Article
Chemistry, Organic
Wafa A. Bawazir, Daniyah K. Alnajjar
Summary: A new type of compound was synthesized by treating 8-nitro-1,2,4-triazino[5,6-b]indole-3-(2H,5H)thione with various alkylating agents and different regioselective conditions. The chemical reactivity of the compound was investigated and its promising antibacterial activity was confirmed through testing.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Article
Chemistry, Physical
Reem L. B. Alanazi, Mehvash Zaki, Wafa A. Bawazir
Summary: The study synthesized Ni(II) and Cu(II) metal complexes of Schiff-base derived from 5H-[1,2,4]triazino[5,6-b]indol-3-amine and salicylaldehyde, using secondary ligands 2,2'-Bipyridine and 1,10 phenanthroline. These complexes exhibited different DNA binding characteristics and tendencies, as well as influences on the HSA structure.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Medicinal
Lili Chen, Ying Yun, Shimeng Guo, Xiaoyan Wang, Muya Xiong, Tingting Zhao, Tifei Xu, Jianhua Shen, Xin Xie, Kai Wang
Summary: Danuglipron is a representative small-molecule agonist of the glucagon-like peptide-1 receptor (GLP-1R) that has shown positive results in clinical trials for the treatment of type 2 diabetes mellitus (T2DM) and obesity. However, it has limitations such as hERG inhibition, lower activity compared to endogenous GLP-1, and short action time. This study introduces a new class of 5,6-dihydro-1,2,4-triazine derivatives that eliminate hERG inhibition caused by danuglipron, and identifies compound 42 as a highly potent and selective GLP-1R agonist with improved efficacy and acceptable drug-like properties. Compound 42 demonstrates longer-lasting effects in reducing glucose excursion and inhibiting food intake, making it a feasible treatment for T2DM and obesity.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Sumeyye Yalduz, Mehmet Yilmaz
Summary: In this study, furo[2,3-d]pyrido[1,2-a]pyrimidin-4-ones were synthesized by microwave-assisted radical cyclizations. The reaction was performed between 2-hydroxy-4H-pirido[1,2-a]pirimidin-4-ones and conjugated alkenes and phenylacetylene using Mn(OAc)(3) as a catalyst. Different reaction conditions were compared to optimize the reaction. The obtained compounds were characterized using spectroscopic techniques and XRD analysis.
Article
Chemistry, Organic
Xiaobiao Lu, Xi Xiao, Ming Zhang, Changfeng Wan, Haoqing Hou, Jieping Wan
Summary: Polycyclic aromatic nitrogen-containing heterocyclic compounds are important in drugs and materials, with indole-fused pyridine compounds being widely used. A new synthesis method was developed for 2-substituted pyrido[2,3-b]indole derivatives using 2-(2-aminophenyl)acetonitrile derivatives and N,N-dimethyl enaminones as substrates, providing high selectivity and efficiency.
CHINESE JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Agriculture, Multidisciplinary
Jian Zhang, Runjiang Song, Shang Wu, Di Cai, Zengxue Wu, Deyu Hu, Baoan Song
Summary: In this study, a series of novel mesoionic pyrido[1,2-a]pyrimidinone compounds were designed and synthesized, and their insecticidal activities were tested. The results showed that compound7 exhibited outstanding insecticidal activities against white-backed planthoppers and bean aphids, with superior activity against the latter compared to the existing insecticide triflumezopyrim. Further analysis indicated that compound7 may interact with specific protein subunits in white-backed planthoppers.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Chemistry, Physical
Sheikdawood Parveen, Thathan Premkumar, Hung-Huy Nguyen, Subbiah Govindarajan
Summary: A new compound, 3,7-diethyl-1H-[1,2,4]triazino[4,3-b][1,2,4]triazine-4,8-dione, was successfully synthesized through a one-step condensation reaction in aqueous medium. The compound was characterized by various spectroscopic techniques and its crystal structure was determined by single-crystal X-ray diffraction. The thermal reactivity and stability of the compound were analyzed using thermogravimetry-differential thermal analysis under different atmospheres. Additionally, the compound exhibited photoluminescent emission.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Poorvi Saraf, Prabhash Nath Tripathi, Manish Kumar Tripathi, Avanish Tripathi, Himanshu Verma, Digambar Kumar Waiker, Royana Singh, Sushant Kumar Shrivastava
Summary: A series of novel derivatives were synthesized and evaluated for their inhibitory potential against COX-2 and 5-LOX enzymes. Compound 6k showed the best inhibitory activity and also exhibited significant anti-inflammatory, antioxidant, and non-cardiotoxic properties.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Esam S. Allehyani
Summary: The text describes the efficient synthesis and characterization of a novel compound, which was used to form two categories of heteroannulated compounds. The synthesized products showed variable inhibitory effects against tested microorganisms, and their structures were elucidated using spectral and elemental microanalysis.
