Exploring the in-vitro anti-diabetic and anti-bacterial potential of a bromothiophene pyrazolo-pyridine derivative and its complex for radiopharmaceutical applications

This study reports 4-(5-bromothiophen-2-yl)-3-methyl-1-1H-pyrazolo[3,4-b]pyridine-6-carbohydrazide (SBrHZD) as an imaging probe with diverse biological potential. SBrHZD showed better in-vitro anti-diabetic potential (IC₅₀ = 3.3 µg/mL) compared with acarbose (4.1 µg/mL). The anti-bacterial activity (MIC = 3 mg/mL) against E. coli was better (inhibition zone = 9.0 ± 0.45 mm), compared with rifampicin (8.30 ± 0.40 mm). Docking simulation revealed SBrHZD binding energy (∆G) of -6.41 and -6.55 kJ/mol for anti-diabetic and anti-bacterial applications, respectively, compared with etazolate's -4.17 and -4.21 kJ/mol. The SBrHZD complex, [^99mTc][Tc-SBrHZD-EDDA-tricine], exhibited ≥ 93% radiochemical yield and 12 h stability. In-vivo biodistribution performed in mice showed normal renal clearance, indicating potential for further in-vivo investigations. (author)