Medicinal significance of benzothiazole scaffold: an insight view

Sharma, Prabodh Chander; Sinhmar, Alka; Sharma, Archana; Rajak, Harish; Pathak, Dharam Pal

doi:10.3109/14756366.2012.720572

Cited by 203 publications

(96 citation statements)

References 138 publications

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“…[2,3] Their derivatives display a broad spectrum of different biological features such as anticancer, antiviral, antibacterial, antifungal, antiinflammatory etc. [4][5][6] In our research group we have published several publications regarding antiproliferative and antitumor activity of versatile benzimidazole and benzothiazole derivatives bearing different amidino supstituents. [7,8] Among all amidino substituted benzazole derivatives, the ones with the cyclic amidino substituent, namely 2-imidazolinyl group, showed the most significant antiproliferative activity in vitro with IC50 values in submicromolar range of concentrations.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antioxidative Potency of Novel Amidino Substituted Benzimidazole and Benzothiazole Derivatives

Racané¹,

Cindrić²,

Perin³

et al. 2017

Croat. Chem. Acta

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Herein we present the synthesis of versatile amidino substituted benzothiazole 3-10 and benzimidazole 12-19 derivatives substituted with the variable number of hydroxy and methoxy groups. Furthermore, the synthesized compounds were explored for their antioxidative activity in vitro by using three biological assays, namely DPPH, ABTS and FRAP. The obtained results indicated that the variable number of hydroxy groups together with the type of the amidino substituent strongly influenced the antioxidative activity and reducing power of tested compounds. The most promising antioxidative activity showed trihydroxy substituted compounds 6, 10, 15 and 19. In general, it was noticed that unsubstituted amidino group induced the more pronounced activity in comparison to derivatives bearing 2-imidazolinyl group.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Antioxidative Potency of Novel Amidino Substituted Benzimidazole and Benzothiazole Derivatives

Racané¹,

Cindrić²,

Perin³

et al. 2017

Croat. Chem. Acta

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“…Several successful clinical drugs such as ethoxzolomide (1), frentizole (2), riluzole (3), zopolrestat (4) and so on and the well-known amyloid imaging agent thioflavin T (5) contain benzothiazole nucleus (Figure 1) [16]. These drugs have applications in the treatment of various diseases/disorders, which are outcome of impaired physiological processes in humans.…”

Section: Introductionmentioning

confidence: 99%

Therapeutic potential of benzothiazoles: a patent review (2010 – 2014)

Kamal

Syed

Mohammed

2015

Expert Opinion on Therapeutic Patents

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Several molecules containing benzothiazole skeleton are agents of choice for the treatment of various human diseases/disorders. Its versatile character of being capable of serving as ligand to various biomolecules attracted the interest of medicinal chemists for the development of therapies for respective ailments, especially, the 2-arylbenzothiazole moiety which is under development for the treatment of cancer. This signifies the increasing importance of benzothiazole nucleus in the area of drug discovery. Its structural simplicity and ease of synthesis provides scope for the development of chemical libraries that could serve in the discovery of new chemical entities progressing towards the market.

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“…The most prominent members of this group are aspirin (5), ibuprofen (6), naproxen (7), diclofenac (8), and indomethacin (9). Most NSAIDs inhibit the activity of cyclooxygenase-1 and cyclooxygenase-2 and thereby the synthesis of prostaglandins and thromboxanes.…”

Section: Introductionmentioning

confidence: 99%

“…Most of the known derivatives of benzothiazole results from substitution at the methyne centre in the thiazole ring (2). Riluzole (3) used in treatment of amyotrophic lateral sclerosis 2 and pramipexole (4), a dopamine agonist used in the treatment of Parkinson's disease 3 , sexual dysfunction 4 , bipolar disorder 5 , clinical depression 6 are good examples of benzothiazoles that aroused interest in further research into the pharmacological applications of benzothiazole derivatives.…”

Section: Introductionmentioning

confidence: 99%

Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies

Ugwu

Okoro

Ukoha

et al. 2018

Journal of Enzyme Inhibition and Medicinal Chemistry

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Twelve new derivatives of benzothiazole bearing benzenesulphonamide and carboxamide were synthesised and investigated for their in vivo anti-inflammatory, analgesic and ulcerogenic activities. Molecular docking showed an excellent binding interaction of the synthesised compounds with the receptors, with 17c showing the highest binding energy (-12.50 kcal/mol). Compounds 17c and 17i inhibited carrageenan-induced rat paw oedema at 72, 76, and 80% and 64, 73, and 78% at 1 h, 2 h, and 3 h, respectively. In the analgesic activity experiment, compounds 17c, 17 g, and 17i had ED 50 (mM/kg) of 96, 127, and 84 after 0.5 h; 102, 134, and 72 after 1 h and 89, 156, and 69 mM/kg after 2 h, respectively, which were comparable with 156, 72, and 70 mM/kg for celecoxib. The ulcerogenic index of the most active derivatives 17c and 17i were 0.82 and 0.89, respectively, comparable to 0.92 for celecoxib. The physicochemical studies of the new derivatives showed that they will not have oral bioavailability problems. ARTICLE HISTORY

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Medicinal significance of benzothiazole scaffold: an insight view

Cited by 203 publications

References 138 publications

Synthesis and Antioxidative Potency of Novel Amidino Substituted Benzimidazole and Benzothiazole Derivatives

Synthesis and Antioxidative Potency of Novel Amidino Substituted Benzimidazole and Benzothiazole Derivatives

Therapeutic potential of benzothiazoles: a patent review (2010 – 2014)

Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies

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