白桦脂酸-三氮唑杂化物作为新型蛋白酪氨酸磷酸酶1B抑制剂的合成与生物活性评价

doi:10.6023/cjoc202604010

有机化学 ›› 2026, Vol. 46 ›› Issue (8): 3123-3138.DOI: 10.6023/cjoc202604010 上一篇下一篇

研究论文

白桦脂酸-三氮唑杂化物作为新型蛋白酪氨酸磷酸酶1B抑制剂的合成与生物活性评价

张玉飞^a^,^b^,^†, 谭丽容^a^,^†, 钟月圆^a^,^†, 刘同征^a^,^*(), 王少华^b^,^*()

^a 暨南大学药学院广州 511436
^b 兰州大学药学院兰州 730000

收稿日期:2026-04-07 修回日期:2026-05-13 发布日期:2026-05-27
通讯作者: 刘同征, 王少华
作者简介:
^†共同第一作者
基金资助:
国家重点研发计划(2023YFA1506404); 甘肃省科技计划(23ZDFA003); 甘肃省科技计划(23JRRA1028); 甘肃省科技计划(23ZDFA015); 甘肃省科技计划(24ZD13FA017); 兰州市科技计划(2023-QN-18); 兰州市科技计划(2023-1-17); 兰州市科技计划(2024-1-17)

Synthesis and Bioactivity Evaluation of Betulinic Acid-Triazole Hybrids as Novel Protein Tyrosine Phosphatase 1B Inhibitors

Yufei Zhang^a^,^b, Lirong Tan^a, Yueyuan Zhong^a, Tongzheng Liu^a^,^*(), Shaohua Wang^b^,^*()

^a College of Pharmacy, Jinan University, Guangzhou 511436
^b School of Pharmacy, Lanzhou University, Lanzhou 730000

Received:2026-04-07 Revised:2026-05-13 Published:2026-05-27
Contact: Tongzheng Liu, Shaohua Wang
About author:
^†These authors contributed equally to this work
Supported by:
National Key R&D Program of China(2023YFA1506404); Science and Technology Program of Gansu Province(23ZDFA003); Science and Technology Program of Gansu Province(23JRRA1028); Science and Technology Program of Gansu Province(23ZDFA015); Science and Technology Program of Gansu Province(24ZD13FA017); Lanzhou Science and Technology Planning Project(2023-QN-18); Lanzhou Science and Technology Planning Project(2023-1-17); Lanzhou Science and Technology Planning Project(2024-1-17)

文章分享

1. cjoc202604010辅助材料.pdf(9049KB)

摘要/Abstract

蛋白酪氨酸磷酸酶1B (PTP1B)是胰岛素和瘦素信号通路的关键负调控因子, 已成为2型糖尿病(T2DM)的潜在治疗靶点. 抑制PTP1B可增强胰岛素敏感性, 为管理糖尿病和肥胖提供了一种潜在的策略. 在这项研究中, 35个白桦脂酸-三氮唑杂环化合物被合成, 并评估了他们的PTP1B抑制活性. 所合成的白桦脂酸(BA)杂环化合物均表现出明显高于母体BA的PTP1B抑制活性. 值得注意的是, (1R,3aS,5aR,5bR,9S,11aR)-5a,5b,8,8,11a-五甲基-9-(2-((5-甲基-4-(((E)- 4-(三氟甲基)亚苄基)氨基)-4H-1,2,4-三唑-3-基)硫代)乙酰氧基)-1-(丙-1-烯-2-基)二十氢-3aH-环戊[a]䓛-3a-羧酸(BAT28)表现出最强的活性, IC₅₀值为(1.06±0.06) μmol/L. 动力学分析表明, BAT28是一种混合型PTP1B抑制剂. CD光谱表明, BAT28与PTP1B结合并诱导酶的构象变化. 分子对接研究进一步证实, BAT28与PTP1B的活性位点相互作用. 使用口服葡萄糖耐量试验(OGTT)的体内实验表明, BAT28有效地降低了小鼠的餐后血糖水平. 此外, 药物代谢动力学(ADME)结果显示BAT28类药性良好. 上述结果提示, BAT28可作为有前景的先导化合物, 用于新型PTP1B抑制剂的开发.

