Benzothiazole: Synthetic Strategies, Biological Potential, and Interactions
with Targets

Benzothiazole is a bicyclic heterocyclic compound that contains benzene fused with 1, 3-thiazole ring. Several researches established the potential of benzothiazoles as important moiety in various adverse pharmacological conditions. Benzothiazole and its derivatives have been in use and marketed as anti-microbial, anti-inflammatory, anti-diabetic, anti-oxidant, anti-convulsant, anti-tumor, etc. The variations in pharmacological potentials of the benzothiazole and its derivatives have been in rational with their chemical structure. Nowadays, hybridization of two or more pharmacophore to synthesize a single molecule with potent pharmacological action is used. This helps to synergize pharmacological properties, make interaction possible with many targets, or minimize the adverse effects associated with them. Several synthetic approaches have been reported for benzothiazole and its derivatives. In this present review, we focused on recently adopted synthetic approaches for the synthesis of the benzothiazole nucleus and its derivatives. The structure-activity relationship in relation with different pharmacological activities has also been highlighted to provide a good understanding to the researchers for future research on benzothiazoles.

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Recent Insights on Synthetic Methods and Pharmacological Potential in Relation with Structure of Benzothiazoles

Yadav

Kumar

Singh

et al. 2023

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Design, Synthesis and Biological Activities of (Thio)Urea Benzothiazole Derivatives

Mendieta-Wejebe

Rosales‐Hernández

Padilla‐Martínez

et al. 2023

IJMS

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(Thio)ureas ((T)Us) and benzothiazoles (BTs) each have demonstrated to have a great variety of biological activities. When these groups come together, the 2-(thio)ureabenzothizoles [(T)UBTs] are formed, improving the physicochemical as well as the biological properties, making these compounds very interesting in medicinal chemistry. Frentizole, bentaluron and methabenzthiazuron are examples of UBTs used for treatment of rheumatoid arthritis and as wood preservatives and herbicides in winter corn crops, respectively. With this antecedent, we recently reported a bibliographic review about the synthesis of this class of compounds, from the reaction of substituted 2-aminobenzothiazoles (ABTs) with iso(thio)cyanates, (thio)phosgenes, (thio)carbamoyl chlorides, 1,1’-(thio)carbonyldiimidazoles, and carbon disulfide. Herein, we prepared a bibliographic review about those features of design, chemical synthesis, and biological activities relating to (T)UBTs as potential therapeutic agents. This review is about synthetic methodologies generated from 1968 to the present day, highlighting the focus to transform (T)UBTs to compounds containing a range substituents, as illustrated with 37 schemes and 11 figures and concluded with 148 references. In this topic, the scientists dedicated to medicinal chemistry and pharmaceutical industry will find useful information for the design and synthesis of this interesting group of compounds with the aim of repurposing these compounds.

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Synthesis and Biological Importance of 2-(thio)ureabenzothiazoles

et al. 2022

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The (thio)urea and benzothiazole (BT) derivatives have been shown to have a broad spectrum of biological activities. These groups, when bonded, result in the 2-(thio)ureabenzothizoles (TBT and UBT), which could favor the physicochemical and biological properties. UBTs and TBTs are compounds of great importance in medicinal chemistry. For instance, Frentizole is a UBT derivative used for the treatment of rheumatoid arthritis and systemic lupus erythematosus. The UBTs Bentaluron and Bethabenthiazuron are commercial fungicides used as wood preservatives and herbicides in winter corn crops. On these bases, we prepared this bibliography review, which covers chemical aspects of UBTs and TBTs as potential therapeutic agents as well as their studies on the mechanisms of a variety of pharmacological activities. This work covers synthetic methodologies from 1935 to nowadays, highlighting the most recent approaches to afford UBTs and TBTs with a variety of substituents as illustrated in 42 schemes and 13 figures and concluded with 187 references. In addition, this interesting review is designed on chemical reactions of 2-aminobenzothiazoles (2ABTs) with (thio)phosgenes, iso(thio)cyanates, 1,1′-(thio)carbonyldiimidazoles [(T)CDI]s, (thio)carbamoyl chlorides, and carbon disulfide. This topic will provide information of utility for medicinal chemists dedicated to the design and synthesis of this class of compounds to be tested with respect to their biological activities and be proposed as new pharmacophores.

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Benzothiazole: Synthetic Strategies, Biological Potential, and Interactions with Targets

Cited by 4 publications

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Recent Insights on Synthetic Methods and Pharmacological Potential in Relation with Structure of Benzothiazoles

Recent Insights on Synthetic Methods and Pharmacological Potential in Relation with Structure of Benzothiazoles

Design, Synthesis and Biological Activities of (Thio)Urea Benzothiazole Derivatives

Synthesis and Biological Importance of 2-(thio)ureabenzothiazoles

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