Synthesis and antiviral activity of novel imidazo[2,1-b]thiazoles coupled with morpholine and thiomorpholines |
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| Authors: | Nagaraju Chirra Varshitha Shanigarapu Naga Pranathi Abburi Ekaterina O. Sinegubova Ravi Kumar Pedapati Yana L. Esaulkova Vladimir V. Zarubaev Srinivas Kantevari |
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| Affiliation: | 1. Fluoro and Agrochemicals Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, India;2. Pasteur Institute of Epidemiology and Microbiology, St. Petersburg, Russia;3. Fluoro and Agrochemicals Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India |
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| Abstract: | Herein described the synthesis and antiviral evaluation of a novel series of morpholine and thio-morpholine coupled imidazo[2,1-b]thiazoles. The three-step reaction sequence involving the condensation of 1,3-dichloroacetone with thiourea followed by coupling with morpholine and thiomorpholine and finally cyclization with substituted α-bromoacetophenones yielded the desired imidazothiazoles 7(a–l) . Screening of all the new compounds for their in vitro antiviral activity against influenza virus A/Puerto Rico/8/34 (H1N1) in MDCK cells, resulted in two potent analogs, 7d (IC50: 1.1 μM, C50: >300 μM, SI = 273) and 7e (IC50: 2.0 μM, C50: >300 μM, SI = 150), with a favorable toxicity profile and are the best anti-influenza hit analogs for further structural optimization. |
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