关键词: 白桦脂酸, 三氮唑, 蛋白酪氨酸磷酸酶1B (PTP1B), 抑制剂

Protein tyrosine phosphatase 1B (PTP1B) is a key negative regulator of insulin and leptin signaling pathways and has emerged as a promising therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Inhibition of PTP1B enhances insulin sensitivity and offers a potential strategy for managing both diabetes and obesity. In this study, 35 betulinic acid (BA)-triazole hybrids were synthesized and evaluated for their PTP1B inhibitory activities. All synthesized BA hybrids exhibited significantly higher PTP1B inhibitory activity than parent compound BA. Notably, (1R, 3aS, 5aR, 5bR, 9S, 11aR)-5a, 5b, 8, 8, 11a-pentamethyl-9-(2-((5-methyl-4-(((E)-4-(trifluoromethyl)benzylidene)amino)-4H-1,2,4-triazol-3-yl)thio)acetoxy)-1-(prop-1-en-2-yl)icosahydro-3aH-cyclopenta[a]chrysene-3a-carboxylic acid (BAT28) demonstrated the most potent activity, with an IC₅₀ value of (1.06±0.06) μmol/L. Kinetic analysis revealed that BAT28 acted as a mixed-type PTP1B inhibitor. CD spectra indicated that BAT28 bound to PTP1B and induced conformation changes in the enzyme. Molecular docking studies further confirmed that BAT28 interacted with the active site of PTP1B. In vivo experiments using an oral glucose tolerance test (OGTT) showed that BAT28 effectively reduced postprandial blood glucose levels in mice. Additionally, BAT28 exhibited favorable drug-like properties based on in silico predictions. These findings suggested that BAT28 represented a promising lead compound for the development of novel PTP1B inhibitors.

Key words: betulinic acid, triazole, protein tyrosine phosphatase 1B (PTP1B), inhibitor

引用此文

张玉飞, 谭丽容, 钟月圆, 刘同征, 王少华. 白桦脂酸-三氮唑杂化物作为新型蛋白酪氨酸磷酸酶1B抑制剂的合成与生物活性评价[J]. 有机化学, 2026, 46(8): 3123-3138.

Yufei Zhang, Lirong Tan, Yueyuan Zhong, Tongzheng Liu, Shaohua Wang. Synthesis and Bioactivity Evaluation of Betulinic Acid-Triazole Hybrids as Novel Protein Tyrosine Phosphatase 1B Inhibitors[J]. Chinese Journal of Organic Chemistry, 2026, 46(8): 3123-3138.

