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Synthesis of Certain Mercapto and Aminopyrimidine Derivatives as Potential Antimicrobial Agents
El-Kerdawy, M.M.,Eisa, H.M.,El-Emam, A.A.,Massoud, M.A.,Nasr, M.N. The Pharmaceutical Society of Korea 1990 Archives of Pharmacal Research Vol.13 No.2
Reaction of ethyl 4-chloro-2-phenylpyrimidine-4-carboxylate (4) with 5-chloro-2-methylthiophenol or 3-aryl-4-phenyl-1, 2, 4-triazole-5 thiol yielded the corresponding thioethers (5) and (8a, b), respectively. Careful alkaline hydrolysis of (5) yielded the corresponding carboxylic acid (6). Reaction of (4) with p-aminoacetophenone yielded compound (10) which was reacted with certain aromatic aldehyde to afford the$\alpha,\beta$-unsaturated ketones (11a-d). Condensation of (11a-d) with malononitrile or phenylhydrazine yielded the 2-amino-3-cyanopyridines (12a-f) or the 2-pyrazolines (13a, b) respectively. Seven representative compounds were tested for their in vitro antimicrobial activity against some pathogenic micro-organisms, some of them were proved to be active.
Synthesis of certain thiaxanthones as potential schistosomicidal agents
El-Kerdawy, M.M.,El-Eman, A.A.,El-Subbagh, H.I. The Pharmaceutical Society of Korea 1986 Archives of Pharmacal Research Vol.9 No.1
Twenty nine substituted thiaxanthone derivatives were synthesized for schistosomicidal evaluation. The compounds, 1-morpholino-4-methyl-6-nitrothiaxanthone and 1-(2-diethyl-aminoethyl-amino)-4 methyl-6-nitrothiaxanthone dipicrate were found to possess promising schistosomicidal activity against Schistosoma mansoni in mice.
Synthesis of Substituted Arylazothioxanthones as Potential Schistosomicidal Agents
El-Kerdawy, M.M.,El-Emam, A.A.,El-Subbagh, H.I.,Abushanab, E. The Pharmaceutical Society of Korea 1989 Archives of Pharmacal Research Vol.12 No.1
A series of 1-chloro-4-methyl-6-arylazo-9H-thioxanthen-9-ones were synthesized and schistosomicidal activity evaluated. It was found that, 1-chloro-4-methyl-6-(2-hydroxy-1-naphthylazo)-9H-thioxanthen-9-one possessed a promising activity against Schisto-soma mansoni in mice.
El-Subbagh, H.I.,Yousif, M.Y.,El-Eman, A.A.,El-Kerdawy, M.M. The Pharmaceutical Society of Korea 1989 Archives of Pharmacal Research Vol.12 No.2
A convenient route is reported for the synthesis of certain series of 4H-thieno[2,3-b][1]benzothiopyran-4-ones, carrying various substituents at position 2 such as arylazomethines (7,8), thiazolidin-4-ones (9-13), ${\alpha},\;{\beta}-unsaturated$ ketones (16,17), 2-pyridones (19-23), tetrahydrothiophen-4-ones (24,28), and nitroalkenes (29,30), as potential schistosomicidal or antihistaminic agents.
Synthesis of certain 2-aminoadmantane derivatives as potential antimicrobial agents
Eisa, Hassan M.,Tantawy, Atif S.,El-Kerdawy, Mohamed-M. The Pharmaceutical Society of Korea 1990 Archives of Pharmacal Research Vol.13 No.1
N-(2-Amamantyl)-N-(5-arylhydrazono-6-methyl-4-oxopyrimidin-2-yl) guanidines (IIIa, b), 2-(2-admantyl-amino)-4-amino-s-triazine (IVa) and its 6-chloromethyl derivative (IVb) were prepared by cylization of 1-(2-admantyl) biguanide HCl (I) with ethyl 2-arylhydrazono-3-oxobutyrates (II), ethyl formate and ethyl chloroacetate, respectively. Where 1-(2-admantyl)-3-(4, 5-dioxo-2-imidazolidinylidene)guanidine (V) was used as intermediate for the synthesis of amides (VIIa, b), hydrazide (VIII) and azomethine derivatives (IX, b) of alkyl 2-(2-admantyl-amino)-4-amino-2-triazine-6-carboxylates (VI a, b). The antimicrobial testing of the prepared compounds proved that compound 1Xb was the most active. It showed a marked bacteriostatic effect against Staphylococcus aureus and Bacillus subtilis.
Some Nucleophilic Substitutions in 2,4- and 2,4,8-Trichloro- pyrido [3,2-d] pyrimidines
Boyomi, Said M.,Ismaiel, Abdel-Kader M.,Eisa, Hassan M.,El-Kerdawy, Mohamed M. The Pharmaceutical Society of Korea 1989 Archives of Pharmacal Research Vol.12 No.1
Reaction of 6-(acetoxymethyl) -2,4-dichloropyrido [3,2-d] pyrimidine (I) with some nucleophiles was investigated. When I reacted with sodium azide afforded 2,4-diazido derivative (II). Treatment of II with sodium hydroxide underwent cyclization of the 2-azido group to tetrazolo, replacement of 4-azido group by hydroxide ion, and hydrolysis of 6-ace-foxy moiety to hydroxy methyl derivative (III). While, reaction of I with hydrazine hydrate resulted in the formation of 2,4 dihydrozino-6-hydroxymethyl derivative (lV).