• Journal of the Korean Chemical Society
• /
• v.45 no.4
• /
• pp.325-333
• /
• 2001

The 4-substituted tetrazolo[1,5-a]quinoxalines were synthesized from 4-chlorotetrazolo-[1,5-a]quinoxaline(8) or 4-hydrazinotetrazolo[1,5-a]quinoxaline(9). Refluxing of the tetrazolo[1,5-a]quinoxaline(12) in N,N-dimethylformamide gave the 1,2,4-triazolo[3,4-c]tetrazolo[1,5-a]quinoxaline(13), which was also obtained by the reaction of compound 9 with ethyl chloroformate in N,N-dimethylformamide. The reaction of compound 9 with isothiocyanates in ethanol provided the tetrazolo[1,5-a]quinoxalines(14), whose reaction with dimethyl acetylenedicarboxylate afforded the tetrazolo[1,5-a]quinoxalines(15). The tetrazolo [1,5-a]quinoxalines(18) were obtained by the reaction of compound 9 with alkyl (ethoxymethylene)cyanoacetates. Some of the compounds showed antibacterial, antifungal or algicidal activities against some strains.

• Archives of Pharmacal Research
• /
• v.21 no.4
• /
• pp.465-469
• /
• 1998

The search for platinum (II)-based compounds with improved therapeutic properties was prompted to design and synthesize a new family of water-soluble, third generation cis-diaminedichloroplatinum (II) complexes linked to uracil and uridine. Six heretofore unreported uracil and uridine-platinum (II) complexes are; [N-(uracil-5-yl-methyl)ethane-1,2-di-amine]dichloroplatinum (II) (3a), [N-(uracil-6-yl-methyl)ethane-1,2-diaminel dichloroplatinum (II) (3b), t[N-($2^1$, $3^1$,$5^1$-tri-O-acetyl)uridine-5-yl-methyl] ethane-1,2-diamineldichloroplatinum (II) (6a), {[N-($2^1$,$3^1$, $5^1$-tri-O-acetyl) uridine-6-yl-methyl]ethane-1,2-diamine)dichloroplatinum (II) (6b),[N-(uridine- 5-yl-methyl)ethane-1,2-diamine]dichloroplatinum (II) (7a), [N-(uridine-6-yl- methyl)ethane-1,2-diamine]dichloroplatinum (II) (7b). These analogues were prepared from the key starting materials, 5-chloromethyluracil (1a) and 6-chloromethyluracil (1b) which were reacted with ethylenediamine to afford the respective 5-[(2-aminoethyl)aminol methyluracil (2a) and 6-[(2-aminoethyl)amino]methyluracil (2b). The cis-platin complexes 3a and 3b were obtained through the reaction of the respective 2a and 2b with potassium tetrachloroplatinate (II). The heterocyclic nucleic acid bases 1a and 1b were efficiently introduced on the .betha.-D-ribose ring via a Vorbruggen-type nucleoside coupling procedure with hexamethyldisilazane, trimethylchlorosilane and stannic chloride under anhydrous acetonitrile to yield the stereospecific .betha.-anomeric 5-chloromethyl- $2^1$,$3^1$,$5^1$-tri-O-acetyluridine (4a) and 6-chloromethyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (4b), respectively. The nucleosides 4a and 4b were coupled with ethylenediamine to provide the respective 5-[(amino-ethyl)aminolmethyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (5a) and 6-[(aminoethyl)amino] methyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (5b). The diamino-uridines 5a and 5b were reacted with potassium tetrachloroplatinate (II) to give the novel nucleoside complexes, 6a and 6b, respectively which were deacetylated into the free nucleosides, 7a and 7b by the treatment with CH$_{3}$ONa. The cytotoxic activities were evaluated against three cell lines (FM-3A, P-388 and J-82) and none of the synthesized compounds showed any significant activity.

