Assistant Lecturer Ameer Hussein Kadhim & Assistant Lecturer Haider Jabbar Madloul Abstract Objective:The objective of this study was to synthesize phenylcinnamamide (substituted acetanilide chalcone) derivatives linked to aspirin and ibuprofen with potential antibacterial and antifungal activity. Methods:Substituted acetanilide compounds were reacted with different arylaldehydes through Claisen-Schmidt condensation in the presence of KOH. They formed differently substituted acetanilide chalcones (1a-e) which are linked to aspirin and ibuprofen through an ester linkage to form compounds (2a-j) using ethyl chloroformate (ECF) as a catalyst. Results:The synthesized compounds have been characterized by elemental analysis, Fourier transform infrared and1 H-nuclear magnetic resonance spectroscopy. An antibacterial evaluation [...]

Assistant Prof. Dr. Ismail Taha Ibrahim Abstract 4-{(4-Methylphenyl)glycyl}-3,4-dihydroquinoxalin-2(1H)-one (QIN) was prepared from 4-(2-chloroacetyl)- 3,4-dihydroquinoxalin-1(1H)-one). ¹²⁵I-QIN was prepared by electrophilic substitution using Chloramine- T as an oxidizing agent. The highest labeling yield, 94%, was obtained under the following conditions: pH 7, 15 min, 100 μg of QIN, 50 μg of Chloramine-T, and carrier-free Na¹²⁵I. The labeled compound was stable for up to 12 h post labeling. A biodistribution study of ¹²⁵I-QIN in mice showed that its brain uptake was about 5.1% at 30 min post injection and remained on this level up to 1 h. As compared to commercially used radiopharmaceuticals for [...]

Assistant Prof. Dr. Ismail Taha Ibrahim Abstract Haloperidol (HP) is a dopamine blocking agent. HP was radiolabeled with 125I using direct electrophilic substitution. Different HP formulations such as intravenous solution (VS), intranasal solution (NS) and intranasal microemulsion (NME) have been prepared. Optimum labeling yield of 125I-HP was obtained 93.42±1.53%. Isopropylmyristate oil (10%), Tween 80 (30%), propylene glycol (15%) and aqueous phase (45%) were used for NME preparation. Using Swiss Albino mice, the % brain uptake were 1.4±0.2, 4.3±0.2 and 5.7±0.4% for VS, NS and NME, respectively. 125I-HP in NME formula showed superiority as drug delivery system for brain imaging. KeywordsHaloperidol · 125I · [...]