Abstract:Condensation of 1-acetyl-1,2,3,4-tetrahydro-9H-carbazole (2) with some amino compounds furnished the corresponding imino derivatives 3a-e. Compound 3a reacted with chloroacetic acid and underwent cyclization to give the thiazolidine derivative 5. Also, treatment of 3c with thionyl chloride caused cyclization to yield the [1,2,6]thiadiazino derivative 6, which gave the corresponding N-formyl derivative 7 upon heating with ethyl formate. In addition, interaction of 3d with ethyl cyanoacetate yielded the monoamide of malonic acid derivative 8. Acylation of carbazole 1 with succinoyl chloride or phenylacetyl choride produced the corresponding azepine (11) and 1,9-diphenyl acetyl derivatives (14), respectively. Compounds 11, 14 were further reacted to give the carbazole derivatives 12, 13 and 15a,b. The cytotoxic activity for some of the prepared compounds against breast cancer B 20 is discussed.
Synthesis and Pharmacological Activity of Some 2,3-Diphenylindole Derivatives.-Five-and six-membered heterocyclic rings are synthesized through variation of the aromatic indole moiety by introducing different acidic groups and cyclization. Compounds (I), (V), (VI), (VIII), and ( IX), are tested for their antiinflammatory and analgesic activities. Derivatives (Ia) and (VIII) are found to be more potent antiinflammatory compounds than indomethacin, and (VIII) and (Vb) are found to be more potent than aspirin. -(ISMAIL, M. M. F.; SHMEISS, N. A. M. M.; EL-DIWANI, H. I.; ARBID, M. S.; Indian
Synthesis of Novel Quinoxaline Carboxylic Acid Derivatives for Antimicrobial Investigation. -A variety of novel quinoxalinecarboxylic acid derivatives exhibiting various antimicrobial activities are synthesized starting from anhydride (I). Schiff base (Xb) proves to be the most active compound. -(EL-GABY, M. S. A.; ISMAIL, M. M. F.; AMMAR, Y. A.; ZAHRAN, M. A.; SHMEISS, N. A. M. M.; Indian J. Chem., Sect. B: Org.
Synthesis and Reactions of Mannich Bases of 3-Hydroxycoumarin-[synthesis of 4-substituted aminomethyl-3-hydroxycoumarins (I) via Mannich reaction and transformation into methylene-bis(coumarins), benzopyranocoumarins, and other derivatives]. -(MIKY, J. A. A.; SALEH, N. M.; SHMEISS, N. A. M. M.; J. Indian Chem. Soc. 74 (1997) 10, 814-815; Dep.
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