• 제목/요약/키워드: Triazole derivatives

검색결과 47건 처리시간 0.029초

Reactions with Heterocyclic Amidines (V). Synthesis of some new imidazo[l, 2-b] pyrazole,pyrazolo[5,1-C]-1,2,4-triazine and pyrazolo [5, 1-c]-1,2,4-triazole derivatives

  • Ali Elagamey, Abdel Ghani;Ahmed Sowellim, Salah Zaki;Mohamed Nabil, Khodeir
    • Archives of Pharmacal Research
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    • 제10권1호
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    • pp.14-17
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    • 1987
  • Several new imidazo [1, 2-b] pyrazole, pyrazolo [5, 1-c]-1, 2, 4-triazine and pyrazolo [5, 1-c] triazole derivatives were prepared from the reaction of 3-antipyrinyl-5-aminopyrazole or its diazonium salt with .alpha.-chloroacetyl derivatives.

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New Thiazolo[3,2-b][1,2,4]triazole Derivatives : Useful Compounds for the Preparation of 7-Substituted Cephalosporins

  • Nam, Ghil-Soo;Lee, Jae-Chul;Chi, Dae-Yoon;Kim, Joong-Hyup
    • Bulletin of the Korean Chemical Society
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    • 제11권5호
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    • pp.383-386
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    • 1990
  • We have synthesized several bicyclic heteroaromatic compounds with bridgehead nitrogen from N-amine salts of heteroaromatic amines. 2-Amino and 2-unsubstituted thiazolo[3,2-b][l,2,4]triazole derivatives 2a-b were prepared by the cyclization reaction from N-amine salts of aminothiazole-5-yl(N-methoxyimino)acetate with cyanogen bromide and formamidine acetic acid salt, respectively. 2-Methylthiazolo[3,2-b][1,2,4]triazole 2c was obtained from N-acetylated N-amine salt of aminothiazole-5-yl(N-methoxyimino)acetate by the cyclization reaction in the presence of polyphosphoric acid (PPA). 2-Substituted and 2-unsubstituted thiazole[3,2-b][1,2,4]triazole derivatives 2a-c were coupled with 7-aminocephalosporanic acid (7-ACA). Coupled cephalosporin derivatives 1a-c did not have good antibacterial activities in vitro.

Diastereomeric Strain-Promoted Azide-Alkyne Cycloaddition: determination of configuration with the 2D NMR techniques

  • Hye Jin Jeong
    • 한국자기공명학회논문지
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    • 제27권2호
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    • pp.10-15
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    • 2023
  • The Strain-Promoted Azide-Alkyne Cycloaddition (SPAAC) is a powerful method for synthesizing triazoles, even under physiological conditions, without a copper catalyst. This technique provides an efficient means for everyone to synthesize complex triazole derivatives rapidly. In order to investigate the configuration of triazole derivatives using bicyclo[6.1.0.]-nonyne (BCN) and chiral azide, it is necessary to employ the 2D NMR. Both 1D and 2D NMR (COSY, HSQC, 15N HMBC) are used to analyze the complex triazole product containing cyclooctyne, a diastereomeric product. The stereometric difference of the proton bonded to the same carbon is determined through the HSQC assignment. The intriguing splitting pattern of carbon resonances also reveals their diastereomeric configuration and will aid in further research based on physiological knowledge.

Synthesis and in vitro Assay of New Triazole Linked Decursinol Derivatives Showing Inhibitory Activity against Cholinesterase for Alzheimer’s Disease Therapeutics

  • Park, Jung-Youl;Shin, Sujeong;Park, Kyoung Chan;Jeong, Eunju;Park, Jeong Ho
    • 대한화학회지
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    • 제60권2호
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    • pp.125-130
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    • 2016
  • With the goal of developing Alzheimer’s disease therapeutics, we have designed and synthesized new triazole linked decursinol derivatives having potency inhibitory activities against cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)]. Since inhibition of cholinesterase (ChE) is still considered to be one of the most effective targets to treat AD patients, many new classes of ChE inhibitors have been synthesized. In an effort of identifying new type of cholinergic drug, decursinol derivatives 11-17 have been synthesized between decursinol and other biological interesting compounds such as lipoic acid, polyphenols, etc by using the click reaction and then evaluated their biological activities. Compound 12 (IC50 = 5.89 ± 0.31 mM against BuChE) showed more effective inhibitory activity against BuChE than galantamine (IC50 = 9.4 ± 2.5 mM). Decursinol derivatives can be considered a new class inhibitor for BuChE and can be applied to be a novel drug candidate to treat AD patients.

1,2,4-Triazine III : 1,2,4-Triazine 유도체의 Methiodide 염 합성과 이들 염의 고리 축소화반응에 의한 1,2,4-Triazole 유도체 합성 (1,2,4-Triazine III : Synthesis of 1-Methyl-1,2,4-triazinium Iodides and Their Ring Contraction Reaction to 1-Methyl-1,2,4-triazoles)

  • 이재근;유향선
    • 대한화학회지
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    • 제33권4호
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    • pp.419-425
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    • 1989
  • 1,2,4-Triazine 유도체들을 acetone 용매하에서 methyl iodide와 반응시켜 다양한 1-methyl-1,2,4-triazinium iodide 염을 합성하였다. 또한 이들 염을 10% NaOH 수용액 내에서 $K_3Fe(CN)_6$로 산화시킨 결과 고리 축소화반응이 일어나 1-methyl-1,2,4-triazole 유도체를 주로 얻을 수 있었으나 $C_6$에 치환기가 없을 경우는 미량이긴 하지만 1,6-dihydro-6-oxo-1,2,4-triazine 유도체도 동시에 얻을 수 있었다. 고리 축소화반응은 $OH^-$에 의해 먼저 pseudo base를 형성하고 이 Pseudo base가 1-methyl-1,2,4-triazole과 1,6-dihydro-6-oxo-1,2,4-triazine으로 진행됨을 확인할 수 있었고 또한 1,2,4-triazine의 3개의 질소원자 중 $N_1$ 원자에 quaternization됨을 확인할 수 있었다.

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6-트리아졸 엑소메칠렌펜남 유도체의 합성 (Synthesis of 6-Triazole Exomethylenepenams Derivatives)

  • 김연숙;오정석;임채욱;임철부
    • 약학회지
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    • 제48권5호
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    • pp.303-308
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    • 2004
  • The synthesis of new 6-triazole exomethylenepenams was described. The 6,6-dibromopenam 5 was reacted with $CH_3$MgBr and substituted triazole 4 to afford the 6-bromo penicillanate 6, which was treated with acetic anhydride to give acetoxy compound 7. The deacetobromination of acetoxy compound 7 with zinc and acetic acid gave 6-exomethylene penams 8 and 9, which were oxidized to sulfones 10 and 11 by m-CPBA. The p-methoxybenzyl compounds 6-11 were deprotected by AlCl$_3$ and neutralized to give the sodium salts 12-17.