Ola A. El-Sayed

Synthesis of some novel quinoline-3-carboxylic acids and pyrimidoquinoline derivatives as potential antimicrobial agents.

The synthesis and in vitro antimicrobial evaluation of several quinoline and pyrimidoquinoline derivatives are described. Treatment of 7‐substituted quinolin‐2(1H)‐one‐3‐carboxylic acids 2a—c with phosphoryl chloride or thionyl chloride gave rise to the 7‐substituted 2‐chloroquinoline‐3‐carboxylic acids 3a—c and 7‐substituted 2‐chloro‐3‐chlorocarbonylquinolines 5a—c respectively. The 2‐chloro function in compounds 3a—c was replaced by 2‐aminothiazole or 2‐aminopyridine to give 2‐(thiazol‐2‐yl)aminoquinoline‐3‐carboxylic acids 4a—c or 2‐(pyrid‐2‐yl)aminoquinoline‐3‐carboxylic acids 4d—f. Treatment of 5a—c with the same heterocyclic amines at room temperature furnished the corresponding 7‐substituted 2‐chloro‐3‐heteryl‐aminocarbonylquinolines 6a—f. The tetracyclic 9‐substituted thiazolo[3′, 2′:1, 2]‐pyrimido[4, 5‐b]quinolin‐5‐ones 7a—c and 10‐substituted pyrido[1′, 2′:1, 2]‐pyrimido[4, 5‐b]quinolin‐6‐ones 7d—f were synthesized by heating 5a—c with the heterocyclic amines in toluene or by heating 6a—f under reflux in dimethylformamide. The products were evaluated in vitro for potential antimicrobial activity.

Synthesis of Aldehydo-sugar Derivatives of Pyrazoloquinoline as Inhibitors of Herpes Simplex Virus Type 1 Replication

Synthesis of a novel series of structurally related pyrazoloquinoline nucleosides is described. All the newly synthesized compounds were examined for their in vitro antiviral activity against herpes simplex type-1 as shown by two different bioassays, namely; crystal violet staining or the MTS tetrazolium dye measurement. The acute toxicity (LD50) values of the biologically active compounds were determined.

Synthesis and Benzodiazepine Receptor Binding Activity of 2, 9-Disubstituted Quinolino[2′, 3′-5, 4](3-pyrazolino)[3, 2-b]purin-4-ones

2, 9‐Disubstituted quinolino[2′, 3′‐5, 4](3‐pyrazolino)pyrimidin‐2‐ones and purin‐4‐ones were synthesized and their benzodiazepine receptor activity was evaluated for their ability to displace [3H]R015‐1788 from its specific binding in bovine brain membranes. Compound 5c caused 83 ± 8 %inhibition in [3H]R015‐1788 specific benzodiazepine receptor binding followed by compounds 5f, 5h, and 5i while other analogs were inactive at 10 μM concentration.