4-(4-Bromophenyl)-thiazol-2-amine derivatives: synthesis, biological activity and molecular docking study with ADME profile

被引：29

作者：

Sharma, Deepika ^{[1
]}

Kumar, Sanjiv ^{[1
]}

Narasimhan, Balasubramanian ^{[1
]}

Ramasamy, Kalavathy ^{[2
,3
]}

Lim, Siong Meng ^{[2
,3
]}

Shah, Syed Adnan Ali ^{[2
,4
]}

Mani, Vasudevan ^{[5
]}

机构：

[1] Maharshi Dayanand Univ, Fac Pharmaceut Sci, Rohtak 124001, Haryana, India

[2] Univ Teknol MARA UiTM, Fac Pharm, Bandar Puncak Alam 42300, Selangor Darul, Malaysia

[3] Univ Teknol MARA UiTM, Pharmaceut Life Sci Community Res, Collaborat Drug Discovery Res CDDR Grp, Shah Alam 40450, Selangor Darul, Malaysia

[4] Univ Teknol MARA, Atta ur Rahman Inst Nat Prod Discovery AuRIns, Bandar Puncak Alam 42300, Selangor Darul, Malaysia

[5] Qassim Univ, Coll Pharm, Dept Pharmacol & Toxicol, Buraydah 51452, Saudi Arabia

来源：

BMC CHEMISTRY | 2019年 / 13卷

关键词：

Synthesis; Molecular docking; Thiazole derivatives; Antimicrobial; Anticancer; SCHIFF-BASES; ANTIBACTERIAL; DESIGN;

D O I：

10.1186/s13065-019-0575-x

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In order to overcome the challenges of microbial resistance as well as to improve the effectiveness and selectivity of chemotherapeutic agents against cancer, a novel series of 4-(4-bromophenyl)-thiazol-2-amine derivatives was synthesized and its molecular structures were confirmed by physicochemical and spectral characteristics. The synthesized compounds were further evaluated for their in vitro antimicrobial activity using turbidimetric method and anticancer activity against oestrogen receptor positive human breast adenocarcinoma cancer cell line (MCF7) by Sulforhodamine B (SRB) assay. The antimicrobial activity results revealed that compound p2, p3, p4 and p6 exhibited promising antimicrobial activity that are comparable to standard norfloxacin (antibacterial) and fluconazole (antifungal). Anticancer screening results demonstrated that compound p2 was found to be the most active one against cancer cell line when compared to the rest of the compounds and comparable to the standard drug (5-fluorouracil). The molecular docking study demonstrated that compounds, p2, p3, p4 and p6 displayed good docking score within binding pocket of the selected PDB ID (1JIJ, 4WMZ and 3ERT) and showed promising ADME properties.

引用

页数：16

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