• Journal of Life Science
• /
• v.14 no.2
• /
• pp.351-355
• /
• 2004

Saccharin derivatives were synthesized by means of 4 reaction steps involved the reaction of 1-methylurea (or 1-methylthiourea) and oxalyl chloride. 1-Alkyl(or phenyl)-3-(1,1,3-trioxo-1,3-dihydro-1$^{6}$ -benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-trione 5 and 1-alkyl(or phenyl)-2-thioxo- 3-(1,1,3-trioxo-1,3-dihydro-1$^{6}$ -benzo-[d]isothiazol-2-ylmethyl)-imidazolidine-4,5-dione 12 were obtained by means of 4 reaction steps involved the reaction of 1-methyl-urea(or 1-methylthiourea) and oxalyl chloride.

• Journal of Life Science
• /
• v.34 no.5
• /
• pp.333-338
• /
• 2024

Kinesin-1 is a heterotetrameric protein composed of two heavy chains (KHCs, also known as KIF5s) with a motor domain and two light chains (KLCs) without a motor domain. KIF5 has three subtypes, namely, KIF5A, KIF5B, and KIF5C, which share high amino acid homology except in their carboxy (C)-terminal region. KIF5A is responsible for transporting cargo within the cell. The adaptor proteins that bind to the C-terminal region of KIF5A mediate between kinesin-1 and cargo. However, the proteins regulating the intracellular cargo transport of kinesin-1 have not yet been fully identified. In this study, we identified ADP-ribosylation factor GTPase-activating protein 1 (ArfGAP1), which is involved in the intracellular trafficking of lysosomes, as a binding partner of KIF5A. KIF5A binds to the C-terminal region of ArfGAP1, and ArfGAP1 binds to the C-terminal region of KIF5A but does not interact with KIF5B, KIF5C, kinesin light chain 1 (KLC1), or KIF3A. When co-expressed in mammalian cells, ArfGAP1 co-localized with KIF5A and co-immunoprecipitated with KIF5A, KIF5B, and KLC1, but not with KIF3B. These results suggest that kinesin-1 may be regulated by ArfGAP1 in the intracellular transport of cargo.

• Journal of Life Science
• /
• v.17 no.7 s.87
• /
• pp.910-914
• /
• 2007

In order to synthesize new bioactive compounds and contrasting agents, reactions of glycine and glutamic acid as an animo acid with paraformaldehyde and hypophosphorous acid were executed. Products are 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid 1 and 3,7-dihydroxy-3,7- dioxoperhydre-1,5,3,7-diazadiphosphocine-1,5-di-(2-glu taric acid) 3. 2-[5-(1,2-Dicarboxyethyl)-3,7-dihydroxy-3,7-dioxo-315.715-[1,5,3,7] diazadiphosphocan-1-yl]-succinic acid 2 by using aspartic acid was not obtained. Esterification of 3,7- dihydroxy-3,7-dioxoperkydro-1,5,3,7-diaza-diphosphocine-1,5-diacetic acid 1 by treatment of methanol, ethanol, and propanol were executed. 3,7-Dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid methyl ester 4, 3.7-dihydroxy-3,7-dioxoperhydro-1,5,3,f-diazadiphosphocine-1.5-diacetic acid ethyl ester 5, and 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid propyl ester 6 were respectively synthesized in good yields. Continuously, we will try synthesis of novel compounds and evaluation of biological activity.

• Journal of Life Science
• /
• v.24 no.1
• /
• pp.14-19
• /
• 2014

Kinesin-1 consists of two heavy chains (KHCs), also called KIF5s, and two light chains (KLCs) that form a heterotetrameric complex. Here, we demonstrate the binding of a neuronal KHC, KIF5A, to the carboxyl (C)-terminal tail region of Fig4 (also known as Sac3), a phosphatase that removes the 5-phosphate from phosphatidylinositol-3,5-bisphosphate ($PtdIns(3,5)P_2$). Fig4 bound to the C-terminal region of KIF5A but not to other KHCs (KIF5B and KIF5C) and KLC1 in yeast two-hybrid assays. The interaction was further confirmed in a glutathione S-transferase pull-down assay and by co-immunoprecipitation. Anti-KIF5A antibody co-immunoprecipitated Fig4 with KIF5A from mouse brain extracts. These results suggest that kinesin-1 could transport the Fig4-associated protein complex or cargo in cells.

