The immunomodulation potential of the synthetic derivatives of benzothiazoles: Implications in immune system disorders through in vitro and in silico studies

[Display omitted] •Benzothiazole derivatives were synthesized.•Effects in immune system disorders (in vitro studies) were evaluated.•New immunomodulatory agents were identified.•Structure–activity relationship was established.•In silico studies were performed. Benzothiazole and its natural or synthe...

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Veröffentlicht in:Bioorganic chemistry 2016-02, Vol.64, p.21-28
Hauptverfasser: Khan, Khalid Mohammed, Mesaik, Mohammad A., Abdalla, Omer M., Rahim, Fazal, Soomro, Samreen, Halim, Sobia A., Mustafa, Ghulam, Ambreen, Nida, Khalid, Ahmad Shukralla, Taha, Muhammad, Perveen, Shahnaz, Alam, Muhammad Tanveer, Hameed, Abdul, Ul-Haq, Zaheer, Ullah, Hayat, Rehman, Zia Ur, Siddiqui, Rafat Ali, Voelter, Wolfgang
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Sprache:eng
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Zusammenfassung:[Display omitted] •Benzothiazole derivatives were synthesized.•Effects in immune system disorders (in vitro studies) were evaluated.•New immunomodulatory agents were identified.•Structure–activity relationship was established.•In silico studies were performed. Benzothiazole and its natural or synthetic derivatives have been used as precursors for several pharmacological agents for neuroprotective, anti-bacterial, and anti-allergic activities. The objecctive of the present study was to evaluate effects of benzothiazole analogs (compounds 1–26) for their immunomodulatory activities. Eight compounds (2, 4, 5, 8–10, 12, and 18) showed potent inhibitory activity on PHA-activated peripheral blood mononuclear cells (PBMCs) with IC50 ranging from 3.7 to 11.9μM compared to that of the standard drug, prednisolone
ISSN:0045-2068
1090-2120
DOI:10.1016/j.bioorg.2015.11.004