Synthesis, Characterization, and Biological Evaluation of Some Novel Pyrazolo[5,1-b]thiazole Derivatives as Potential Antimicrobial and Anticancer Agents

Abstract

The pharmacological activities of thiazole and pyrazole moieties as antimicrobial and anticancer agents have been thoroughly described in many literature reviews. In this study, a convenient synthesis of novel pyrazolo[5,1-b]thiazole-based heterocycles was carried out. The synthesized compounds were characterized by IR, 1H and 13C NMR spectroscopy and mass spectrometry. Some selected examples were screened and evaluated for their antimicrobial and anticancer activities and showed promising results. These products could serve as leading compounds in the future design of new drug molecules.

Recent Advances in the Development of Pyrazole Derivatives as Anticancer Agents

“…Alsayari et al synthesized new pyrazolo[5,1-b]thiazole-based heterocycles and evaluated their in vitro inhibition against HepG2 hepatocellular carcinoma and HCT116 colon carcinoma cell lines using the MTT assay [ 136 ]. Compound 126 ( Figure 13 for structures of compounds 126 – 139 ) displayed that the best IC 50 values were 6.9 and 13.6 µg/mL against both cell lines.…”

تشييد وتشخيص بعض المشتقات البايرازول ، ترايازول ، اوكسادايازول ، ثايازول ، ثايادايازول الحاملة لبارا- تلوين سلفونامايد الجديدة

“…Hydrazide derivatives are considered to be important compounds that have an important role in organic and medical chemistry, where they attract a big interest by researchers through the past years because of their effective biological activities, including antimicrobials 1 , anticancer 2 , anti-tuberculosis 3 , antivirals 4 , anti HIV 5 , antifungals 6 , antimalarial 7 , and anti-inflammatory 8 .…”

Design, Synthesis, Characterization and Computational Studies of Mannich Bases Oxadiazole Derivatives as New Class of Jack Bean Urease Inhibitors

“…[30][31][32][33][34][35] It is documented that some of the 1,3,4 oxadiazoles derived Mannich bases decrease inflammation and prevent fungal growth and they also possess analgesic, antiulcer, antibacterial, anti-HIV, anti-convulsant, anti-tuberculosis and anticancer activities and as inhibitors of various other enzymes and are used in many other applications. [36][37][38][39] The broad therapeutic applications of oxadiazoles and Mannich bases have prompted us to synthesize Mannich bases of 1,3,4-oxadiazole-2-thiones and evaluate their antiurease activity. The data shows that Mannich bases of 1,3,4-oxadiazole-2-thiones are strong inhibitors of the urease enzyme and suggest further studies on more derivatives.…”

“…The bacterial ureases can also be inhibited by the five‐membered heterocycles like 1,2,4 triazoles and 1,3,4 oxadiazoles [30–35] . It is documented that some of the 1,3,4 oxadiazoles derived Mannich bases decrease inflammation and prevent fungal growth and they also possess analgesic, antiulcer, antibacterial, anti‐HIV, anti‐convulsant, anti‐tuberculosis and anticancer activities and as inhibitors of various other enzymes and are used in many other applications [36–39] . The broad therapeutic applications of oxadiazoles and Mannich bases have prompted us to synthesize Mannich bases of 1,3,4‐oxadiazole‐2‐thiones and evaluate their antiurease activity.…”