• Journal of Life Science
• /
• v.13 no.1
• /
• pp.54-58
• /
• 2003

1-Methyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5a, 1-ethy1-3-(1,1,3-trioxo-1,3-dihydro-lλ$^6$/-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5b 1-phenyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo [d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5c were obtained by means of 4 reaction steps involved the reaction of 1-methyl-urea and oxalyl chloride. Biological tests(Plant Response Screening Result, Insect Primary Screening Result and Fungicide Primary Screening Result) of synthesized sacccarin derivatives were executed.

• Journal of the Korean Chemical Society
• /
• v.55 no.6
• /
• pp.974-977
• /
• 2011

Ethyl 1-aminotetrazole-5-carboxylate (1) has been utilized to construct a variety of novel tetrazolo [1,5-b]-1,2,5-oxadiazepine derivatives which repesent a relatively little explored group with interesting antibacterial activities. The synthesized compounds were elucidated using IR, $^1H$ NMR and mass spectroscopic methods, besides elemental analyses.

• Korean Journal of Environmental Agriculture
• /
• v.42 no.4
• /
• pp.389-395
• /
• 2023

This study evaluated the effects of gibberellic acid (GA₃) on the growth and quality of creeping bentgrass (Agrostis palustris Huds.). Experimental treatments included a No application of fertilizer and GA₃ (NFG) Control [3 N active ingredient (a.i.) g/m²], 0.3GA₃ (GA₃ 0.3 a.i. mg/m²/200 mL), 0.6GA₃ (GA₃ 0.6 a.i. mg/m²/200 mL), 1.2GA₃ (GA₃ 1.2 a.i. mg/m²/200 mL), and 2.4GA₃ (GA₃ 2.4 a.i. mg/m²/200 mL). Additionally, the study included a 1.5N+GA₃ experiment with similar GA₃ treatments combined with 1.5N a.i. g/m² : NFG, Control (3N a.i. g/m²), 1.5N+ 0.3GA₃ (1.5N a.i. g/m²+GA₃ 0.3 a.i. mg/m²/200 mL), 1.5N+0.6GA₃ (1.5N a.i. g/m²+GA₃ 0.6 a.i. mg/m²/200 mL), 1.5N+1.2GA₃ (1.5N a.i. g/m²+GA₃ 1.2 a.i. mg/m²/ 200 mL), and 1.5N+2.4GA₃ (1.5N a.i. g/m²+GA₃ 2.4 a.i. mg/m²/200 mL). Compared to the NFG, turf color index chlorophyll content was not significantly different (p< 0.05). However, shoot length in 1.2GA₃, 2.4GA₃, 1.5N+0.3GA₃, 1.5N+0.6GA₃, 1.5N+1.2GA₃, and 1.5N+2.4GA₃ treatments increased by 0.8%, 10.6%, 5.15%, 8.3%, 13.5 %, and 21.6%, respectively, compared to the control. As compared to the control, clipping yield in 1.5N+1.2GA₃ and 1.5N+2.4GA₃ treatments increased by 7.1% and 14.3 %, respectively. These results indicated that GA₃ application increased shoot length, with the 1.2GA₃ treatment showing shoot length similar to the control (3N a.i. g /m² ).

• Korean Journal of Environmental Biology
• /
• v.21 no.3
• /
• pp.276-285
• /
• 2003

To control pythium root rot, Bacillus lentimorbus WJ5a17 with high anti-fungal activity against Pythium ultimum was induced from B. lentimorbus WJ5 by gamma radiation ($^{60}Co$). The biocontrollers of FWJ5 and FWJ5a17 were formulated ($1.0\times 10^{11}$) with B. lentimorbus WJ5 and WJ5a17, respectively, The population density of FWJ5 and FWJ5a17 maintained highly up to $1.0\times 10^{9}$ CFU $g^{-1}$ in nursery and field soils until 30 days after treatment. P. ultimum spores germination were inhibited 71.0% and 81.4% by FWJ5 and FWJ5a17, respectively. Pythium root rot of yea pepper, Chinese cabbage and radish were significantly (p < 0.05) controled by one time treatment of FWJ5 and FWJ5a17.