Benzothiazole
(Synonyms: 苯并噻唑) 目录号 : GC61752Benzothiazole是一种天然的杂环核。Benzothiazole杂环核具有抗癌、抗菌、抗糖尿病、抗炎、抗病毒、抗利什曼等多种生物活性。
Cas No.:95-16-9
Sample solution is provided at 25 µL, 10mM.
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Benzothiazole is a natural occurring heterocyclic nuclei. Benzothiazole nucleus possesses a number of biological activities such as anticancer, antimicrobial, antidiabetic, anti-inflammatory, antiviral, antileishmanial, and antiviral[1].
[1]. Ruhi Ali, et al. Biological Aspects of Emerging Benzothiazoles: A Short Review, Journal of Chemistry, vol. 2013, Article ID 345198, 12 pages, 2013.
Cas No. | 95-16-9 | SDF | |
别名 | 苯并噻唑 | ||
Canonical SMILES | C12=CC=CC=C1SC=N2 | ||
分子式 | C7H5NS | 分子量 | 135.18 |
溶解度 | DMSO: 110 mg/mL (813.73 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 7.3975 mL | 36.9877 mL | 73.9754 mL |
5 mM | 1.4795 mL | 7.3975 mL | 14.7951 mL |
10 mM | 0.7398 mL | 3.6988 mL | 7.3975 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Benzothiazole derivatives as anticancer agents
J Enzyme Inhib Med Chem 2020 Dec;35(1):265-279.PMID:31790602DOI:10.1080/14756366.2019.1698036.
Benzothiazole (BTA) belongs to the heterocyclic class of bicyclic compounds. BTA derivatives possesses broad spectrum biological activities such as anticancer, antioxidant, anti-inflammatory, anti-tumour, antiviral, antibacterial, anti-proliferative, anti-diabetic, anti-convulsant, analgesic, anti-tubercular, antimalarial, anti-leishmanial, anti-histaminic and anti-fungal among others. The BTA scaffolds showed a crucial role in the inhibition of the metalloenzyme carbonic anhydrase (CA). In this review an extensive literature survey over the last decade discloses the role of BTA derivatives mainly as anticancer agents. Such compounds are effective against various types of cancer cell lines through a multitude of mechanisms, some of which are poorly studied or understood. The inhibition of tumour associated CAs by BTA derivatives is on the other hand better investigated and such compounds may serve as anticancer leads for the development of agents effective against hypoxic tumours.
Benzothiazole-based Compounds in Antibacterial Drug Discovery
Curr Med Chem 2018;25(38):5218-5236.PMID:28990510DOI:10.2174/0929867324666171009103327.
Numerous compounds with a Benzothiazole scaffold that have been described in the literature show promising activities against several Gram-positive and Gramnegative bacteria, and also against Mycobacterium tuberculosis. Benzothiazole-based antibacterial compounds bind to different biological targets in bacterial cells and have been shown to be inhibitors of enzymes that are important for essential processes in the bacterial cells, such as cell-wall synthesis, cell division, and DNA replication, or are important for different biosynthetic pathways of essential compounds in bacterial cells, such as the biosynthesis of histidine and biotin. This review focuses on the antibacterial potential of benzothiazole-based compounds, in terms of their specific interactions with targets in bacterial cells. We assess the importance of the Benzothiazole scaffold in the discovery of new antibacterial compounds, the potential of benzothiazole-based compounds against resistant bacterial strains, optimization of their antibacterial activity, and the future perspectives of benzothiazole-based antibacterials.
Advances in 2-substituted Benzothiazole scaffold-based chemotherapeutic agents
Arch Pharm (Weinheim) 2021 Dec;354(12):e2100246.PMID:34467567DOI:10.1002/ardp.202100246.
Targeted therapy plays a pivotal role in cancer therapeutics by countering the drawbacks of conventional treatment like adverse events and drug resistance. Over the last decade, heterocyclic derivatives have received considerable attention as cytotoxic agents by modulating various signaling pathways. Benzothiazole is an important heterocyclic scaffold that has been explored for its therapeutic potential. Benzothiazole-based derivatives have emerged as potent inhibitors of enzymes such as EGFR, VEGFR, PI3K, topoisomerases, and thymidylate kinases. Several researchers have designed, synthesized, and evaluated Benzothiazole scaffold-based enzyme inhibitors. Of these, several inhibitors have entered various phases of clinical trials. This review describes the recent advances and developments of Benzothiazole architecture-based derivatives as potent anticancer agents.
Review on the Developments of Benzothiazole-containing Antimicrobial Agents
Curr Top Med Chem 2022;22(32):2630-2659.PMID:36503470DOI:10.2174/1568026623666221207161752.
The infectious diseases caused by bacterial resistance to antibiotics constitute an increasing threat to human health on a global scale. An increasing number of infections, including tuberculosis, pneumonia, salmonellosis and gonorrhea, are becoming progressively challenging to cure owing to the ineffectiveness of current clinically used antibiotics and presents a serious health threat worldwide in medical community. The major concern of this global health threat is the ability of microorganisms to develop one or several mechanisms of resistance to antibiotics, making them inefficient to therapeutic treatment. The quest for discovering novel scaffold with antimicrobial property is particularly in great need to face future challenges in hospital and healthcare settings. Hence, the development of benzothiazoles is of considerable interest to medicinal chemists. Benzothiazole, being part of an important class of heterocyclic scaffold retains a wide spectrum of various attractive pharmacological activities. Antibiotic resistance represents an increasing burden comprising medical cost, hospital stay and mortality. Several derivatives containing a Benzothiazole scaffold, reported in the literature, were found to display remarkable potencies towards diverse Grampositive and Gram-negative bacterial pathogens. The principal focus concerns the antibacterial potential of benzothiazole-based derivatives as antimicrobial agents interacting with targets in bacterial pathogens. In this review, we also disclose the significance of the Benzothiazole moiety in the discovery of new antibacterial compounds, the potential of benzothiazole-based derivatives in the case of resistant bacterial strains, optimization of their antibacterial activity, and their future perspectives. The structure-activity relationship study and the mode of action of the title derivatives are highlighted too.
Advancement in Pharmacological Activities of Benzothiazole and its Derivatives: An Up to Date Review
Mini Rev Med Chem 2021;21(3):314-335.PMID:32819243DOI:10.2174/1389557520666200820133252.
Benzothiazole is a heterocyclic aromatic and bicyclic compound in which, benzene ring is attached with thiazole ring. This nucleus is established in marine as well as terrestrial natural compounds. The Benzothiazole skeleton is established in a broad variety of bioactive heterocycles and natural products. The Benzothiazole nucleus is considered as the principle moiety in several biologically active compounds. Over the decade, chemists are paying more attention towards the revision of the biological and therapeutic activities such as antimicrobial, analgesic, antiinflammatory, antitubercular, antiviral and antioxidant of Benzothiazole containing compounds. The molecular structures of a number of potent drugs including Frentizole, Pramipexole, Thioflavin T and Riluzole etc., are based on Benzothiazole skeleton. The present work is the compilation and presentation of all available information in a systematic manner with an aim to present the findings in a way, which may be beneficial for future research.