Category: pyridine-derivatives. In 2019.0 BIOORG CHEM published article about 1,3,4-THIADIAZOLE DERIVATIVES; PHARMACOLOGICAL-ACTIVITIES; ANTIMICROBIAL ACTIVITIES; ANTIBACTERIAL ACTIVITY; SCHIFF-BASES; 1,2,4-TRIAZOLE; SYSTEM in [Taha, Muhammad; Almandil, Noor Barak; Ibrahim, Mohamed; Mosaddik, Ashik; Khan, Khalid Mohammed] Imam Abdulrahman Bin Faisal Univ, IRMC, Dept Clin Pharm, POB 1982, Dammam 31441, Saudi Arabia; [Rashid, Umer] COMSATS Univ, Dept Chem, Islamabad, Pakistan; [Ali, Muhammad] Univ Nizwa, Nat & Med Plants Sci Res Ctr, POB 33, Birkat Al Mauz 616, Nizwa, Oman; [Gollapalli, Mohammed] Imam Abdulrahman Bin Faisal Univ, CCSIT, POB 1982, Dammam 31441, Saudi Arabia; [Khan, Khalid Mohammed] Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan in 2019.0, Cited 36.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.
Twenty-five thiadiazole derivatives 1-25 were synthesized from methyl 4-methoxybenzoate via hydrazide and thio-hydrazide intermediates, and evaluated for their potential against beta-glucuronidase enzyme. Most of the compounds including 1 (IC50 = 26.05 +/- 0.60 mu M), 2 (IC50 = 42.53 +/- 0.80 mu M), 4 (IC50 = 38.74 +/- 0.70 mu M), 5 (IC50 = 9.30 +/- 0.29 mu M), 6 (IC50 = 6.74 +/- 0.26 mu M), 7 (IC50 = 18.40 +/- 0.66 mu M), and 15 (IC50 = 18.10 +/- 0.53 mu M) exhibited superior activity potential than the standard D-saccharic acid-1,4-lactone (IC50 = 48.4 +/- 1.25 mu M). Molecular docking studies were conducted to correlate the in vitro results and to identify possible mode of interaction with enzyme active site.
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem