Benzothiazole: A Versatile and Multitargeted Pharmacophore in the Field of Medicinal Chemistry

Agarwal, Shikha; Gandhi, Divyani; Kalal, Priyanka

doi:10.2174/1570178614666170707160654

Cited by 31 publications

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“…Benzothiazole (BT) is a privileged bicyclic ring system present in a wide variety of synthetic and natural products. BT and its derivatives play a distinctive role in medicinal chemistry due to their diverse biological activities such as antiprotozoal, antimicrobial, anticancer, antischizophrenia, antihypertensive, antiinflammatory, and antiviral activities [21][22][23][24][25]. Venugopala et al 2013 [26], also screened benzothiazole analogs for their mosquitocidal and repellent properties against Anopheles arabiensis by mosquito feeding-probing assay, cone bio-assay and standard World Health Organization (WHO) larvicidal assay.…”

Section: Introductionmentioning

confidence: 99%

Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents

et al. 2019

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Aedes aegypti is associated with the transmission of numerous human and animal diseases, such as yellow fever, dengue fever, chikungunya, and more recently Zika virus. Emerging insecticide resistance has created a need to develop new mosquitocidal agents for effective control operations. A series of benzothiazole-piperidine derivatives (1-24) were investigated for their larvicidal and adulticidal effects on Ae. aegypti It was observed that compounds 2, 4, 6, 7, 8, 11 and 13 showed notable larvicidal activity. Furthermore, compounds 6 and 10 showed promising adulticidal activity. Based on the mosquitocidal properties of these compounds, docking studies were also carried out in the active site of the AeSCP2 enzyme to explore any insights into further in vitro enzyme studies. Docking results indicated that all these active compounds showed reasonable interactions with critical residues in the active site of this enzyme. This outcome suggested that these compounds might show their larvicidal and adulticidal effects via the inhibition of AeSCP2. According to in vitro and in silico studies, compounds 2, 4, 6, 7, 8, 10, 11 and 13 stand out as candidates for further studies.

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Section: Introductionmentioning

confidence: 99%

Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents

et al. 2019

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“…Benzothiazoles, as a bicyclic heterocycles with fused benzene and thiazole rings containing electron-rich heteroatoms, nitrogen and sulfur, attract great interest from researchers for drug design due to their high biological and pharmacological activity [ 1 , 2 , 3 , 4 , 5 ]. The present review covers the literature from 2015.…”

Section: Introductionmentioning

confidence: 99%

Modern Approaches to the Synthesis and Transformations of Practically Valuable Benzothiazole Derivatives

2021

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The review is devoted to modern trends in the chemistry of 2-amino and 2-mercapto substituted benzothiazoles covering the literature since 2015. The reviewed heterocycles belong to biologically active and industrially demanded compounds. Newly developed synthesis methods can be divided into conventional multistep processes and one-pot, atom economy procedures, realized using green chemistry principles and simple reagents. The easy functionalization of the 2-NH2 and 2-SH groups and the benzene ring of the benzothiazole moiety allows considering them as highly reactive building blocks for organic and organoelement synthesis, including the synthesis of pharmacologically active heterocycles. The review provides a summary of findings, which may be useful for developing new drugs and materials and new synthetic approaches and patterns of reactivity.

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“…Among the heterocyclic compounds, N‐ and S‐bearing scaffolds are of much interest for the researchers [3,4]. One of the prominent heterocyclic moieties, benzothiazole (BT) possesses a thiazole ring, fused with a benzene ring, and serves as a fundamental building block in several organic syntheses and acts as a chief model for the development of numerous therapeutic and potent agents [5–7]. It possesses a plethora of biological and industrial applications, namely antimicrobial [8], anticonvulsant [9], anti‐HIV [10], antidiabetic [11], antiparkinson [12], antiproliferative [13], falciparum inhibitors [14], anti‐leishmanial [15], Mycobacterium tuberculosis shikimate kinase inhibitor [16], polymer chemistry [17], clothing textiles [18], pesticides [19], corrosion inhibitors [20], and so on.…”

Section: Introductionmentioning

confidence: 99%

Urea nitrate–catalyzed C‐N and C‐S bond formation: A mechanochemical approach for 5‐chloro‐2‐arylbenzo[d]thiazole derivatives

Sethiya

Sahiba

Soni

et al. 2021

Journal of Heterocyclic Chem

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A series of substituted 5‐chloro‐2‐arylbenzo[d]thiazoles were synthesized using 4‐chloro‐2‐aminothiophenol and aromatic aldehydes in the presence of urea nitrate as a catalyst using the mechanochemical grindstone technique. This protocol was effectively carried out under metal‐free conditions at room temperature, and the desired products were obtained in high to excellent yields in short reaction time (30–60 s). The structure of all the synthesized derivatives was confirmed by spectral characterization. The designed protocol has several benefits like eco‐friendly, solvent‐free, high yields, easy workup, and recyclability of catalyst. The catalyst was reusable at least four times without significant loss of activity. The good functional group tolerance with a series of derivatives has been demonstrated.

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Benzothiazole: A Versatile and Multitargeted Pharmacophore in the Field of Medicinal Chemistry

Cited by 31 publications

References 0 publications

Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents

Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents

Modern Approaches to the Synthesis and Transformations of Practically Valuable Benzothiazole Derivatives

Urea nitrate–catalyzed C‐N and C‐S bond formation: A mechanochemical approach for 5‐chloro‐2‐arylbenzo[d]thiazole derivatives

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