导出引用 EndNote|Reference Manager|ProCite|BibTeX|RefWorks

分享此文

图/表 9

参考文献 21

[1]	(a) ElSayed, N.; Aleppo, G.; Aroda, V.; Bannuru, R.; Brown, F.; Bruemmer, D.; Collins, B.; Hilliard, M.; Isaacs, D.; Johnson, E.; Kahan, S.; Khunti, K.; Leon, J.; Lyons, S. K.; Perry, M.; Prahalad, P.; Pratley, R.; Seley, J.; Stanton, R.; Gabbay, R. Diabetes Care 2023, 46, S19.
	(b) Eleftheriou, P.; Geronikaki, A.; Petrou, A. Curr. Top. Med. Chem. 2019, 19, 246.
	(c) Sun, J.; Xiao, D.; Lang, M.; Xu, X. Mol. Diversity 2025, 29, 1669.
	(d) Hu, C.; Liang, B.; Sun, J.; Li, J.; Xiong, Z.; Wang, S.; Xu, X. Eur. J. Med. Chem. 2024, 264, 115957.
[2]	(a) Zhou, Y.; Liu, L.; Xiang, R.; Bu, X.; Qin, G.; Dai, J.; Zhao, Z.; Fang, X.; Yang, S.; Han, J.; Wang, G. Int. Immunopharmacol. 2023, 114, 109529.
	(b) Kou, X.; Li, H.; Xu, X. Int. J. Biol. Macromol. 2025, 333, 148794.
	(c) Li, M.; Sun, J.; Liang, B.; Min, X.; Hu, J.; Wu, R.; Xu, X. Bioorg. Chem. 2024, 144, 107177.
	(d) Qian, S.; Zhang, M.; He, Y.; Wang, W.; Liu, S. Future Med. Chem. 2016, 8, 1239.
[3]	(a) Cole, J.; Florez, J. Nat. Rev. Nephrol. 2020, 16, 377.
	(b) Min, X.; Guo, S.; Lu, Y.; Xu, X. J. Lumin. 2024, 269, 120437.
	(c) Liang, B.; Xiao, D.; Wang, S.; Xu, X. Eur. J. Med. Chem. 2024, 275, 116595.
[4]	(a) Byon, J.; Kusari, A.; Kusari, J. Mol. Cell. Biochem. 1998, 182, 101.
	(b) Kenner, K.; Anyanwu, E.; Olefsky, J.; Kusari, J. J. Biol. Chem. 1996, 271, 19810.
	(c) Sharma, B.; Xie, L.; Yang, F.; Wang, W.; Zhou, Q.; Xiang, M.; Zhou, S.; Lv, W.; Jia, Y.; Pokhrel, L.; Shen, J.; Xiao, Q.; Gao, L. Eur. J. Med. Chem. 2020, 199, 112373.
[5]	(a) Hussain, H.; Green, I. R.; Abbas, G.; Adekenov, S. M.; Hussain, W.; Ali, I. Expert Opin. Ther. Pat. 2019, 29, 689.
	(b) Rath, P.; Ranjan, A.; Chauhan, A.; Verma, N. K.; Bhargava, A.; Prasad, R.; Jindal, T. Appl. Biochem. Biotechnol. 2022, 194, 4683.
	(c) Agrawal, N.; Dhakrey, P.; Pathak, S. Chem. Biol. Drug Des. 2023, 102, 921.
[6]	(a) Lu, Y.; Xu, L.; Cong, Y.; Song, G.; Han, J.; Wang, G.; Zhang, P.; Chen, K. Carbohydr. Polym. 2019, 205, 63.
	(b) Xu, C.; Shi, X.; Sun, H.; Yu, L.; Zhang, L.; Lan, D.; Wu, X.; Chen, M.; Cheng, N.; Pan, Y.; He, J.; Yin, R.; Zhou, L.; Gao, N.; Zhao, J. Carbohydr. Polym. 2025, 355, 123351.
	(c) Cao, W.; Wu, J.; Zhao, X.; Li, Z.; Yu, J.; Shao, T.; Hou, X.; Zhou, L.; Wang, C.; Wang, G.; Han, J. Carbohydr. Polym. 2023, 325, 121565.
	(d) Xu, L.; Lu, Y.; Cong, Y.; Zhang, P.; Han, J.; Song, G.; Wang, G.; Chen, K. Carbohydr. Polym. 2019, 206, 811.
	(e) Wei, Z.; Chen, G.; Zhang, P.; Zhu, L.; Zhang, L.; Chen, K. Carbohydr. Polym. 2018, 198, 302.
[7]	(a) Li, J.; Shen, B.; Nie, S.; Duan, Z.; Chen, K. Carbohydr. Polym. 2019, 206, 163.
	(b) Wang, C.; Wang, R.; Chen, Y.; Wang, L.; Zhou, S.; Wang, H. Bioorg. Med. Chem. Lett. 2019, 29, 1282.
	(c) Zhou, J.; Yu, L.; Fan, Y.; Guo, C.; Lv, X.; Zhou, Z.; Huang, H.; Miao, D.; Zhang, S.; Li, X.; Zhao, P.; Liu, X.; Hu, W.; Zhang, C. Eur. J. Med. Chem. 2022, 245, 114860.
	(d) He, L.; Zhu, Y.; Fan, Q.; Miao, D.; Zhang, S.; Liu, X.; Zhang, C. Bioorg. Med. Chem. Lett. 2019, 29, 549.
	(e) Qin, L.; Cheng, X.; Wang, S.; Gong, G.; Su, H.; Huang, H.; Chen, T.; Damdinjav, D.; Dorjsuren, B.; Li, Z.; Qiu, Z.; Bian, J. J. Med. Chem. 2024, 67, 988.
[8]	(a) Paduch, R.; Kandefer-Szerszeń M.; Trytek, M.; Fiedurek, J. Arch. Immunol. Ther. Exp. 2007, 55, 315.
	(b) Sánchez-Quesada, C.; López-Biedma, A.; Warleta, F.; Campos, M.; Beltrán, G.; Gaforio, J. J. Agric. Food Chem. 2013, 61, 12173.
	(c) Choi, Y.; Park, S.; Kim, J.; Won, K.; Kim, B.; Son, J.; Lee, S.; Kim, Y. J. Med. Food 2013, 16, 2.
	(d) Hung, N. Vietnam J. Sci. Technol. 2018, 56, 69.
[9]	(a) Wahab, H.; Dianita, R.; Rathnasamy, S.; Hsing, H. Biomed. Res. Ther. 2020, 7, 3579.
	(b) Diaz-Rojas, M.; Gonzalez-Andrade, M.; Aguayo-Ortiz, R.; Rodriguez-Sotres, R.; Perez-Vasquez, A.; Madariaga-Mazon, A.; Mata, R. Front. Pharmacol. 2023, 14, 1281045.
[10]	(a) Huang, J.; Su, J.; Wang, H.; Chen, J.; Tian, Y.; Zhang, J.; Feng, T.; Di, L.; Lu, X.; Sheng, H.; Zhu, Q.; Chen, X.; Wang, J.; He, X.; Yerkinkazhina, Y.; Xie, Z.; Shu, Y.; Kang, T.; Tang, H.; Qian, J.; Zhu, W. J. Med. Chem. 2024, 67, 17319.
