Article
Biochemistry & Molecular Biology
Zhang Hu, Hongrui Dong, Zhenyu Si, Yurong Zhao, Yuanwei Liang, Jean-Marc Sabatier, Athina Geronikaki
Summary: Infectious diseases present a major challenge to human health, emphasizing the need for the development of novel antimicrobial agents. In this study, a series of triazolo[4,3-a]pyrazine derivatives were synthesized and evaluated for their antibacterial activity. Some of the compounds displayed moderate to good antibacterial activity against both Gram-positive and Gram-negative bacteria. Particularly, compound 2e showed excellent antibacterial activity comparable to ampicillin.
Article
Biochemistry & Molecular Biology
Alexandra E. E. Kopotilova, Tatyana N. N. Moshkina, Emiliya V. V. Nosova, Galina N. N. Lipunova, Ekaterina S. S. Starnovskaya, Dmitry S. S. Kopchuk, Grigory A. A. Kim, Vasiliy S. S. Gaviko, Pavel A. A. Slepukhin, Valery N. N. Charushin
Summary: Amino-[1,1 ']-biphenyl-containing 3-aryl-[1,2,4]triazolo[4,3-c]quinazoline derivatives with fluorescent properties were synthesized and their structures were confirmed by X-ray diffraction. The compounds exhibited non-planar structures with aryl substituents forming pincer-like conformations. The UV/Vis and photoluminescent properties were investigated in different solvents and in solid state, showing broad emission wavelengths and high quantum yields. Solvatochromic properties and aggregation-induced emission enhancement were observed for the substituted triazoloquinazolines. Moreover, changes in absorption and emission spectra were induced by trifluoroacetic acid and acidochromism was observed for some triazoloquinazoline compounds. Electronic-structure calculations were performed for the synthesized compounds.
Article
Biochemistry & Molecular Biology
Khaled El-Adl, Mohamed-Kamal Ibrahim, Mohammed S. I. Alesawy, Ibrahim H. Eissa
Summary: Novel derivatives of [1,2,4]triazolo[4,3-c]quinazoline and bis([1,2,4]triazolo)[4,3-a:4',3'-c]quinazoline were designed, synthesized, and evaluated for their anticancer activities against HepG2 and HCT-116 cell lines. The compounds displayed high sensitivity towards HCT-116 cells, with certain derivatives showing potent inhibitory effects and strong DNA-binding affinities. Most of the derivatives exhibited good ADMET profiles, indicating their potential as effective anticancer agents.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Manel Ben Hassen, Dhouha Msalbi, Badr Jismy, Fares Elghali, Sami Aifa, Hassan Allouchi, Mohamed Abarbri, Fakher Chabchoub
Summary: A series of new [1,2,4]triazolo[4,3-a]pyrimidine derivatives were synthesized using a one-pot three-component synthesis. The structures of the compounds were confirmed by various analyses. The compounds were evaluated for their antitumor activity and displayed promising results against cancer cell lines.
Article
Chemistry, Physical
Ab Majeed Ganai, Tabasum Khan Pathan, Sachin Balaso Mohite, Veronika Vojackova, Eva Reznickova, Karolina Kozlanska, Vladimir Krystof, Katya Govender, Sithabile Mokoena, Srinivas Reddy Merugu, Mahesh Palkar, Kimeshni Moodley, Rajshekhar Karpoormath
Summary: A series of novel 1,2,4-triazolo[4,3-b]pyridazine derivatives were designed and synthesized, with good to moderate yields. Spectroscopic studies (NMR and IR) confirmed the synthesis of the compounds, and the fluorine coupled 13C NMR data were explained. The compounds were tested for their in-vitro anti-proliferative activity against four human cancer cell lines, with compound 8l showing the most promising results.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Multidisciplinary
Chunyi Liu, Qiang Fei, Nianjuan Pan, Wenneng Wu
Summary: Crop diseases caused by fungi have a significant impact on food security and economic development. In this study, a novel series of 1,2,4-triazolo[4,3-c]trifluoromethylpyrimidine derivatives with thioether moiety were synthesized, inspired by the use of fungicides containing 1,2,4-triazole and trifluoromethylpyrimidine. The antifungal activities of these compounds were evaluated, and several compounds showed significant antifungal activities against multiple Botrytis cinearea species, indicating their potential as leading structures or candidates for resistance against Botrytis cinerea.
