Author(s):
Mhamad Jawdat Khalof, Samer Haj Kadoorc, Djamila Ben Hadda, Mustapha Fawaz Chehna
Email(s):
mhamadkhalof8991@gmail.com , mf.chehna@gmail.com
DOI:
10.52711/0974-360X.2026.00365 
Address:
Mhamad Jawdat Khalof1*, Samer Haj Kadoorc, Djamila Ben Hadda2, Mustapha Fawaz Chehna1
1Department of Pharmaceutical Chemistry and Quality Control, Faculty of Pharmacy, University of Aleppo, Aleppo, Syria.
2Department of Pharmaceutical Chemistry and Quality Control, Faculty of Pharmacy, Ebla Private University, Idlib, Syria.
3Department of Laboratory of Medicine, Faculty of Medicine, University of Aleppo, Syria.
*Corresponding Author
Published In:
Volume - 19,
Issue - 6,
Year - 2026
ABSTRACT:
Blood clots (thrombi) are notable causes of morbidity and mortality and are related to deep vein thrombosis (DVT), pulmonary embolism (PE), myocardial infarction (MI), and stroke. Coagulation Factor IXa (FIXa) is a primary therapeutic target since it plays an important role in the intrinsic pathway of coagulation. We designed and synthesized new quinoline-sulfonamide derivatives (A1, B1, C1) to test for potential anticoagulants using molecular docking and in vitro assays. We synthesized the derivatives through the reaction of quinoline-8-sulfonyl chloride and primary amines that gave yields ranging from (75 - 82%). Molecular docking with the Molegro Virtual Docker (MVD) showed strong binding responses ranging from -86.941 to -165.44kcal/mol with FIXa. mediated by hydrogen bonds with key catalytic residues (e.g., Ser 195, His 57, Asp 189). Compound A1 had the best binding (-121.45kcal/mol), and in vitro APTT was significantly prolonged (46.6±1.8sec, respectively vs control of 33.8±4.3 sec) and suggests inhibition of the intrinsic pathway. In contrast, compounds B1 and C1 showed minimal effects on APTT and prothrombin time (PT). These findings highlight the potential of quinoline-sulfonamide derivatives, particularly A1, as FIXa inhibitors with promising anticoagulant properties.
Cite this article:
Mhamad Jawdat Khalof, Samer Haj Kadoorc, Djamila Ben Hadda, Mustapha Fawaz Chehna. In vitro Studies of Novel Quinoline-Sulfonamide Derivatives as Potent Factor IXa Inhibitors: Design via Molecular Modeling and Synthesis using a Facile Method. Research Journal Pharmacy and Technology. 2026;19(6):2551-6. doi: 10.52711/0974-360X.2026.00365
Cite(Electronic):
Mhamad Jawdat Khalof, Samer Haj Kadoorc, Djamila Ben Hadda, Mustapha Fawaz Chehna. In vitro Studies of Novel Quinoline-Sulfonamide Derivatives as Potent Factor IXa Inhibitors: Design via Molecular Modeling and Synthesis using a Facile Method. Research Journal Pharmacy and Technology. 2026;19(6):2551-6. doi: 10.52711/0974-360X.2026.00365 Available on: https://rjptonline.org/AbstractView.aspx?PID=2026-19-6-22
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