	(b) Liu, D.; Yu, B.; Guan, X.; Song, B.; Pan, H.; Wang, R.; Feng, X.; Pan, L.; Huang, H.; Wang, Z.; Wu, H.; Qiu, Z.; Li, Z.; Bian, J. Chem. Sci. 2023, 14, 4174.
	(c) Qiu, X.; Li, Y.; Yu, B.; Ren, J.; Huang, H.; Wang, M.; Ding, H.; Li, Z.; Wang, J.; Bian, J. Eur. J. Med. Chem. 2021, 211, 113091.
	(d) Ye, W.; Fan, C.; Fu, K.; Wang, X.; Lin, J.; Nian, S.; Liu, C.; Zhou, W. Eur. J. Med. Chem. 2022, 244, 114846.
	(e) Xu, X.; Wang, J.; Wang, M.; Yuan, X.; Li, L.; Zhang, C.; Huang, H.; Jing, T.; Wang, C.; Tong, C.; Zhou, L.; Meng, Y.; Xu, P.; Kou, J.; Qiu, Z.; Li, Z.; Bian, J. J. Med. Chem. 2021, 64, 4588.
[11]	Kumar, S.; Misra, S.; Kashaw, S.; Kashaw, V.; Kumar, A. Talanta 2026, 305, 129543.
[12]	Fermo, A.; Bisi, A.; Orioli, R.; Gobbi, S.; Belluti, F. Molecules 2026, 31, 355.
[13]	(a) Liu, Z.; Bai, X.; Sheng, L.; Sun, L.; Li, J.; Zhang, T. Chem. Nat. Compd. 2023, 59, 508.
	(b) Song, Z.; He, X.; Li, C.; Gao, L.; Wang, Z.; Tang, Y.; Xie, J.; Li, J.; Chen, G. Carbohydr. Res. 2011, 346, 140.
[14]	(a) Zheng, P.; Xiong, Z.; Liao, C.; Zhang, X.; Feng, M.; Wu, X.; Lin, J.; Lei, L.; Zhang, Y.; Wang, S.; Xu, X. J. Enzyme Inhib. Med. Chem. 2021, 36, 1938.
	(b) Lin, J.; Xiao, D.; Lu, L.; Liang, B.; Xiong, Z.; Xu, X. J. Mol. Struct. 2023, 1283, 135279.
[15]	(a) Zhang, X.; Zheng, Y.; Hu, C.; Wu, X.; Lin, J.; Xiong, Z.; Zhang, K.; Xu, X. Arabian J. Chem. 2022, 15, 104072.
	(b) Wu, X.; Zhu, W.; Lu, L.; Hu, C.; Zheng, Y.; Zhang, X.; Lin, J.; Wu, J.; Xiong, Z.; Zhang, K.; Xu, X. Arabian J. Chem. 2023, 16, 104659.
[16]	Zhang, Y.; Yu, X.; Li, J.; Liang, B.; Sun, J.; Min, X.; Xiong, Z.; Chen, W.; Xu, X. J. Mol. Struct. 2024, 1315, 138889.
[17]	(a) Welte, S.; Baringhaus, K.; Schmider, W.; Müller, G.; Petry, S.; Tennagels, N. Anal. Biochem. 2005, 338, 32.
	(b) Li, M.; Li, H.; Min, X.; Sun, J.; Liang, B.; Xu, L.; Li, J.; Wang, S.; Xu, X. J. Med. Chem. 2024, 67, 8406.
	(c) Zheng, Y.; Lu, L.; Li, M.; Xu, D.; Zhang, L.; Xiong, Z.; Zhou, Y.; Li, J.; Xu, X.; Zhang, K.; Xu, L. Bioorg. Chem. 2024, 143, 106985.
[18]	(a) Wu, S.; Tang, J.; Zhou, Y.; Xu, X.; Zhang, H.; Wang, S. Chin. J. Org. Chem. 2024, 44, 613 (in Chinese).
	(吴思敏, 唐嘉欣, 周于佳, 徐学涛, 张昊星, 王少华, 有机化学, 2024, 44, 613.)
	(b) Wen, Y.; Yu, Q.; Yang, F.; Li, J.; Lang, M.; Yan, J.; Xu, X. Mol. Diversity 2025, https://doi.org/10.1007/s11030-026-11487-5.
	(c) Wu, Q.; Fang, W.; Liu, H.; Liu, Z.; Xu, X. Front. Pharmacol. 2024, 15, 1451452.
[19]	(a) Feng, M.; Liang, B.; Sun, J.; Min, X.; Wang, S.; Lu, Y.; Xu, X. J. Mol. Struct. 2024, 1310, 138311.
	(b) Liang, B.; Li, J.; Wu, S.; Kou, X.; Liu, T.; Xu, X. J. Mol. Struct. 2025, 1322, 140481.
	(c) Zhou, H.; Wen, Y.; Wang, S.; Liu, Y.; Li, B.; Xu, X. Mol. Diversity 2025, DOI: 10.1007/s11030-025-11369-2.
[20]	(a) Zhu, P.; Yang, Y.; Qian, J.; Han, J.; Kong, D.; Sun, B.; Zhang, J.; Wei, J.; Guo, Q.; Nian, S.; Zhou, L.; Wang, G.; Hou, S. J. Mol. Struct. 2025, 1321, 140125.
	(b) Yang, X.; Huang, Z.; Ding, K.; Yang, H.; Wang, L.; Xia, Q.; Hu, R.; Shi, G.; Xu, B.; Qin, A. Sci. China Chem. 2025, 68, 1426.
	(c) Wei, W.; Xu, Q.; Wu, L.; Gong, G.; Tian, Y.; Huang, H.; Li, Z. Eur. J. Med. Chem. 2024, 270, 116333.
	(d) Peng, J.; Liu, T.; Guan, L.; Xu, Z.; Xiong, T.; Zhang, Y.; Song, J.; Liu, X.; Yang, Y.; Hao, X. Talanta 2024, 273, 125938.
	(e) Fan, Y.; Zhang, Y.; Zhang, G.; Ma, L.; Lv, Y.; Li, J.; Luan, Y.; Zhang, Y.; Chen, Y.; Ren, H.; Liu, W.; Li, M.; Wu, Y.; Chen, S.; Han, B.; Tang, Q.; Chen, L. Wesselius, A.; Su, W.; Zeegers, M.; Gu, Y.; Qin, Q.; Hao, H.; Xia, J.; Zhang, H.; Yu, E. Anal. Chem. 2025, 97, 12345.
[21]	(a) Su, L.; Zhu, X.; Ding, H.; Hu, L.; Chen, J.; Qi, S.; Luo, K.; Ling, W.; Tian, X. Sens. Actuators, B 2024, 412, 135792.
	(b) Guo, L.; Dai, H.; Ma, J.; Wang, J.; Hua, Y.; Zhou, L. BMC Chem. 2021, 15, 19.
	(c) Ding, H.; Luo, L.; Su, L.; Chen, J.; Li, Y.; Hu, L.; Luo, K.; Tian, X. Biosens. Bioelectron. 2023, 247, 115939.
	(d) Chang, X.; Gao, P.; Li, Q.; Liu, H.; Hou, H.; Wu, S.; Chen, J.; Gan, L.; Zhao, M.; Zhang, D.; Sun, S.; Wang, B. Sens. Actuators, B 2021, 345, 130363.
	(e) Zeng, Y.; Liu, F.; Wang, J.; Shao, B.; He, T.; Xiang, Z.; Wang, Y.; Zhu, S.; Yang, T.; Yu, S.; Gong, C.; Liu, L. Chin. Chem. Lett. 2025, 36, 109734.

