• 약학회지
• /
• 제31권6호
• /
• pp.370-375
• /
• 1987

1, 4-Benzodiazepin 5-one was prepared from 2-aminobenzamide derivatives by acid catalyzed intermolecular cyclization. N-Alkylation of 2-aminobenzamide with $\alpha$-bromo acetaldehyde diethylacetal to 2(2', 2'-diethoxyethyl) aminobenzamide (I) and subsequent treatment of I with acid gave 1, 4-benzdiazepin 5-one, where as the acetyl derivatives of I did not react to 1, 4-benzodiazepin 5-one but to methyl 4-quinazolone (IV).

• 약학회지
• /
• 제34권2호
• /
• pp.133-138
• /
• 1990

The reaction of 2-aminobenzamide with phthalic acid anhydride In dioxane produced a bicyclic product 2,8-dioxoisoindole(1,2,a) quinazoline (I) in addition to hydrolysis product 2(2-Carboxyphenyl)-1,2-2H-quinazoline-4-one (II). The yields were 64% and 30% respectively. On the other hand, the same reaction in DMF afforded compound (I) and 2(2N-dimethyl carbamyl phenyl)-1,4-2H-quinazoline-4-one (III) in 30% and 60% yield respectively. The compound III was also obtained by the reaction of compound II with dimethylamine. However the reaction of 2-aminobenzamide with neat succinic acid anhydride gave only bicyclic product 2,8-oxopyrrolidine (2,1,a)-1,4-2H-quinazoline (IV) in 93%.

• 약학회지
• /
• 제29권2호
• /
• pp.103-106
• /
• 1985

Reaction between 2-aminobenzamide and thionylchloride gave benzo-2-this-1,3[2H]-diazine-4-one-2-oxide (I) at room temperature. With other carbonyl derivatives quinazoline-4-one derivatives (II-VIII) were obtained.

• 약학회지
• /
• 제30권5호
• /
• pp.203-207
• /
• 1986

2-Aminobenzamide reacts with not only keton radical but also carbonyl group in carboxylic acid, to form easily -N-C-N-novel ring cyclization as a result I and V. In addition, it reacts with 1, 2-cyclohexadione or benzil, whitch are both 1, 2-diketone compounds, at the both ketone radical sites to give V or VII respectively. On the reaction with dimethone, however, which has 1, 3-diketone radical, it reacted with only one carbanyl group and VI was produced. We investigated the reaction with cr-ketoester such as ethyl pyruvate and diethyl rnesoxalate. In the reaction with ethylpyruvate, amine group in 2-aminobenzamide reacted not with ketone radical but carbonyl group in ester (product VIII). On the other hand, diethyl measoxalate reacted at the ketone radical site rather than the ester site (product IX).

• 한국환경성돌연변이발암원학회지
• /
• 제11권2호
• /
• pp.107-117
• /
• 1991

The effect of 3-aminobenzamide (3AB), an inhibitor of poly (ADP-ribose) polymerase, on ethyl methanesulfonate (EMS)-or bleomycin (BLM)-induced DNA repair synthesis and chromosome aberrations was examined during the cell cycle of Chinese hamster ovary (CHO)-K$_1$ cells. The synchronized cells were obtained by using thymidine double block method and mitotic selection method. Three assays were employed in this study: unscheduled DNA synthesis, alkaline elution and chromosome aberrations. 3AB alone did not induce DNA repair and chromosome aberrations in all phases. The post-treatment with 3AB inhibited DNA repair synthesis induced by EMS or BLM in G$_2$ phase, whereas 3AB did not affect chromosome aberrations induced by EMS or BLM in all phases. These results suggest that 3AB aggravates the cell cycle disturbance which occur after DNA damage, and leads to an accumulation of cells at G$_2$ phase, and inhibits DNA repair synthesis, while the effect 3AB on chromosome aberrations may need reevaluated.

• 한국환경농학회지
• /
• 제16권3호
• /
• pp.264-268
• /
• 1997

식물이 토양미생물 유래 유기화합물의 선택적인 흡수에 주목하여 근권주위의 토양시료로부터 방선균을 중심으로 분리하였다. 방선균 K9301주 배양액에 식물유묘를 24시간 처리후하였다. 처리후의 배양액중의 하나의 대사산물이 소식됨을 알수 있었다. 이 대사산물은 벼뿐만 아니라 밀에서도 선택적으로 흡수되었다. TLC상의 Rf0.6의 대사산물 spot를 분리하였으며 2-aminobenzamide로 동정되었다.

