Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids:Design,synthesis and in vitro anti-mycobacterial activity evaluation

被引：2

作者：

Yaohuan Zhang ^{[1
]}

Ruo Wang ^{[1
]}

Tesen Zhang ^{[1
]}

Weitao Yan ^{[1
]}

Yihong Chen ^{[1
]}

Yanping Zhang ^{[1
]}

机构：

[1] Muyang Zhou College of Chemistry, Fuzhou University

来源：

Chinese Chemical Letters | 2019年 / 30卷 / 03期

关键词：

Benzofuran; Isatin; Hybrid compounds; Anti-mycobacterial; Anti-tubercular; Multi-drug resistant; Structure-activity relationship;

D O I：

暂无

中图分类号：

TQ460.1 [基础理论];

学科分类号：

1007 ;

摘要：

A series of novel benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids were designed, synthesized and evaluated for their in vitro anti-TB activities against drug-sensitive MTB H;Rv and MDR-TB isolates as well as cytotoxicity. All benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids exhibited considerable in vitro anti-mycobacterial activities against the tested three MTB strains, and all of them also showed acceptable cytotoxicity. The most active hybrid 7f was >4.8 and >51 folds more potent than the first line anti-TB agents RIF and INH against both drug-sensitive MTB H;Rv and MDR-TB isolates, respectively. The results demonstrated the potential utility of benzofuran-isatin-hydroxylimine/-thiosemicarbazide hybrids as anti-TB agents.

引用

页码：653 / 655

页数：3

共 50 条

[21] Design, synthesis and evaluation of indole-2-carboxamides with pan anti-mycobacterial activity
Franz, Nicholas D.
Belardinelli, Juan Manuel
Kaminski, Michael A.
Dunn, Louis C.
de Moura, Vinicius Calado Nogueira
Blaha, Michael A.
Truong, Dan D.
Li, Wei
Jackson, Mary
North, E. Jeffrey
BIOORGANIC & MEDICINAL CHEMISTRY, 2017, 25 (14) : 3746 - 3755
[22] 1H-1,2,3-triazole-tethered 8-OMe Ciprofloxacin and Isatin Hybrids: Design, Synthesis and in vitro Anti-mycobacterial Activities
Xu, Zhi
Song, Xu-Feng
Qiang, Min
Lv, Zao-Sheng
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2017, 54 (06) : 3735 - 3741
[23] Design, Synthesis, and in vitro Anti-mycobacterial Evaluation of Propylene-1H-1,2,3-triazole-4-methylene-tethered (Thio)semicarbazone-isatin-moxifloxacin Hybrids
Xu, Zhi
Song, Xu-Feng
Fan, Jing
Lv, Zao-Sheng
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2018, 55 (01) : 77 - 82
[24] In vitro interaction of Mycobacterium tuberculosis and macrophages: Activation of anti-mycobacterial activity of macrophages and mechanisms of anti-mycobacterial activity
OBrien, L
Roberts, B
Andrew, PW
TUBERCULOSIS, 1996, 215 : 97 - 130
[25] Heteronuclear 5-Fluoroisatin Dimers: Design, Synthesis, and Evaluation of Their In Vitro Anti-mycobacterial Activities
Deng, Jia-Lun
Liu, Xiao-Cheng
Cai, Guang-Wei
Zhang, Gang
Hu, Li
Qiu, Li
Li, Zi-Yong
Xu, Zhi
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2018, 55 (06) : 1509 - 1513
[26] Design, Synthesis, and In Vitro Anti-mycobacterial Activities of 1,2,3-Triazole-tetraethylene Glycol Tethered Isatin Dimers
Zhao, Shi-Jia
Lv, Zao-Sheng
Deng, Jia-Lun
Gao, Feng
Zhang, Guang-De
Xu, Zhi
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2018, 55 (12) : 3006 - 3010
[27] Synthesis and in vitro evaluation of novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids for their anti-mycobacterial activities
Yan, Xinjia
Lv, Zaosheng
Wen, Jing
Zhao, Shijia
Xu, Zhi
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 143 : 899 - 904
[28] The synthesis and evaluation of quinolinequinones as anti-mycobacterial agents
Santoso, Kristiana T.
Menorca, Ayana
Cheung, Chen-Yi
Cook, Gregory M.
Stocker, Bridget L.
Timmer, Mattie S. M.
BIOORGANIC & MEDICINAL CHEMISTRY, 2019, 27 (16) : 3532 - 3545
[29] Synthesis and in vitro anti-mycobacterial activity of 5-substituted pyrimidine nucleosides
Johar, M
Manning, T
Kunimoto, DY
Kumar, R
BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (24) : 6663 - 6671
[30] Design, Synthesis and In Vitro Anti-mycobacterial Activities of 8-OMe Ciprofloxacin-1H-1,2,3-triazole-isatin-(thio) Semicarbazide/Oxime Hybrids
Xu, Zhi
Song, Xufeng
Hu, Yuanqiang
Qiang, Min
Lv, Zaosheng
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2018, 55 (01) : 192 - 198

← 1 2 3 4 5 →