Compound	IC₅₀/(μmol•L^－1)	Compound	R	IC₅₀/(μmol•L^－1)
BAT1	2.41±0.18	BAT19		3.40±0.19
BAT2	2.56±0.14	BAT20		2.77±0.15
BAT3	2.08±0.12	BAT21		3.17±0.19
BAT4	1.87±0.08	BAT22		3.87±0.05
BAT5	4.25±0.23	BAT23		4.06±0.27
BAT6	4.46±0.19	BAT24		2.14±0.14
BAT7	1.86±0.11	BAT25		2.35±0.16
BAT8	3.05±0.23	BAT26		3.32±0.21
BAT9	2.20±0.09	BAT27		2.94±0.09
BAT10	5.01±0.10	BAT28		1.06±0.06
BAT11	1.84±0.05	BAT29		3.53±0.27
BAT12	1.97±0.09	BAT30		2.84±0.13
BAT13	3.13±0.20	BAT31		3.91±0.25
BAT14	3.17±0.22	BAT32		1.95±0.16
BAT15	1.87±0.13	BAT33		2.50±0.14
BAT16	1.91±0.13	BAT34		1.68±0.11
BAT17	2.94±0.17	BAT35		4.42±0.28
BAT18	1.21±0.06	BA	—	8.66 ± 0.81

