• Title/Summary/Keyword: Heterocycle

Search Result 24, Processing Time 0.02 seconds

Synthesis and Antimicrobial Evaluation of 3-(Substituted) Pyrrolidine Cephalosporins (3-(치환) 피로리딘세파로스포린의 합성과 항균활성평가)

  • 유지석;하재천;고옥현;유진철;강형룡
    • YAKHAK HOEJI
    • /
    • v.43 no.3
    • /
    • pp.306-315
    • /
    • 1999
  • To develop new cephalosporin antibiotics with improved antibacterial activities, a series of 7$\beta$-[2-(2-aminothiazol-4-y)-(Z)-2-(1-carboxy-1-methylethoxyimino)acetamido] -3-[5-(heterocycle)thiomethylpy-rrolidin-3-ylthio]methyl-3-cephem-4-carboxylic acid (14~18) having aminothiazol carboxymethylethoxy-imino group on the C-7 position and (heterocycle) thiomethyl pyrrolidinthiomethyl group on the C-3 position of the cephem ring were synthesized. These compounds were tested for antimicrobial activity in vitro against Gram(+) and Gram(-) bacteria. Compounds 15 and 16 showed remarkable antibacterial activity against Salmonella typhimurium TV119 and Alcalienes faecalis KCTC1004, but most of compounds showed lower activity than cefotaxime.

  • PDF

Synthesis of Aryloxyallylthiopyridazine Derivatives (Aryloxyallylthiopyridazine 유도체 합성)

  • 권순경;김미경
    • YAKHAK HOEJI
    • /
    • v.46 no.2
    • /
    • pp.89-92
    • /
    • 2002
  • Allylthio group of the sulfur compounds of garlic oil plays an important role for prevention and treatment of hepatic diseases induced by toxic substances or carbon tetrachloride. Thus allylthio group as pharmacologically active group was introduced into pyridazine heterocycle ring. Aryloxyallylthiopyridazine derivatives were synthesized and their hepatoprotective activities were screened in rat. The activities of these compounds were weaker than alkoxyallylthiopyridazine derivatives, which exhibit a superior hepatoprotective effect.

Stereoselective Synthesis of a Novel Cyclohexene Version of Carbovir

  • Li, Hua;Hong, Joon-Hee
    • Bulletin of the Korean Chemical Society
    • /
    • v.28 no.10
    • /
    • pp.1645-1650
    • /
    • 2007
  • This paper describes a racemic and stereoselective synthetic route for a novel cyclohexenyl carbocyclic adenine analogue. The required stereochemistry of the target compound was controlled using a stereoselective glycolate Claisen rearrangement followed by α-chelated carbonyl addition. The introduction of 6-chloropurine was achieved using Mitsunobu conditions, and further modifications of the corresponding heterocycle gave the target cyclohexenyl nucleoside.

Pyridazine Derivatives Developed as Medicines (의약품으로 개발된 Pyridazine 유도체)

  • 권순경
    • Biomolecules & Therapeutics
    • /
    • v.8 no.1
    • /
    • pp.1-12
    • /
    • 2000
  • Although the first pyridazine was obtained in 1886, this heterocycle was not thoroughly investigated such isomers as pyrimidine and pyrazine especially in the field of drug development because pyridazine derivatives do not occur as natural products. Recently medicinal chemists have an growing interest in the pyridazine derivatives, since many Pyridazine derivatives were found to possess various potential therapeutic activities. In this paper sixty-eight pyridazine derivatives, which are already introduced as medicines or are being developed as drugs were classified according to their pharmacological activities, reviewed since 1955 and the relationship of structure-activities was discussed.

  • PDF

Synthesis of Pyrimidopyrimidine by Ring Transformation of s-Triazine (s-Triazine의 Ring Transfromation에 의한 Pyrimidopyrimidine의 합성)

  • 정원근;김상기;천문우;김득준
    • YAKHAK HOEJI
    • /
    • v.28 no.2
    • /
    • pp.97-100
    • /
    • 1984
  • We have investigated the feasibility of using cyclic ambident nucleophiles in s-triazine ring transformation reaction and found that they can replace the $N_{1}-C_{2-N_{3}$ fragment of s-triazine directly in basic conditions, yielding the corresponding bicyclic products. In this paper, we described the reaction and mechanistic aspects of s-triazine to pyrimidopyrimidine transformation by 6-aminouracil derivatives. This type of ring transformation is supposed to be first attempt that deals with the successful s-triazine to bicyclic heterocycle transformation.

  • PDF