Abstract
With the aim of developing potential H1-antihistaminic agents, a series of novel 2-substituted-3-carboxamido-4-oxo-4H-pyrimido[2,1-b][1,3]benzothiazole (8a–g) and 2-substituted-3-carboxamido-8-chloro-4-oxo-4H-pyrimido[2,1-b][1,3]benzothiazole (9a–g) were synthesized and evaluated in vitro for H1-antihistaminic activity on guinea pig ileum preparation. IC50 values of the compounds were found to be in the micromolar range. Chlorpheniramine maleate was used as a standard drug. The active derivatives (8d–8g and 9d–9g) were found to have IC50 values comparable to reference standard chlorpheniramine maleate. The sedative potential of both series (8a–g and 9a–g) is less than the reference drug. Hence, it could serve as prototype molecules for further development as a new class of H1-antihistaminic agents.
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Acknowledgments
The authors are thankful to the Head, the Department of Chemistry, Vinayakrao Patil Mahavidyala Vaijapur-423 701 (M.S.), India for partial support of this study; the Government Medical College, Aurangabad for providing the experimental animals; and the Department of Analytical Chemistry, University of Pune, Pune; and SAIF, Chandigarh University, Chandigarh, India for providing spectra of compounds.
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Gupta, S.V., Baheti, K.G., Ganorkar, S.B. et al. Synthesis and pharmacological investigation of novel 2-substituted-3-carboxamido-4H-pyrimidobenzothiazole derivatives as a new class of H1-antihistaminic agent. Med Chem Res 22, 1065–1072 (2013). https://doi.org/10.1007/s00044-012-0100-4
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DOI: https://doi.org/10.1007/s00044-012-0100-4