Compound	IC₅₀/(μmol•L^－1)	Compound	R	IC₅₀/(μmol•L^－1)
BAT1	2.41±0.18	BAT19		3.40±0.19
BAT2	2.56±0.14	BAT20		2.77±0.15
BAT3	2.08±0.12	BAT21		3.17±0.19
BAT4	1.87±0.08	BAT22		3.87±0.05
BAT5	4.25±0.23	BAT23		4.06±0.27
BAT6	4.46±0.19	BAT24		2.14±0.14
BAT7	1.86±0.11	BAT25		2.35±0.16
BAT8	3.05±0.23	BAT26		3.32±0.21
BAT9	2.20±0.09	BAT27		2.94±0.09
BAT10	5.01±0.10	BAT28		1.06±0.06
BAT11	1.84±0.05	BAT29		3.53±0.27
BAT12	1.97±0.09	BAT30		2.84±0.13
BAT13	3.13±0.20	BAT31		3.91±0.25
BAT14	3.17±0.22	BAT32		1.95±0.16
BAT15	1.87±0.13	BAT33		2.50±0.14
BAT16	1.91±0.13	BAT34		1.68±0.11
BAT17	2.94±0.17	BAT35		4.42±0.28
BAT18	1.21±0.06	BA	—	8.66 ± 0.81

[PTP1B]∶[BAT28]	α-Helix/%	β-Sheet/%	β-Turn/%	Random coil/%
1∶0	47.2	9.4	15.5	30.3
1∶1	48.0	9.1	15.2	29.0
1∶2	51.1	8.1	15.0	28.8
1∶3	58.3	6.0	14.1	26.5

[PTP1B]∶[BAT28]	α-Helix/%	β-Sheet/%	β-Turn/%	Random coil/%
1∶0	47.2	9.4	15.5	30.3
1∶1	48.0	9.1	15.2	29.0
1∶2	51.1	8.1	15.0	28.8
1∶3	58.3	6.0	14.1	26.5

白桦脂酸-三氮唑杂化物作为新型蛋白酪氨酸磷酸酶1B抑制剂的合成与生物活性评价

Synthesis and Bioactivity Evaluation of Betulinic Acid-Triazole Hybrids as Novel Protein Tyrosine Phosphatase 1B Inhibitors