FRONTIERS IN CHEMISTRY
(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
Chemistry, Multidisciplinary
Xiaobo Liu, Yuzhen Li, Qian Zhang, Qingshan Pan, Pengwu Zheng, Xinyang Dai, Zhaoshi Bai, Wufu Zhu
Summary: In this study, a series of novel compounds were synthesized and evaluated for their inhibitory activities against cancer cells and their molecular interaction mechanisms. Compound 17l showed excellent antiproliferative activities and kinase inhibitory activities, and could intervene in cellular signaling pathways.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Khaled El-Adl, Abdel-Ghany A. El-Helby, Helmy Sakr, Alaa Elwan
Summary: In this study, 17 novel [1,2,4]triazolo[4,3-a]quinoxaline derivatives were designed and synthesized as potential anticancer agents. The compounds were evaluated for their activities against HepG2, HCT-116, and MCF-7 cancer cell lines, with compound 12(d) showing the highest potency. Molecular docking studies were conducted to investigate the binding modes of the compounds with the DNA active site, and the data obtained from these studies correlated well with the biological testing results.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Mohamed S. Alesawy, Mohamed-Kamal Ibrahim, Ibrahim H. Eissa, Khaled El-Adl
Summary: In this study, a series of novel compounds were designed, synthesized, and evaluated for their anticancer activity, DNA binding affinity, and ADMET profiles. Compound 6(f) exhibited the highest anticancer activity and DNA binding affinity, and our derivatives showed good pharmacokinetic properties, making them potential templates for the design of more effective anticancer drugs.
ARCHIV DER PHARMAZIE
(2022)
Article
Plant Sciences
F. N. Makhubu, S. M. Nkadimeng, G. Fouche, M. C. Khosa, L. J. McGaw
Summary: The study aimed to isolate and characterize nematicidal compounds from the leaves of Leonotis leonurus, with results showing potential for controlling nematodes and phytopathogens. However, it does not support the use of free-living nematodes as a model for isolating anti-parasitic compounds from plants.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Inci Selin Dogan, Bahittin Kahveci, Suat Sari, Kubra Kolci, Rengin Reis, Hande Sipahi
Summary: In this study, a series of new 1,2,4-triazolo[4,3-a]quinoxaline compounds were synthesized and compound 3 f exhibited good anti-inflammatory effect by significantly reducing nitrite levels. Molecular docking studies predicted high affinity of these compounds to the active site of iNOS.
Article
Infectious Diseases
Charalampos Kamoutsis, Maria Fesatidou, Anthi Petrou, Athina Geronikaki, Vladimir Poroikov, Marija Ivanov, Marina Sokovic, Ana Ciric, Alejandro Carazo, Premysl Mladenka
Summary: This research investigated the antimicrobial activity of 19 synthesized compounds and found that they exhibited potent antibacterial and antifungal properties, with some showing inhibitory effects on biofilm formation. Docking studies suggested potential mechanisms of action against bacterial and fungal targets, and toxicity testing in human cells confirmed their low toxicity levels.
Article
Agriculture, Multidisciplinary
Xiaofeng Cao, Mingxia Wang, Zhong Li, Xiaoyong Xu
Summary: Plant-parasitic nematodes pose a major threat to modern agriculture and chemical nematicides are still needed to manage them. In this study, aurone analogues were synthesized and evaluated for their nematicidal activity against Meloidogyne incognita. Compound 6 and its derivatives showed impressive nematicidal activity, with compound 32 having the best activity. Compound 32 also exhibited excellent inhibition on egg hatching and moderate inhibition on the motility of Caenorhabditis elegans.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Multidisciplinary Sciences
Jung-Hoon Kim, Navin Pandit, Miyoun Yoo, Tae Hyun Park, Ji U. Choi, Chi Hoon Park, Kwan-Young Jung, Byung Il Lee
Summary: BRD4 has two tandem bromodomains (BD1 and BD2) that can recognize acetylated lysine for epigenetic reading, making them promising therapeutic targets for various diseases, including cancers. BRD4 is well-studied and many chemical scaffolds for inhibitors have been developed. Research on BRD4 inhibitors for different diseases is actively ongoing.
SCIENTIFIC REPORTS
(2023)