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

Abstract

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.

The medicinal chemistry of piperazines: A review

“…Various heterocyclic analogs of piperazine are synthesized and modified towards anticancer activity that acts against different cell lines such as MDA‐MB‐435, and HCT‐8, HL‐60, etc. (Yadav et al., 2023). Singh et al.…”

“…Various heterocyclic analogs of piperazine are synthesized and modified towards anticancer activity that acts against different cell lines such as MDA-MB-435, and HCT-8, HL-60, etc. (Yadav et al, 2023). Singh et al reported a synthesis of two groups of piperazine salicylanilide derivatives 4-(3-(4-ethylpiperazin-1-yl)propoxy)-N-phenyl benzamide (77) and (4-(3-(4-ethylpiperazin-1-yl) propoxy) phenyl) (4-phenylpiperazin-1-yl) methanone (78).…”

“…Various compounds containing piperazine moiety are found to have good antiviral activity which can be used against various viruses such as HAdV7, HSV-1, HAVHM17, TMV, etc. (Yadav et al, 2023).…”

COX inhibitory profiles of a series of thiadiazole-benzothiazole hybrids

“…The benzothiazole core serves as a privileged building block of small molecule ligands endowed with a broad range of biological activities such as anti-inflammatory activity targeting a plethora of crucial enzymes including COXs [21][22][23][24][25][26][27][28].…”

Synthesis, biological evaluation and mechanism of action of benzothiazole derivatives with aromatic hydrazone moiety, a new class of antileishmanial compounds

“…The strategy of researching novel drug candidates with new mechanisms of action are also objective of our studies, and in recent years the benzothiazole nucleus has received much attention by the scientific community. Benzothiazole is a bicyclic heterocyclic compound, presenting a benzene ring fused to a five-membered ring comprising nitrogen and sulfur atoms, named thiazole (Singh et al, 2023;Yadav et al, 2023). This moiety is associated to a wide spectrum of biological activities, including antitubercular (Pinheiro et al, 2019), antibacterial (Kashyap et al, 2023), antiinflamatory (Sluter et al, 2023), anticonvulsant (Kyllo et al, 2023), antimalarial (Okonkwo et al, 2023), anthelmintic (Swaroopa et al, 2022), antileishmanial (Lasing et al, 2020), antidiabetic (Kousaxidis et al, 2023), antidepressant (Liu et al, 2022), and antitumor agents (Huang et al, 2023).…”