An article Synthesis of oxadiazole-coupled-thiadiazole derivatives as a potent beta-glucuronidase inhibitors and their molecular docking study WOS:000476649000011 published article about BIOLOGICAL EVALUATION; ANTIFUNGAL ACTIVITY; SCHIFF-BASES; 1,3,4-THIADIAZOLE; CANCER; SERIES; ANTICONVULSANT; ANALOGS; BEARING; URINE in [Taha, Muhammad; Mosaddik, Ashik] Imam Abdulrahman Bin Faisal Univ, IRMC, Dept Clin Pharm, POB 31441, Dammam, Saudi Arabia; [Imran, Syahrul] Univ Teknol MARA UiTM, Atta Ur Rahman Inst Nat Prod Discovery, Puncak Alam Campus, Bandar Puncak Alam 42300, Selangor De, Malaysia; [Alomari, Munther] Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat, Dept Stem Cell Res, POB 1982, Dammam 31441, Saudi Arabia; [Rahim, Fazal] Hazara Univ, Dept Chem, Mansehra 21120, Pakistan; [Wadood, Abdul] Abdul Wali Khan Univ Mardan, Dept Biochem, Mardan 23200, Pakistan; [Uddin, Nizam] Univ Karachi, Dept Chem, Karachi 75270, Pakistan; [Gollapalli, Mohammed; Alqahtani, Mohammed A.; Bamarouf, Yasser A.] Imam Abdulrahman Bin Faisal Univ, CCSIT, Dept Comp Informat Syst, POB 1982, Dammam 31441, Saudi Arabia in 2019.0, Cited 54.0. Category: pyridine-derivatives. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1
A new series of oxadiazole with thiadiazole moiety (6-27) were synthesized, characterized by different spectroscopic techniques and evaluated for beta-glucuronidase inhibitory potential. Sixteen analogs such as 6, 7, 8, 9, 10, 12, 13, 14, 17, 18, 20, 23, 24, 25, 26 and 27 showed IC50 values in the range of 0.96 +/- 0.01 to 46.46 +/- 1.10 mu M, and hence were found to have excellent inhibitory potential in comparison to standard D-saccharic acid 1,4-lactone (IC50= 48.4 +/- 1.25 mu M). Two analogs such as 16 and 19 showed moderate inhibitory potential while analogs 11, 15, 21 and 22 were found inactive. Our study identifies new series of potent beta-glucuronidase inhibitors for further investigation. Structure activity relationships were established for all compounds which showed that the activity is varied due to different substituents on benzene ring. The interaction of the compounds with enzyme active site were confirmed with the help of docking studies, which reveals that the electron withdrawing group and hydroxy group make the molecules more favorable for enzyme inhibition.
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem