Volume : 13, Issue : 08, August – 2026

Title:

BENZOTHIAZOLE A PRIVILEGED HETEROCYCLIC SCAFFOLD IN MEDICINAL CHEMISTRY

Authors :

Likhit kumar J Punjali, Anusha P. Shalavadi, Tabasum Killedar*, Sadhya D C, V H. Kulkarni, S D. Joshi

Abstract :

Benzothiazole is a privileged sulphur and nitrogen containing heterocyclic scaffold that has attracted considerable attention in medicinal chemistry owing to its structural diversity, ease of functionalization, and broad spectrum of biological activities. The unique physicochemical properties of the benzothiazole nucleus enable the development of structurally diverse derivatives with significant therapeutic potential. This review provides a comprehensive overview of the chemistry of benzothiazole, including its structural features, aromatic characteristics, and commonly employed synthetic strategies for the preparation of biologically active derivatives. Particular emphasis is placed on the recent advances in the pharmacological applications of benzothiazole derivatives, highlighting their antitubercular, anticancer, antifungal, anti-inflammatory, antidiabetic, anticonvulsant, antioxidant, antimalarial, and antidepressant activities, together with representative lead compounds and their biological significance. In addition, clinically approved drugs containing the benzothiazole scaffold are discussed to demonstrate the successful translation of this pharmacophore into therapeutic agents. Overall, this review highlights the versatility of the benzothiazole nucleus as a valuable platform for rational drug design and underscores its continuing importance in the discovery and development of next-generation pharmaceuticals.
Keywords: Benzothiazole, Medicinal Chemistry, Heterocyclic Scaffold, Pharmacological Activities, Drug Discovery.

Cite This Article:

Please cite this article in press Tabasum Killedar et al., Benzothiazole A Privileged Heterocyclic Scaffold In Medicinal Chemistry. Indo Am. J. P. Sci, 2026; 13(08).

REFERENCES:

[1] Chemica AA-M-DP, 2017 undefined. A review: biological importance of heterocyclic compounds. Res Al-MullaDer Pharma Chem 2017•researchgate.net 2017; 9: 141–147.
[2] Prajapati NP, Vekariya RH, Borad MA, et al. Recent advances in the synthesis of 2-substituted benzothiazoles: A review. 2014. Epub ahead of print 2014.
[3] Zhu XY, Etukala JR, Eyunni VK, et al. Benzothiazoles as probes for the 5HT 1A receptor and the serotonin transporter (SERT): A search for new dual-acting agents as potential antidepressants.
[4] Irfan A, Batool F, Zahra Naqvi SA, et al. Benzothiazole derivatives as anticancer agents. J Enzyme Inhib Med Chem 2020; 35: 265–279.
[5] Weekes AA, Dix MC, Bagley MC, et al. Rapid and convenient thermal or microwave-assisted synthesis of substituted 2-phenylbenzothiazoles. Synth Commun 2010; 40: 3027–3032.
[6] Londhe BS, Pratap UR, Mali JR, et al. Synthesis of 2-arylbenzothiazoles catalyzed by biomimetic catalyst, β-Cyclodextrin. Bull Korean Chem Soc 2010; 31: 2329–2332.
[7] Nalage S V., Bhosale S V., Bhosale DS, et al. P2O5 mediated rapid condensation of 2-aminothiophenol with aromatic aldehydes at ambient temperature. Chinese Chem Lett 2010; 21: 790–793.
[8] Maleki B, Salehabadi H, Moghaddam MK. Room-temperature synthesis of 2-arylbenzothiazoles using sulfuric acid immobilized on silica as a reusable catalyst under heterogeneous condition. Acta Chim Slov 2010; 57: 741–745.
[9] Rostami A, Yari A. Sulfamic acid as a recyclable and green catalyst for rapid and highly efficient synthesis of 2-arylbenzothiazoles in water at room temperature. J Iran Chem Soc 2012; 9: 489–493.
[10] Sarkar S. Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring. Istanbul J Pharm 2019; 48: 28–31.
[11] Hemeda LR, El Hassab MA, Abdelgawad MA, et al. Discovery of pyrimidine-tethered benzothiazole derivatives as novel anti-tubercular agents towards multi- and extensively drug resistant Mycobacterium tuberculosis. J Enzyme Inhib Med Chem; 38. Epub ahead of print 2023.
[12] Saha P, Sau S, Kalia NP, et al. Antitubercular activity of 2-mercaptobenzothiazole derivatives targeting Mycobacterium tuberculosis type II NADH dehydrogenase. RSC Med Chem 2024; 15: 1664–1674.
[13] Osmaniye D, Levent S, Karaduman AB, et al. Synthesis of new benzothiazole acylhydrazones as anticancer agents. Molecules 2018; 23: 1–14.
[14] Paengsri W, Baramee A. Synthesis and evaluation of anti-tuberculosis and anti-cancer activities of hydroxynaphthoquinone derivatives. Chiang Mai J Sci 2013; 40: 70–76.
[15] Yadav S, Lim SM, Ramasamy K, et al. Synthesis and evaluation of antimicrobial, antitubercular and anticancer activities of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamides. Chem Cent J 2018; 12: 1–14.
[16] Çapan G, Ulusoy N, Ergenç N, et al. New 6-phenylimidazo[2,1-b]thiazole derivatives: Synthesis and antifungal activity. Monatshefte fur Chemie 1999; 130: 1399–1407.
[17] Liu Y, Wang Y, Dong G, et al. Novel benzothiazole derivatives with a broad antifungal spectrum: Design, synthesis and structure-activity relationships. Medchemcomm 2013; 4: 1551–1561.
[18] Luo B, Li D, Zhang AL, et al. Synthesis, antifungal activities and molecular docking studies of benzoxazole and benzothiazole derivatives. Molecules; 23. Epub ahead of print 2018.
[19] Ugwu DI, Okoro UC, Ukoha PO, et al. Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies. J Enzyme Inhib Med Chem 2018; 33: 405–415.
[20] Khan A, Qazi NG, Alvi AM, et al. Synthesis of new benzothiazole derivatives with in-depth In-vitro, In-vivo anti-oxidant, anti-inflammatory and anti-ulcer activities. PLoS One 2026; 21: e0337639.
[21] Sadhasivam G, Kulanthai K. Synthesis, characterization, and evaluation of anti-inflammatory and anti-diabetic activity of new benzothiazole derivatives. J Chem Pharm Res 2015; 7: 425–431.
[22] Kumar S, Rathore DS, Garg G, et al. Synthesis and Evaluation of Some Benzothiazole Derivatives As Antidiabetic Agents. Int J Pharm Pharm Sci 2017; 9: 60.
[23] Hassan MZ, Khan SA, Amir M. Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. Eur J Med Chem 2012; 58: 206–213.
[24] Malik S, Bahare RS, Khan SA. Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2- ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: A hybrid pharmacophore approach. Eur J Med Chem 2013; 67: 1–13.
[25] Ugale VG, Patel HM, Wadodkar SG, et al. Quinazolino-benzothiazoles: Fused pharmacophores as anticonvulsant agents. Eur J Med Chem 2012; 53: 107–113.
[26] Yadav AG, Patil VN, Asrondkar AL, et al. Anti-Oxidant and Anti-Microbial Activities of Pyrazolyl-Benzothiazole Derivatives Using Vilsmeier-Haack Reaction. Rasayan JChem 2012; 5: 117–120.
[27] Koppireddi S, Komsani JR, Avula S, et al. Novel 2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetamides as antioxidant and/or anti-inflammatory compounds. Eur J Med Chem 2013; 66: 305–313.
[28] Suresh1* C, Rao1 JV, Jayaveera2 KN, et al. Synthesis of 2-Hydrazino Benzothaizoles-2-Amino-(4-Substituted)- Acetanilides for Anti Oxidant Activity. Int J Pharm Biol Sci (e-ISSN 2230-7605) 2011; 1: 409–413.
[29] Ongarora DSB, Gut J, Rosenthal PJ, et al. Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: Synthesis and pharmacological evaluation. Bioorganic Med Chem Lett 2012; 22: 5046–5050.
[30] Ge JF, Zhang QQ, Lu JM, et al. Synthesis of cyanine dyes and investigation of their in vitro antiprotozoal activities. Medchemcomm 2012; 3: 1435–1442.