• 약학회지
• /
• 제33권4호
• /
• pp.246-252
• /
• 1989

2-Amino-1-N-methyl benzamide, 2-N-benzyl amino benzamide, 2-N-phenyl amino benzamide of 2-amino benzamide derivatives were reacted with ${\alpha}-bromo$ acetaldehyde diethyl acetal in basic condition. 2-N-alkylated products were prepared from 2-amino-1-N-methyl benzamide and 2-N-phenyl amino benzamide. 1-N-benzyl-1.4-benzodiazepin-5-one was prerpared from 2-N-benzyl aminobenzamide via intramolecular cyclization. However, 2-amino-1-N-methyl benzamide with sodium amide did not react to 1.4-benzodiazepin-5-one derivative but 3-methyl-quinazoline-2.4-dione was obtained.

• 한국동물학회지
• /
• 제26권3호
• /
• pp.171-179
• /
• 1983

MMS와 자외선에 의한 DNA의 절제회복과 단사절단에 미치는 poly(ADP-ribose) polymerase의 저해제인 3-aminobenzamide의 영향을 CHO 세포를 재로로 조사하여 다음과 같은 결과를 얻었다. 1. MMS에 의한 비주기성 DNA 합성률과 DNA 단사 절단률은 이 저해제에 의해 모두 증가하였다. 이는 poly (ADP-ribose) polymeraserk MMS에 의해 유발된 염기 절제회복의 incision step를 억제하는 결과라 생각된다. 2. 자외선에 의한 비주기성 DNA 합성률과 DNA단사 절단률은 이 저해제에 의해 모두 감소하였다. 이는 poly(ADP-ribose) polymerase가 자외선에 의해 유발된 nucleotide 절제회복의 incision step을 돕는 작용을 하는 결과로 생각된다. 3. MMS와 자외선을 복합처리한 실험군에서는, DNA 단사 절단률은 이 저해제에 의해 영향을 받지 않았으며, 비주기성 DNA 합성률은 자외선 단독 처리군의 수준으로 증가되었다. 이는, 이 저해제가 MMS와 자외선으로 유발된 절제회복의 incision step에는 독립적으로 작용하며, 그 이후의 단계에서, MMS에 의해 부분적으로 불활성화 되었던 pyrimidine dimers의 절제를 완전하게 해주는 것으로 해석된다.

• 생명과학회지
• /
• 제12권2호
• /
• pp.219-225
• /
• 2002

진핵세포의 염색체는 전사, 복제, 회복 등의 과정에서 관여하는 단백질의 기능으로 구조가 변하게 된다. 이때 관여하는 단백질은 DNA-단백질의 상호작용에 의해서 이루어지게 되는데, 이때 단백질의 일부분은 일정한 상동성이 존재하게 된다. 이러한 부분은 motif나 domain으로 구성되는데, 예를 들면, SAP domain등을 들 수 있다. S. pombe genomic DNA 데이터베이스를 검색하여 Arabidopsis PARP 과 KU70과 상동성을 보이는 새로운 유전자를 찾았다. 이를 SAPuvs (SAP UV Sensitive)라 명명하였으며, Ura4를 선별표지로 이용하여 S. pombe SAPuvs 유전자 결실세포를 구성하였다. SAPuvs 유전자 결실세포는 자외선 조사 실험에서 정상의 세포에 비해 현저하게 죽었다. 그러나, MMS 또는 MMS와 3AB의 처리 실험에서는 저항성을 보였다. 이러한 결과로 SAPuvs는 DNA 상해회복에서 염색사구조 형성에 연관되어 있음을 확인하였다.

• 대한의생명과학회지
• /
• 제11권4호
• /
• pp.441-446
• /
• 2005

The molecular mechanism of ischemia/reperfusion injury remains unclear. Reactive oxygen species (ROS) are implicated in cell death caused by ischemia/reperfusion in vivo or hypoxia in vitro. Poly (ADP-ribose) polymerase (PARP) activation has been reported to be involved in hydrogen peroxide-induced cell death in renal epithelial cells. This study was therefore undertaken to evaluate the role of P ARP activation in chemical hypoxia in opossum kidney (OK) cells. Chemical hypoxia was induced by incubating cells with antimycin A, an inhibitor of mitochondrial electron transport. Exposure of OK cells to chemical hypoxia resulted in a time-dependent cell death. In OK cells subjected to chemical hypoxia, the generation of ROS was increased, and this increase was prevented by the $H_2O_2$ scavenger catalase. Chemical hypoxia increased P ARP activity and chemical hypoxia-induced cell death was prevented by the inhibitor of PARP activation 3-aminobenzamide. Catalase prevented OK cell death induced by chemical hypoxia. $H_2O_2$ caused PARP activation and $H_2O_2-induced$ cell death was prevented by 3-aminobenzamide. Taken together, these results indicate that chemical hypoxia-induced cell injury is mediated by PARP activation through H202 generation in renal epithelial cells.