• 제목/요약/키워드: quinoline derivatives

검색결과 44건 처리시간 0.035초

Synthesis of Some Pyrimido[4,5-b]quinoline Derivatives

  • Marjani, Ahmad Poursattar;Khalafy, Jabbar;Ebrahimlo, Ali Reza Molla;Prager, Rolf.H.
    • Bulletin of the Korean Chemical Society
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    • 제32권7호
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    • pp.2183-2186
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    • 2011
  • A series of pyrimidoquinoline derivatives was synthesized in good yield and short reaction times by reaction of 3-arylaminoisoxazol-5(2H)-ones with derivatives of 2-chloro-3-formylquinoline in toluene under reflux conditions.

Fluorescence Sensing Properties of 2-(2'-Hydroxyphenyl)quinoline and Derivatives

  • Helal, Aasif;Lee, Sang-Hoon;Ren, Wen Xiu;Cho, Chan-Sik;Kim, Hong-Seok
    • Bulletin of the Korean Chemical Society
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    • 제32권5호
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    • pp.1599-1603
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    • 2011
  • Novel chemosensors based on 2-(2'-hydroxyphenyl)quinoline were prepared and evaluated for sensing metal cations. The photophysical properties of chemosensors 1-3 were examined and their ion-selectivity was evaluated by measuring their fluorescent emission responses to alkali, alkaline earth, and transition metal ions. Chemosensors 1, 2 and 3 show ratiometric and enhanced fluorescence changes with transitional metals that are efficient fluorescence quenchers, especially 3 has a high binding constant with $Hg^{+2}$ in $CH_3CN$.

Synthesis of Novel 3-Aminohydantoinyl-1.2-benzothiazine Derivatives for the COX-2 inhibitors

  • Park, Myung-Sook;Lee, Myung-Sook;Shin, Hae-Soon;Kwon, Soon-Kyoung
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.344.1-344.1
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    • 2002
  • We report the synthesis of several new 3-aminohydantoinyl-1.2-benzothiazine derivatives and propose an another mechanism of the cyclization to the hydantoins for the development candidates of COX-2 inhibitors. 3-Aminohydantoins 3a-d were prepared through cyclization of the condensation products that were formed by heating amino acids and tert-bytyl carbazate in quinoline according to the method of Lalezari. (omitted)

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Synthesis of 8-Alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-ones and Evaluation of their Anticonvulsant Properties

  • Sun, Xian-Yu;Jin, Yun-Zhe;Li, Fu-Nan;Li, Gao;Chai, Kyu-Yun;Quan, Zhe-Shan
    • Archives of Pharmacal Research
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    • 제29권12호
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    • pp.1080-1085
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    • 2006
  • A series of 8-alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-one derivatives were synthesized using 7-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and the subcutaneous pentylenetetrazole test (sc-PTZ), and their neurotoxicities were measured by the rotarod neurotoxicity test (Tox). The tests demonstrated that 8-hexyloxy-4,5-dihydro-[1.2.4]triazole[4.3-a]quinoline-1-one (4e) and 8-heptyloxy-4,5-dihydro-[1,2,4]triazole[4, 3-a]quinoline-1-one (4f) were the most potent anticonvulsants, with 4e having $ED_{50}$ values of 17.17 mg/kg and 24.55 mg/kg and protective index ($PI=TD_{50}/ED_{50}$) values of 41.9 and 29.3 in the MES and sc-PTZ tests, respectively, and 4f having $ED_{50}$ values of 19.7 mg/kg and 21.2 mg/kg and PI values of 36.5 and 33.9 in the MES and sc-PTZ tests, respectively. The PI values of 4e and 4f were many fold better than that of the marketed drugs phenytoin, carbamazepine, phenobarbital and valproate, which have PI values in the range of 1.6-8.1 in the MES test and <0.22-5.2 in the sc-PTZ test. Structure-activity relationships were also discussed.

The Synthesis of 6-(N-Arylamino)-7-Chloro-5,8-Quinolinedione Derivatives for Evaluation of Antifugal Activities

