The imidazole derivatives are nitrogen-containing heterocyclic rings and produce significant various pharmacological activity like anticancer, antitubercular, antifungal, anti-inflammatory, antiviral, antidepressant, antileishmanial activity and many more. The present study was planned to synthesize novel imidazoles and assess them as their anticancer and anthelmintic activity. To make an equivalent Schiff's base, sulfanilamide was first condensed with heteryl aldehydes. Using silica gel as a solid support, the Schiff's base was further treated with NH4OAC and acetylated/benzoylated isatin, yielding matching imidazoles. A comparison of the created microwave approach with the conventional method is discussed in this work. The physical and analytical data of synthesized compounds were studied, and were evaluated for their anticancer and anthelmintic activity. The findings demonstrated significant anticancer and anthelmintic activity of novel synthesized imidazoles compounds (1b – 8b). The synthesized imidazoles possessed significant cytotoxic activity against Hep-2 cell line. The findings suggested the microwave method was more appropriate for the synthesis of imidazoles compounds (1b – 8b).
Design and synthesis of 7-substituted-2-pyrimidinyl chromen-4-one derivatives as selective Cyclooxygenase-2 inhibitors (1) Method: The compounds were designed using molecular hybridization technique, docking studies was performed using Autodock Vina, compounds having higher affinity than celecoxib were selected and synthesized followed by spectral characterization. The synthesized derivatives (1a, 1b, 2-9) were subjected to ADMET and PASS prediction studies. In vitro antioxidant potential was assayed by DPPH method and in vitro anti-inflammatory activity was assessed by protein denaturation method. (2)Result: Compounds under study have been found to exhibit good to moderate anti-inflammatory activity. Among these, compounds 1a, 1b and 4 exhibited maximum anti-inflammatory activity which is comparable to the activity of Diclofenac sodium. Compound 1a and 4 are found to be the most potent antioxidant with a remarkable IC50 value of 6.99 and 7.25 respectively, which is a little less than the standard drug, ascorbic acid, (IC50=6.94). In addition, a comparative examination of calculated Lipinski’s parameters reveals that all the compounds have the tendency to be orally bioavailable. PASS studies also show that certain compounds also have higher probability of anti-neoplastic activity. (3) Conclusion: Based on the outcomes, compounds 1a, 1b, 3, 4 and 8 can act as novel leads for the development of COX-2 inhibitors showing potent anti-inflammatory and antioxidant activity which can have lesser GI side effects and can be used in chronic disorders.
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