• 제목/요약/키워드: Pyridine derivatives

검색결과 82건 처리시간 0.029초

소염진통제 개발 (II) - 접합 헤테로고리 화합물 - (Development of Antiinflammatory Agents(II) - Fused Heterocycles -)

  • 박노상;김현숙;임희종;정영식;최중권;함원훈
    • 약학회지
    • /
    • 제35권2호
    • /
    • pp.73-84
    • /
    • 1991
  • Quinoline, pyrazolo-[5, 4-b]-pyridine, isoxazolo-[5, 4-b]-pyridine, pyrazolo-[4, 3-c]-quinoline, isoxazolo-[5, 4-e]-thiazine, and isothiazolo-[5, 4-e]-thiazine derivatives were prepared as possible antiinflammatory agents. Some of the synthesized compounds showed antiinflammatory activities comparable to Aspirin and Naproxen.

  • PDF

Gas Phase Proton Affinity, Basicity, and pKa Values for Nitrogen Containing Heterocyclic Aromatic Compounds

  • Hwang, Sun-Gu;Jang, Yun-Hee;Chung, Doo-Soo
    • Bulletin of the Korean Chemical Society
    • /
    • 제26권4호
    • /
    • pp.585-588
    • /
    • 2005
  • Bipyridine and its derivatives have been widely used as the ligands in transition metal complexes. The proton affinities of pyridine derivatives were calculated using an ab initio quantum mechanical method (B3LYP with various double zeta and triple zeta basis sets) in combination with the Poisson-Boltzmann continuum solvation model. Van der Waals radii of the atoms in the heterocyclic rings for the solvation energy calculation were set to values determined to reproduce the $pK_a$ values of guanine and oxoguanine derivatives and that of chlorine was optimized to reproduce the experimental values of relating compounds. The $pK_a$ values for the heterocyclic ring compounds were in agreement with the experimental values with a mean unsigned error of 0.45 $pK_a$ units.

Synthesis of Several New Isoxazole, Imidazo[1, 2-a]pyridine, Imidazo[1, 2-a]pyrimidine, Benzoxadiazine and Benzothiazine Derivatives from Hydroximoyl Halides

  • Abdelhamid, Abdou O.;Abdou, Sadek E.;Mahgoub, Sayed A.
    • Archives of Pharmacal Research
    • /
    • 제15권4호
    • /
    • pp.317-321
    • /
    • 1992
  • Furoyldroximoyl chloride 3d reacted with 2-aminopyridine, 2-aminopyrimidine. O-aminophenol, O-phenylenediamine and aminothiophenol to afford imidazo [1, 2-a]pyridine 6. imidazo[1, 2-a]pyrimidine 8, benzoxadiazine 10, nitrosobenzopyrizine 13a and nitrosobenzothiazine 13b, respectively. Isoxazoline 18 and pyrrolidino[3, 4-d]isoxazolin-4, 6-dione derivatives 19a and 19b obtained by the reaction of 3 with acrylonitrile and N-arylmaleimide. Hydroximoyl chloride 3 reacted with thiophenol and sodium benzene-sulfinate to yield furylglyoxaloxime 16a and 16b, respectively. Hydroximoyl chloride 3 reacted also with some active methylene compound to give isoxazole derivatives 20-23, respectively.

  • PDF

Design. Synthesis and Antitumor Evaluation of Terpyridine Derivatives Containing Pyridines at 4'- Position

  • Lim, Hyun-Tae;Moon, Yoon-Soo;Zhao, Longxuan;Kim, Eun-Kyung;Kim, Tae-Hyung;Lee, Eung-Seok
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
    • /
    • pp.347.3-347.3
    • /
    • 2002
  • Recent study indicated that terpyridine and its derivatives displayed highly active antitumor properties. In this presentation. derivatives of terpyridines having three pyridine moieties at 2',4',6'-position of central pyridine skeleton were prepared, and evaluated their cytotoxicity against several human cancer cell lines and topoisomerase I inhibitory activities. Most of the prepared compounds showed strong cytotoxicity compared to doxorubicln. In addition. several compounds displayed better cytotoxicity than that of doxorubicin. In addition, several compounds displayed better cytotoxicity than that of doxorubicin. Structure-activity relationship study was perfomed to be indicated that [2.2':6',2']terpyidine skeleton is important to show strong xytotoxicity. Significant topoxicity. Significant topoisomerase I inhibitory activity was not observed for prepared compounds.

  • PDF

The Reaction of Digitoxin and Digoxin with Cyanoacetic Acid Hydrazide: Synthesis of Coumarin, Thiazole, Thiophene and Pyridine Derivatives with Potential Biological Activities

  • Doss, Senot H.;Wardakhan, Wagnat W.;Louca, Nadia A.
    • Archives of Pharmacal Research
    • /
    • 제24권5호
    • /
    • pp.377-384
    • /
    • 2001
  • The reaction of either Digitoxin or Digoxin with cyanoacetic acid hydrazide gave the hydrazone derivatives 3a and 3b respectively. The reactivity of the latter products towards chemical reagents was studied to give heterocyclic derivatives with potential biological activities.

  • PDF

Synthesis and In Vitro Antibacterial Activity of C-3' Pyridinium Cephalosporin Derivatives

  • Chung, In-Hwa;Kim, Choong-Sup;Seo, Jae-Hong;Chung, Bong-Young
    • Archives of Pharmacal Research
    • /
    • 제22권4호
    • /
    • pp.391-397
    • /
    • 1999
  • The quaternary ammonium cephalosporin derivatives were prepared with various pyridines substituted at the 3 or/and 4 position. Their in vitro antibacterial activities were determined and substituent effect on pyridine nucleus was studied. Preparation of substituted pyridines are also described.

  • PDF

Synthesis of 6-Formyl-pyridine-2-carboxylate Derivatives and their Telomerase Inhibitory Activities

  • Jew, Sang-Sup;Park, Boon-Saeng;Lim, Doo-Yeon;Kim, Myoung-Goo;Chung, In-Kwon;Kim, Joo-Hee;Hong, Chung-Il;Kim, Joon-Kyum;Park, Hong-Jun;Lee, Jun-Hee;Park, Hong-Jun;Lee, Jun-Hee;Park, Hyeung-Geun
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
    • /
    • pp.181.4-182
    • /
    • 2003
  • Telomeres are DNA-protein complexes at the ends of chromosomes, which play an essential protective role against DNA degradation and aberrant recombination during cell divisions. Several telomerase inhibitors have been reported as candidates for new antitumor drugs. Among them, 2-thiobenzylpyridines, developed by Geron. Co Ltd. as a telomerase inhibitor, were chosen as lead compounds. Twenty-one pyridine-2- carboxylate derivatives were prepared by the coupling of 6-formyl-2-carboxylic acid with the corresponding phenol, thiophenol, and aniline, substituted with various functional groups. (omitted)

  • PDF