%. Subsequent cyclocondensation of the enaminone moiety with nitrogen dinucleophiles leads to pyrimidine-azole conjugates with yields of 55-83%.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Caiyun Yu, Yuanshuang Xu, Xinying Zhang, Xuesen Fan
Summary: This paper presents an efficient synthesis of N-arylindoles through the cascade reaction, which simultaneously introduces the N-aryl unit and constructs the indole scaffold. The method offers several advantages, including readily accessible and halide-free substrates, additive-free reaction conditions, good efficiency, excellent atom economy, and compatibility with diverse functional groups.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Jun Liu, Ying Meng, Ming-Han Yang, Xiao-Yi Zhang, Jian-Fu Zhao, Ping-Hua Sun, Wei-Min Chen
Summary: In this study, several 3-hydroxypyridin-4(1H)-one hybrids were designed and synthesized, and their potential as inhibitors of P. aeruginosa biofilm formation was evaluated. The most active compound, 12h, exhibited significant biofilm inhibitory activity. Mechanistic studies revealed that 12h inhibited biofilm formation by suppressing the expression of lasB and pqsA. Furthermore, 12h improved the antibiotic susceptibility of P. aeruginosa and reduced its acute virulence in Vero cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Organic
Han-Fu Liu, Mu-Xue He, Hai-Tao Tang
Summary: This study presents a new electrocatalytic method for the synthesis of 3-hydroxyalkylquinoxalin-2(1H)-ones via a radical pathway, avoiding the use of stoichiometric oxidants and heavy metal catalysts. The method has potential application value, as demonstrated by scale-up studies in electrochemical continuous flow reactors.
ORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Chemistry, Applied
Jingzhi Sui, Yun He, Tao Wang, Yong Liang, Zunting Zhang
Summary: The synthesis of three types of quinoline compounds, including trans-4a,12b-dihydrodibenzo[fh]quinolin-2(1H)-ones (2), dibenzo[f,h]quinolin-2(1H)-ones (3) and 3,4-dihydrodibenzo[f,h]quinolin-2(1H)-ones (4), was achieved through photo-induced annulation of 6-([1,1'-biphenyl]-2-yl)pyridine-2(1H)-ones (1) under 313 nm UV light. The highest yield reached 95%.
ADVANCED SYNTHESIS & CATALYSIS
(2021)
Article
Neurosciences
Woo-Ju Song, Jang-Hyuk Yun, Myeong-Seon Jeong, Kil-Nam Kim, Taekyun Shin, Hyoung-Chun Kim, Myung-Bok Wie
Summary: Trimethyltin (TMT) is an environmental neurotoxin that affects human dopaminergic neuronal survival through various mechanisms. Several antioxidants and drugs can alleviate TMT toxicity, including by altering apoptosis-related proteins and affecting necrotic features in cells.
Article
Chemistry, Applied
Daokai Xiong, Zhengjie Zhang, Jing Zhang, Yurong Wang, Jianguo Yang, Zhiming Wang, Pengfei Zhang
Summary: Hexafluoroisopropanol (HFIP) is widely used as a versatile reaction media in organic synthesis, but its application as a catalyst has been rarely explored. This study presents the HFIP-catalyzed Mannich-type reaction between quinoxalin-2(1H)-ones and difluoroenoxysilanes. The developed protocol allows for the incorporation of various substituents under mild reaction conditions, providing a divergent approach to the synthesis of difluoro-substituted 3,4-dihydroquinoxalin-2(1H)-ones and monofluoroquinoxalin-2(1H)-ones in yields of 51-92%.
ADVANCED SYNTHESIS & CATALYSIS
(2023)
Article
Chemistry, Multidisciplinary
Mateus Mittersteiner, Genilson S. Pereira, Ludger A. Wessjohann, Helio G. Bonacorso, Marcos A. P. Martins, Nilo Zanatta
Summary: This study presents two strategies for preparing O-alkyl derivatives of 6-substituted-4-(trifluoromethyl)pyrimidin-(1H)-ones. A total of 18 derivatives of the targeted pyrimidines were obtained through direct chemoselective O-alkylation.
Review
Plant Sciences
Gugulethu P. Khumalo, Ben Erik Van Wyk, Yunjiang Feng, Ian E. Cock
Summary: Traditional medicinal plants from southern Africa are commonly used to treat inflammation and pain-related ailments, but there is still a lack of research on their anti-inflammatory properties and further studies are needed.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Jaismy Jacob, S. L. Manju
Summary: This study synthesized molecules with dual COX-2 and 5-LOX inhibitory activity using thiazole and thiazolidene-based pharmacophores, and identified a promising compound with potential for improved anti-inflammatory properties.
MEDICINAL CHEMISTRY RESEARCH
(2021)
Article
Plant Sciences
Fiaz Alam, Muhammad Hanif, Asad ur Rahman, Sayyad Ali, Saeed Jan
Summary: The study evaluated the analgesic, antipyretic, and anti-inflammatory properties of Gaultheria trichophylla extract and salicylate-rich fraction in vivo, in vitro, and in silico. The results showed significant effects, supporting the traditional medicinal use of these components.
JOURNAL OF ETHNOPHARMACOLOGY
(2023)
Article
Plant Sciences
N. Mbhele, B. Ncube, A. R. Ndhlala, A. Moteetee
Summary: This study investigated the antioxidant and anti-inflammatory activities of six indigenous medicinal plants in South Africa and found their potential as wound healing agents.