  • Ryu, Chung-Kyu;Kim, Hee-Jeong
    • Archives of Pharmacal Research
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    • 제17권3호
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    • pp.139-144
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    • 1994
  • A series of 6-(N-aylamono)-7-chloro-5, 8-quinolinedione derivatives was newly synthesized for the evaluation of antifugal activities. 5-Amino-8-hydroxy-quinoline (II) was treated with $KCLO_3$ in HCl to give 6,7-dichloro-5,8-quinolinediones (III). 6-(N-Arylamino)-7-chloro5,8-quinolinediones 1-13 were prepared by regioselective nucleophilic substitution of III with arylamines. In the presence of $CeCl_3$, the N-arylamono groups were introduced at the 6-position of 5,8-quinolinedione ring by the regioselective substitution. These derivatives 1-12 were tested for natifungal and also antibacterial activites, in vitro, against Canadida albicans, Aspergillus nier, Tricophyton mentagrophytes, Bacillus subtilis, Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coil. The MIC values were determined by the two-fold agar/steak dilution method. Newly obtained 6-(N-arylamino)-7-chloro5,8-quinolinedione derivatives showed potent antifungal and antibacterial activities. Among these derivatives, 1,3,5,7,8 and 9 showed more potent antifungal activities than fluconazole and griseofulvin. Also most of derivatives were found to be more active than ampicillin against gram-positive bacteria. 1 and 7 showed the very potent antifungal activities. 1 was the most efective in preventing the growth of Candida albicans, Aspergillus niger, Tricophyton mentagrophytes, Bacillus subtills and Staphylococcus aureus at MIC $1.6\;\mu{g/ml}$.

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이미지 센서 컬러 필터용 다이온 성분을 포함하는 신규 황색 퀴놀린 유도체 (New Yellow Quinoline Derivatives Including Dione Moiety for Image Sensor Color Filters)

  • 박선우;오세영;강유나;권혁민;대선우;이찬규;김대원;장민식;박종욱
    • 공업화학
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    • 제34권1호
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    • pp.80-85
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    • 2023
  • 이미지 센서 컬러 필터에 사용하기 위해 새로운 노란색 퀴놀린-다이온 염료 파생물을 설계하고 합성했습니다. 합성된 화합물은 퀴놀린과 디온 그룹으로 구성된 기본 화학 구조를 가지고 있습니다. 새로운 재료는 상업적 장치 제조 공정을 모방한 조건에서 광학적, 열적 특성을 기반으로 평가되었습니다. 이들의 관련 성능을 비교한 결과, 제조된 두 화합물 사이에서 2-(3-hydroxyquinolin-2(1H)-ylidene)-1H-indene-1,3(2H)-dione (HQIDO)이 다음과 같은 우수한 성능을 나타냈습니다. 프로필렌 글리콜 모노메틸 에테르 아세테이트 용매에서 0.5 wt%보다 큰 용해도, 각각 298 ℃의 높은 분해온도를 포함하는 이미지 센서 컬러 필터 재료. 결과는 HQIDO가 이미지 센서 착색제에서 노란색 염료 첨가제로 사용될 수 있음을 시사합니다.

새로이 분류된 천연 항암제 : Conjugated Dienoic Derivatives of Linoleic Acid (CLA) (Naturally-Occurring Novel Anticatcinogens : Conjugated Dienoic Derivatives of Linoliec Acid (CLA))

  • 하영래;마이클파리자
    • 한국식품영양과학회지
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    • 제20권4호
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    • pp.401-407
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    • 1991
  • 동물실험을 통하여 새로이 밝혀진 항암제(anti-initiator/anti-ptomotor)인 CLA는 grilled ground beef에서 처음 분리되었다. CLA는 grilled ground beef 외에도, cheese 및 이들 관련식품에 많이 존재한다. CLA는 반추동물의 위에 서식하는 혐기성 bacteria에 의해 linoleic acid로부터 생성되며, 식품 가공 중에서도 생성된다. 이것은 또한 in vivo에서 linoleic acid의 carbon centered free radical 형태의 산화에 의해 생성되기도 한다. CLA는 아주 강력한 항산화제임이 밝혀져, 지금까지 알려지 있지 않았는 free radical에 대응하여 membrane을 보호하는 in situ defense mechanism 역할을 한다. 이는 또한 cytochrome P450 isozyme의 활성을 저해하는 반면, ODC 효소 활성 역시 저해한다. 그래서, 적어도 CLA의 이 세가지 biological activity가 CLA 항암기작에 관여하는 것으로 생각된다.

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Regioselective Substitution of 6,7-DichloroQuinoline-5.8-dione: Synthesis, Cytotoxicity, and X-ray crystal stucture of 4a,10.11- Triazabenzo [3.2-a] fluorene-5,6-diones

  • Lee, Hyun-Jung;Park, So-Young;Lee, Chong-Ock;Suh, Myung-Eun
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.342.1-342.1
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    • 2002
  • 6.7-Dicholroquinoline-5.8-dione reacted with 2-aminopyridine derivatives, Out of the four possible products which could be achieved in this reaction. condensation and rearrangement product. 4a.10.11-triazabenzo[3.2-a] fluorine-5.6-dione was obtained as major product. The definite structure was identified with X-ray crystallographic study. (omitted)

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