• Bulletin of the Korean Chemical Society
• /
• v.17 no.7
• /
• pp.607-612
• /
• 1996

A series of new NLO-active poly(4-nitrophenylallylamine) derivatives was synthesized by the nucleophilic substitution reaction of several substituted 4-nitrohalobenzenes and poly(allylamine hydrochloride). All polymers obtained were amorphous and their glass transition temperatures (Tg) were observed around 148-160 ℃. For each of these polymers, their specific Tg values were dependent on characteristic electronic structures. UV-visible absorption spectra showed maximum absorption intensity at 355-393 nm for π-π* transition of alkylaminonitrophenyl groups. The χ(2)value of poly(4-nitrophenylallylamine), as determined by the second harmonic generation at 1064 nm, for a thin polymer film poled at an elevated temperature, was 1.4x10-8esu. The third-order NLO properties of poly(4-nitrophenylallylamine) derivatives were evaluated through measurement of degenerate four-wave mixing technique and χ(3) coefficient in the range of 2.7~3.2x10-12 esu at 602 nm was found with 400 fs laser pulses.

• YAKHAK HOEJI
• /
• v.44 no.4
• /
• pp.318-324
• /
• 2000

9 New cephalosporin derivatives were synthesized and screened for antibacterial activities against various bacteria. (6R,7R) -7$\beta$-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(fluoromethoxyimino)acetamido]-3-[(2-hydroxycarbamoyl)-s-triazolo[1,5-a]-pyrimidin-7-yl]thiomethyl]-3-cephem-4-carboxylic acid sodium salt (compound 3) showed 2 fold enhanced in vitro activity against P. aerurginosa, compared to ceftazidime.

• Bulletin of the Korean Chemical Society
• /
• v.20 no.5
• /
• pp.551-555
• /
• 1999

11-Deoxydaunomycinone 15 and 10-fluoroanthracyclinone derivatives 9, 10 were obtained. Naphthalenone 4 prepared from 2-(2,4-pentadienyl)-1,3-dioxane 2 with methyl vinyl ketone and hydrolysis with HClO4 was condensed with phthalidesulfone 5 through Michael type reaction, and was converted to 7 by epoxidation. Epoxide 7 was transformed to trione 12 using reduction-oxidation or hydrofluorination process, and then to 15 by introducing several functional groups. Compound 8 obtained in the course of the reaction of epoxide 7 and HF/ Pyr was used for the synthesis of compounds 9, 10.

• Archives of Pharmacal Research
• /
• v.28 no.11
• /
• pp.1205-1212
• /
• 2005

2-Thiouracil-5-sulphonic acid N-(4-acetylphenyl) Amide (1) was reacted with a series of aromatic aldehydes giving chalcones 2 (Claisen-Schemidt reaction), some of these chalcones were reacted with urea and thiourea giving pyrimidine-2-one and pyrimidine-2 thione derivatives respectively of the type 3a,b and 4a,b. In addition many chalcones were reacted with hydroxylamine hydrochloride giving isoxazoline derivatives 5a,b. They could also reacted with phenylhydrazine to give pyrazoline derivatives 5a,b, chalcones also were reacted withethylcyano acetate and/or malononitryl in pyridine giving pyran derivatives 7a,c and 8a,c. In another pathway chalcones were epoxidised by $H_{2}O_{2}$ giving epoxides 9a,c which in turn were reacted with phenylhydrazine giving 4-hydroxypyrazoline derivatives 10a,c. In another reaction chalcones were reacted with ethylcyanoacetate in presence of amm.acetate giving pyridone derivatives 11a,d which could be prepared also in exellent yield from compound 1 by its reaction with certain aromatic aldehydes and ethylcyanoacetate in presence of ammonium acetate. Finally, compound 1 was reacted with semicarbazide giving semicarbazone intermediate 12 which in turn was reacted with thionyl chloride giving thiadiazole derivative 13. The biological effects of some of the new synthesized compounds were also investigated.

• Journal of the Korean Applied Science and Technology
• /
• v.28 no.1
• /
• pp.118-125
• /
• 2011

New type of 5-fluorobenzimidazole derivatives was synthesized through the reaction of 4-fluoro-5-(2,6-dimethylmorpholinyl)-2-aminoaniline with 5-nitro-2-furoic acid and 5-methoxy-3-chlorobenzothiophene-2-carboxylic acid in presence of PPA and treatment of $OH^-$. the resulting substituted 5-fluorobenzimidazole derivatives(6), (7) was characterized by high solubility in common polar organic solvents. We considered 5-fluorobenzimidazole derivatives were useful especially for antifungal drugs. These results are discussed from the viewpoints of the chemical and physical structures of the 5-fluorobenzimidazole derivatives.