Volume : 13, Issue : 08, August – 2026

Title:

EVALUATION OF ANTIHYPERLIPIDEMIC ACTIVITY OF SAPINDUS EMARGINATUS IN RATS

Authors :

Chinthala Jamima*, Dr.R.narasimha Rao, Dr.N. Raghunandhan

Abstract :

Obesity and hyperlipidemia have become major disorders predominantly causing prevailing cardiovascular diseases and ultimately death. The prolonged use of anti-obesity drugs and statins for reducing obesity and blood lipid levels is leading toward adverse effects of kidneys and muscles, specifically rhabdomyolysis. The objective of this study is to evaluate potential of seeds of Sapindus emarginatus against hyperlipidemia. In this model of Hyperlipidemia, 30 adult male wistar rats (200-250gms) were evenly divided into 5 groups in both groups. Group-1 and Group-2 served as untreated and model controls respectively, while Group-3, 4 and 5 were the treatments groups which were simultaneously treated with standard, 100 and 200 mg/kg extract respectively along with High Fat Diet. On last day, blood samples for biochemical parameters, were obtained under inhaled diether anaesthesia. The outcomes of this study were expressed as mean standard error and data were evaluated by using analysis of variance followed by multiple comparisons. Oral administration of 100 mg/ kg and 200mg/kg body weight of Methanolic extract residual fraction of Moringa oleifera. Leaves exhibited a significant reduction (P < 0.01) in serum lipid parameters such as triglycerides, total cholesterol, low density lipoprotein (LDL), very LDL and increase in high density lipoprotein in hyperlipidemic rats when compared with hyperlipidemic control in both models. Our results demonstrated that Methanolic extract fraction of Sesbania grandiflora. Possessed significant antihyperlipidemic activity.
Keywords: Sesbania grandiflora, Cholesterol, LDL, triglycerides and antihyperlipidemic activity.

Cite This Article:

Please cite this article in press Chinthala Jamimaet al., Evaluation of Antihyperlipidemic activity of Sapindus Emarginatus in rats,, Indo Am. J. P. Sci, 2026; 13(08).

REFERENCES:

1. Amit G, Vandana S, Sidharth M. HYPERLIPIDEMIA: An Updated Review. Inter J of Biopharma & Toxicol Res 2011;1:81-89.
2. Virchow RP, Thrombose IG. In Gesammelte Abhandlungen zur Wissenschaftlichen Medicin. Frankfurt-am-Main, Meidinger Sohn & Company 1856, S 458-564.
3. Ankur rohilla, Nidhi Dagar, Seema Rohilla, Amarjeet Dahiya, Ashok Kushnoor. HYPERLIPIDEMIA- a deadly pathological condition. Inter J Curr Pharma Res 2012;4:15-18
4. Ross R, Glomset JA. The pathogenesis of atherosclerosis. N Engl J Med 1976;295:369-77.
5. Grundy SM, Vega GL. Hypertriglyceridemia: causes and relation to coronary heart disease – Semin. Thromb. Hemost 1988;14:249-64.
6. Dargel R. Lipoproteins and the etiopathogenesis of atherosclerosis. Zentralbl Allg Pathol 1989; 135: 501-504.