RichHTML

PDF

补充材料

可视化

摘要/Abstract

引用此文

分享此文

图/表 9

参考文献 21

相关文章 15

编辑推荐

相关统计

本文评价

[1]	敖选丽, 马超洁, 王淑冰, 何蕾, 赏宇, 朱锦阳, 李建秀, 张琴, 张荣平, 侯博. 2,4-二酮内酰胺衍生物的设计、合成及其抑制Mpro活性筛选[J]. 有机化学, 2026, 46(8): 3104-3113.
[2]	于丰恺, 朱先进, 徐紫涵, 石凌宇, 石永佳, 李旭锋, 杨道山. 铜催化三组分反应合成含硫醚片段的三氮唑类化合物[J]. 有机化学, 2026, 46(7): 2825-2834.
[3]	李静, 高峰, 张万斌. 抗肿瘤药物CDK4/6抑制剂合成工艺研究进展[J]. 有机化学, 2026, 46(2): 315-355.
[4]	鲁佳琪, 王紫薇, 张磊, 张萍. C(2)-1,2,4-三氮唑取代的1,5-苯并硫氮杂䓬的合成及抑菌活性[J]. 有机化学, 2025, 45(8): 2885-2895.
[5]	郑彬, 韦敏, 林雯雯, 潘成学. 茚并异喹啉酮N-杂化衍生物的合成及其拓扑异构酶I抑制和抗肿瘤活性研究[J]. 有机化学, 2025, 45(8): 2815-2824.
[6]	李慧, 阿布力米提•阿布都卡德尔, 周磊. 可见光条件下N-苄基苯并三氮唑自由基脱氮气开环合成6-取代菲啶[J]. 有机化学, 2025, 45(5): 1770-1777.
[7]	颜逸韬, 陈颖露, 胡涵显, 吴军. 双取代嘧啶-联苯化合物的合成及除草活性和分子作用机制研究[J]. 有机化学, 2025, 45(1): 358-366.
[8]	樊莹, 黄丹凤, 马虎, 白祖瑜, 王克虎, 王君姣, 胡雨来. 二氟甲基取代的1,2,4-三氮唑啉化合物的合成[J]. 有机化学, 2024, 44(9): 2820-2831.
[9]	郑佰峰, 左炀, 陈琼, 吴琼友. 新型苯并噻唑-嘧啶二酮类化合物的设计、合成与除草活性研究[J]. 有机化学, 2024, 44(7): 2371-2376.
[10]	程婷婷, 宋高磊, 成龙, 王凡, 孙新宇, 谢治富, 张梅, 张仰明, 李静雅, 南发俊. 烷基共轭二烯基二酸作为新型ACLY抑制剂的发现[J]. 有机化学, 2024, 44(11): 3476-3489.
[11]	孙泽人, 翟冰新, 何光超, 沈慧, 陈琳雅, 张杉, 邹毅, 朱启华, 徐云根. 新型1,2,3-三氮唑类衍生物的合成及抗炎活性研究[J]. 有机化学, 2023, 43(6): 2143-2155.
[12]	纪健, 刘进华, 管丛, 陈绪文, 赵芸, 刘顺英. 原位生成的磺酸催化N-磺酰基-1,2,3-三氮唑与醇偶联高区域选择性合成N²-取代1,2,3-三氮唑[J]. 有机化学, 2023, 43(3): 1168-1176.
[13]	徐欢, 吴鸿飞, 张晓鸣, 路星星, 孙腾达, 亓悦, 林誉凡, 杨新玲, 张莉, 凌云. 含1,2,3,4-四氢异喹啉片段磺酰肼和酰肼类化合物的设计、合成及生物活性研究[J]. 有机化学, 2023, 43(2): 725-733.
[14]	高建飞, 李瞬依, 何玉龙, 李英霞, 王贺瑶, 黄二芳, 胡春. 作为FABP4/5抑制剂喹啉类化合物的设计合成与生物活性研究[J]. 有机化学, 2023, 43(2): 636-645.
[15]	孙昌兴, 张福豪, 张欢, 李鹏辉, 姜林. 新型2-(1-甲基-1H-吡唑-4-基)嘧啶-4-甲酰胺的设计、合成、杀菌活性及分子对接研究[J]. 有机化学, 2023, 43(1): 229-235.