SYNTHETIC COMMUNICATIONS
(2022)
Article
Chemistry, Medicinal
Michael Moir, Samuel Lane, Andrew P. Montgomery, David Hibbs, Mark Connor, Michael Kassiou
Summary: The development of selective CB2 receptor agonists is a promising therapeutic approach for inflammatory diseases. Through structure-activity relationship studies, a potent and selective pyrazolo-[2,3-e]-[1,2,4]-triazine agonist has been discovered, with key structural features of the linkage group being important for its activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Alexander A. Lukoyanov, Andrey A. Tabolin, Yulia Nelyubina, Sema L. Ioffe, Alexey Yu. Sukhorukov
Summary: It has been discovered that six-membered cyclic nitronates can react with aryne to form a tricyclic nitroso acetal. This reaction involves the selective cleavage of the N-O bond of the isoxazoline ring, leading to the synthesis of compounds with potential synthetic value.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Physical
Maryam Tahmasby, Ali Darehkordi, Marziyeh Mohammadi, Farzaneh Nejadkhorasani
Summary: This study describes an efficient method for synthesizing potentially biologically active [2H]-pyrido [1,2-b]1,2,4-triazines derivatives. The intramolecular hydrogen bonding interactions were investigated at the theoretical level, revealing that the strength of the hydrogen bonding increases in the presence of electron-donor substituents.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Organic
Dongping Cheng, Hongshuang Xia, Huafang Gu, Yawei Wang, Jing-Hua Li, Xiaoliang Xu
Summary: An efficient tandem oxidative reaction of uracils/thiouracil with 1,3-diarylpropenes catalyzed by DDQ/tert-butyl nitrite/TBN/O-2 is reported. This reaction involves oxidative coupling, intramolecular cyclization, and dehydro-aromatization processes to produce multi-substituted pyrido[2,3-d]pyrimidines/thiopyrido[2,3-d]pyrimidines in moderate to excellent yields. It offers the advantages of high atom economy, green terminal oxidant, and metal-free conditions.
SYNTHESIS-STUTTGART
(2023)
Article
Chemistry, Analytical
Natasa Perin, Darko Babic, Petar Kassal, Ana Cikos, Marijana Hranjec, Robert Vianello
Summary: This study presents the synthesis and characterization of three novel pH probes with potential application in pH-sensing materials. The systems were designed with different numbers and positions of isobutylamine groups, affecting their photophysical and acid-base properties. Computational analysis suggests that a system with three amino substituents may serve as an excellent starting point for a potential pH sensor.
Article
Chemistry, Applied
Hedieh Rostami, Lotfi Shiri
Summary: This study successfully reported the synthesis of pyrido[2,3-d:5,6-d']dipyrimidines using magnetic nanoparticles with excellent yields in water. The synthesized catalyst was identified using various techniques, providing important references for further research.
APPLIED ORGANOMETALLIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Hamada Mohamed Ibrahim, Haider Behbehani
Article
Chemistry, Multidisciplinary
Hamada Mohamed Ibrahim, Haider Behbehani, Noha S. Mostafa
Article
Chemistry, Multidisciplinary
Haider Behbehani, Hamada Mohamed Ibrahim
Article
Multidisciplinary Sciences
Hamada Mohamed Ibrahim, Haider Behbehani
SCIENTIFIC REPORTS
(2020)
Article
Multidisciplinary Sciences
Haider Behbehani, Fatemah A. Aryan, Kamal M. Dawood, Hamada Mohamed Ibrahim
SCIENTIFIC REPORTS
(2020)
Article
Chemistry, Multidisciplinary
Haider Behbehani, Kamal M. Dawood, Fatemah A. Aryan, Hamada Mohamed Ibrahim
Summary: A suitable and effective Q-tube-assisted strategy for the synthesis of novel thiochromeno[4,3-b]pyridine and chromeno[4,3-b]pyridine derivatives was developed, showing superior results compared to conventional methods. The proposed mechanistic route involves two sequential dehydrative stages and was authenticated through X-ray crystallographic analysis.
Article
Chemistry, Organic
Hamada Mohamed Ibrahim, Haider Behbehani
JOURNAL OF ORGANIC CHEMISTRY
(2020)
Article
Chemistry, Multidisciplinary
Hamada Mohamed Ibrahim, Haider Behbehani, Wael Abdelgayed Ahmed Arafa
Article
Chemistry, Multidisciplinary
Hamada Mohamed Ibrahim, Wael Abdelgayed Ahmed Arafa, Haider Behbehani