• Journal of Microbiology and Biotechnology
• /
• v.12 no.6
• /
• pp.1006-1009
• /
• 2002

The biological activities of farnesoic acid derivatives against pathogenic fungi and bacteria were investigated. Farnesoic acid and its derivatives showed growth inhibitory activities against various bacteria. Among the compounds tested, geranylgeranoic acid (3) had potent antibacterial activity against Salmonella typhimurium, Proteus vulgaris, and Bacillus subtilis with minimum inhibitory concentration (MIC) in the range of $6.25-12.5{\mu}g/ml$. On the other hand, amide derivatives of farnesoic acid showed some antifungal activities. In particular, 3,7,11-trimethyl-dodeca-2,6,10-trienoic acid amide (5a) had a potent antifungal activity against Aspergillus niger, Candida albicans, and Trichophyton sp. with MIC in the range of $6.25-12.5{\mu}g/ml$.

• Archives of Pharmacal Research
• /
• v.13 no.2
• /
• pp.198-200
• /
• 1990

3, 4-Diphenyl-5-cyanopyridazin-6-one 3 was prepared from the reaction of cyano acetamide 2 with benzihydrazone in dry pyridine. A series of its derivatives was prepard. Tolyl and benene sulphonyl derivatives 6a and 6b are also prepared. 3, 4-Diphenyl-5-cyanopyridazin-6-thione 5 was obtained from 3 by the action of $P_2S_5$ while 3, 4 diphenyl-5-cyano 6-chloropyridazine 4 was obtained from 3 by the action POCl$_3$. The reaction of 4 with hydrazine hydrate directly afforded the pyrazolopyridazine derivative 7. Compound 4 also reacted with phenylhydrazine, aniline, thiophenol and anthranilic acid to yield pyridazine derivatives 8, 9, 10 and 11, respectively. On treatment of compound 11 with acetic anhydride it cyclised to afford pyridazino pyrimidine derivatives 12.

• Archives of Pharmacal Research
• /
• v.28 no.8
• /
• pp.877-884
• /
• 2005

A number of wogonin derivatives have been synthesized as congeners of wogonin and evaluated for their inhibitory activities of $PGE_2$ production. Wogonin derivatives modified at the B ring of wogonin were obtained from 2,4-Dihydroxy-3,6-dimethoxyacetophenone (1) via several steps. Most wogonin derivatives exhibited much reduced inhibitory activities against COX-2 catalyzed $PGE_2$ production compared to that of wogonin. Alkylation of 5,7-phenol groups and substitution at the B ring of wogonin generally caused reduction of inhibitory activity.

• YAKHAK HOEJI
• /
• v.40 no.6
• /
• pp.697-704
• /
• 1996

Quinolone derivatives, SJ5b (ethyl 5,12-dihydro-5-dihydro-5-oxobenzoxazolo[3,2-a]quinoline-6-carboxylate) and SQ7b (3-fluoro-2-(4-methylpiperazin-1-yl)-5.12-dihydro-5-oxobenzoxa zolo[3,2-a]quinoloine carboxylic acid) showed in vitro cytotoxicities against various tumor cell lines. SJ5b and SQ7b completely inhibited the DNA relaxation activities of human placental topoisomerase II at the concentration of 15.63 and 1.95 ${\mu}$g/ml, respectively. However, unlike etoposide which stabilize the topoisomerase II-DNA complex, SQ7b did not cause topoisomerase II-mediated DNA cleavage and SJ5b weakly stabilized the topoisomerase II-DNA cleavable complex. Through both experiments. DNA relaxation assay by the increment of topoisomerase II concentration and DNA unwinding assay, it was shown that SJ5b and SQ7b did not interact with topoisomerase II itself but bound to DNA. Therefore, it was concluded that DNA binding of SJ5b and SQ7b caused the inhibition of topoisomerase II related to DNA relaxation but no or very weak stabilization of topoisomerase II-DNA cleavable complex. In addition, SJ5b and SQ7b prevented whole cell nucleic acid syntheses in HL60 cells.

• Journal of the Korean Chemical Society
• /
• v.43 no.5
• /
• pp.535-539
• /
• 1999

1,3-Dimethyllumazine derivatives were synthesized by using Timmis reaction. The reaction of 4-amino-1,3-dimethyl-5-nitrosouracil(1) with 2,4-pentanedione, ethyl cyanoacetate, and ethyl acetoacetate provided 6-acetyl-1,3,7-trimethyllumazine (2), ethyl 7-amino-1,3-dimethyllumazine-6-carboxylate (4), and ethyl 1,3,7-trimethyllumazine-6-carboxylate (5) in good yieId, respectively. The various 1,3-dimethyllumazine derivatives were prepared from the side chain reactions of 6-acetyl and ester group in compound 2,4, and 5. The structure and physical properties of obtained compounds were characterized NMR, UV, IR spectrum, and elementary analysis.