A series of novel molecules containing thiazole ring structure were designed and synthesized. The structures of the synthesized compounds were elucidated and confirmed by (1)H NMR, (13)C NMR, Mass spectrum and the purity was checked through HPLC analysis. Among these synthesized compounds, 3a-3i and 6a-6c were tested for their antimicrobial activity (minimum inhibitory concentration) against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus niger for antifungal activity respectively. The results of the antimicrobial screening data revealed that most of the tested compounds showed moderate to good microbial inhibitions.
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http://dx.doi.org/10.1016/j.bmcl.2016.06.030 | DOI Listing |
Aim: Human carbonic anhydrases (hCAs) are involved in many physiological processes including respiration, pH control, ion transport, bone resorption, and gastric fluid secretion. Recently, CA IX and CA XII have been studied for their role in cancer diseases, motivating the design of inhibitors of these isoforms.
Material And Method: Here, we used the tail approach to design a new series of monoaryl () and bicyclic () benzensulfonamide derivatives CA IX and CA XII inhibitors.
Pest Manag Sci
January 2025
State Key Laboratory of Elemento-Organic Chemistry, Department of Chemistry, Nankai University, Tianjin, China.
Background: Increasing the diversity of lead compounds has been shown to enhance the efficacy of diamide insecticides. Fifty novel compounds were precisely designed and synthesized utilizing fragment-based assembly and virtual screening coupling.
Results: The median lethal concentration (LC) values of compounds X-30 and X-40 against Mythimna separata were 0.
J Med Chem
January 2025
College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.
The P2YR is activated by UDP and UDP glucose and is involved in many human inflammatory diseases. Based on the molecular docking analysis of currently reported P2YR antagonists and the crystallographic overlap study between PPTN and compound , a series of 3-substituted 5-amidobenzoate derivatives were designed, synthesized, and identified as promising P2YR antagonists. The optimal compound (methyl 3-(1-benzo[]imidazol-2-yl)-5-(2-(-tolyl) acetamido)benzoate, IC = 0.
View Article and Find Full Text PDFJ Pestic Sci
November 2024
Graduate School of Agriculture, Ehime University.
The enantiospecific anti-phytopathogenic fungal activity of a new type of coumarin bearing a phenylpropanoid unit at the 3-position was found. ()-3-[1-Methoxy-3-(4-methoxyphenyl)prop-2-yl]coumarin (()-: EC=16.5 µM) was 30 times more effective than the ()-form against the Japanese pear pathotype.
View Article and Find Full Text PDFRSC Adv
January 2025
Institute of Chemistry, Vietnam Academy of Science and Technology (VAST) 18 Hoang Quoc Viet, Cau Giay Hanoi Vietnam
Podophyllotoxin, along with its numerous derivatives and related compounds, is well known for its broad-spectrum pharmacological activity, especially for anticancer potential. In this study, several isatin-podophyllotoxin hybrid compounds were successfully synthesized with good yields through microwave-prompted three-component reactions of 2-amino-1,4-naphthoquinone, various substituted isatins, and tetronic acid. Their cytotoxicity was assessed against four types of human cancer cell lines, HepG2 (hepatoma carcinoma), MCF7 (breast cancer), A549 (non-small lung cancer), and KB (epidermoid carcinoma), alongside nontumorigenic HEK-293 human embryonic kidney cells.
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