SOUTH AFRICAN JOURNAL OF BOTANY
(2022)
Review
Chemistry, Applied
Kai Sun, Fang Xiao, Bing Yu, Wei-Min He
Summary: The review provides an overview of recent advances in the photo-/electrocatalytic functionalization of quinoxalin-2(1H)-ones, covering a variety of reactions and discussing the reaction scope and mechanism in detail.
CHINESE JOURNAL OF CATALYSIS
(2021)
Review
Oncology
Dan Pu, Liyuan Yin, Lin Huang, Changlong Qin, Yuwen Zhou, Qiang Wu, Yan Li, Qinghua Zhou, Lu Li
Summary: COX-2, frequently expressed in cancer cells, is associated with poor prognosis. PGE2, a key factor in immunosuppression, triggers tumor immune evasion and leads to poor response to immunotherapy. COX-2 inhibitors may help to restrain the immunosuppressive effects of PGE2 and enhance or reverse the response to immune checkpoint inhibitors.
FRONTIERS IN ONCOLOGY
(2021)
Review
Chemistry, Medicinal
Ryldene Marques Duarte da Cruz, Francisco Jaime Bezerra Mendonca-Junior, Natalia Barbosa de Melo, Luciana Scotti, Rodrigo Santos Aquino de Araujo, Reinaldo Nobrega de Almeida, Ricardo Olimpio de Moura
Summary: This review discusses the role of thiophene-based derivatives in inflammation and their significance in the design and discovery of novel anti-inflammatory drugs, focusing on structural characteristics and mechanism studies.
Article
Chemistry, Medicinal
Khaled R. A. Abdellatif, Mohamed A. Abdelgawad, Heba A. H. Elshemy, Shahinda S. R. Alsayed, Gehan Kamel
ARCHIVES OF PHARMACAL RESEARCH
(2015)
Article
Chemistry, Medicinal
Khaled R. A. Abdellatif, Mohamed A. Abdelgawad, Madlen B. Labib, Taha H. Zidan
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2015)
Article
Biochemistry & Molecular Biology
Khaled R. A. Abdellatif, Phoebe F. Lamie, Hany A. Omar
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Medicinal
Khaled R. A. Abdellatif, Eman K. A. Abdelall, Wael A. A. Fadaly, Gehan M. Kamel
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2016)
Article
Biochemistry & Molecular Biology
Khaled R. A. Abdellatif, Mohamed A. Abdelgawad, Heba A. H. Elshemy, Shahinda S. R. Alsayed
BIOORGANIC CHEMISTRY
(2016)
Article
Chemistry, Medicinal
Khaled R. A. Abdellatif, Amany Belal, Hany A. Omar
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2013)
Article
Chemistry, Medicinal
Khaled R. A. Abdellatif, Abeer Moawad, Edward E. Knaus
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2014)
Article
Biochemistry & Molecular Biology
Ahmed M. Gouda, Ahmed H. Abdelazeem, El-Shaimaa A. Arafa, Khaled R. A. Abdellatif
BIOORGANIC CHEMISTRY
(2014)
Article
Biochemistry & Molecular Biology
Khaled R. A. Abdellatif, Heba A. H. Elshemy, Samir A. Salama, Hany A. Omar
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Zhangjian Huang, Carlos A. Velazquez, Khaled R. A. Abdellatif, Morshed A. Chowdhury, Julie A. Reisz, Jenna F. DuMond, S. Bruce King, Edward E. Knaus
JOURNAL OF MEDICINAL CHEMISTRY
(2011)
Article
Biochemistry & Molecular Biology
Khaled R. A. Abdellatif, Eman K. A. Abdelall, Mohamed A. Abdelgawad, Rasha R. Ahmed, Rania B. Bakr
Article
Biochemistry & Molecular Biology
Heba F. Salem, Rasha M. Kharshoum, Amr F. Gamal, Fatma I. Abo El-Ela, Khaled R. A. Abdellatif
JOURNAL OF LIPOSOME RESEARCH
(2020)
Article
Engineering, Multidisciplinary
Ahmed Emam, Khaled R. A. Abdellatif, Noha H. Amin, Khaled M. Elokely
Summary: HCV, an RNA virus with no available vaccine, poses challenges for developing effective medications due to genetic differences and mutations leading to drug resistance. Important amino acids affecting ligand recognition have been identified, with mutations potentially impacting ligand affinity, as demonstrated through molecular dynamics simulation studies.
INTERNATIONAL JOURNAL OF MODELLING AND SIMULATION
(2022)
Article
Chemistry, Multidisciplinary
Mohamed A. S. Badawy, Eman K. A. Abdelall, EL-Shaymaa EL-Nahass, Khaled R. A. Abdellatif, Hamdy M. Abdel-Rahman
Summary: In this study, a novel series of benzimidazole derivatives were designed and synthesized, with some compounds showing selective inhibition to COX-2 isozyme. Among them, compound 11b exhibited the strongest inhibitory activity against COX-2 with good anti-inflammatory activity and lower ulcerogenic liability. Molecular docking studies were consistent with the in vitro COX-2 inhibitory activities.
Article
Chemistry, Medicinal
Khaled R. A. Abdellatif, Mohamed A. Abdelgawad, Madlen B. Labib, Taha H. Zidan
ARCHIV DER PHARMAZIE
(2017)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)