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Synthesis and antifungal activities of N-1,3,4-thiadiazol-2-yl-4-oxo-thiochroman-2-yl-formamide derivatives
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Xiao-yan HAN1, Sheng-bin LI1, Guo-chao LIANG1, Guan ZHOU1, Yi-fan ZHONG1, Hui QI1, Ya-li SONG1, 2, *, Xiao-qiang QIAO1, 2, *
Acta Pharmaceutica Sinica | 2017, 52(1) : 113 - 119
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Acta Pharmaceutica Sinica | 2017, 52(1): 113-119
• ORIGINAL ARTICLES •
Synthesis and antifungal activities of N-1,3,4-thiadiazol-2-yl-4-oxo-thiochroman-2-yl-formamide derivatives
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Xiao-yan HAN1, Sheng-bin LI1, Guo-chao LIANG1, Guan ZHOU1, Yi-fan ZHONG1, Hui QI1, Ya-li SONG1, 2, *, Xiao-qiang QIAO1, 2, *
Affiliations
  • 1. College of Pharmaceutical Sciences, Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China
  • 2. Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of the Ministry of Education, Hebei University, Baoding 071002, China
Published: 2017-01-12 doi: 10.16438/j.0513-4870.2016-1023
Outline
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Thiochromanones and 1,3,4-thiadazoles as heterocyclic compounds have broad biological activities. In order to find novel compounds with antifungal bioactivity, substituted thiophenol and maleic anhydride were used to synthesize the intermediate 4-oxothiochromane-2-carboxylic acid. It was reacted with 2-amino-1,3,4-thiadiazol to get fourteen target compounds containing 1,3,4-thiadazole moiety. The structures of the obtained compounds were confirmed by 1H NMR, 13C NMR and HR-MS. All compounds were investigated for antifungal activity via microdilution broth method. The results showed that the target compounds 3a and 3c to Epidermophyton floccosum and Mucor racemosus exhibited better antifungal activity than the positive control fluconazole, in which the minimum inhibition concentration can reach 8 μg·mL-1 and 16 μg·mL-1. Compound 3e showed significant inhibitory activity to Helminthosporium maydis, Sclerotinia sclerotiorum and Botrytis cinerea compared with that of the positive control carbendazim. Compound 3b exhibited inhibitory activity to Helminthosporium maydis better than the positive control carbendazim.

thiochromanone  /  1,3,4-thiadazole  /  microdilution broth method  /  antifungal activity
韩晓燕, 李生彬, 梁国超, 周冠, 钟一凡, 齐慧, 宋亚丽, 乔晓强. N-1,3,4-噻二唑-2-基硫色满-4-酮-2-甲酰胺衍生物的合成及抗真菌活性测定. 药学学报, 2017 , 52 (1) : 113 -119 . DOI: 10.16438/j.0513-4870.2016-1023
Xiao-yan HAN, Sheng-bin LI, Guo-chao LIANG, Guan ZHOU, Yi-fan ZHONG, Hui QI, Ya-li SONG, Xiao-qiang QIAO. Synthesis and antifungal activities of N-1,3,4-thiadiazol-2-yl-4-oxo-thiochroman-2-yl-formamide derivatives[J]. Acta Pharmaceutica Sinica, 2017 , 52 (1) : 113 -119 . DOI: 10.16438/j.0513-4870.2016-1023
Appendix
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Year 2017 volume 52 Issue 1
510
232
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Article Info
doi: 10.16438/j.0513-4870.2016-1023
  • Receive Date：2016-10-20
  • Online Date：2026-01-14
  • Published：2017-01-12
Article Data
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History
  • Received：2016-10-20
  • Revised：2016-12-01
Funding
Affiliations
    1. College of Pharmaceutical Sciences, Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China
    2. Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of the Ministry of Education, Hebei University, Baoding 071002, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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