YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Active Conformation of Thromboxane $A_2$ and Thromboxane $A_2$ Receptor Antagonists

트롬복산 $A_2$와 트롬복산 $A_2$ 수용체 길항제의 활성형태

  • Lee, Jong-Dal (Department of Pharmacy, College of Pharmacy, Yeungnam University) ;
  • Doh, Seong-Tak (Department of Clinical Pathology, Taegu Junior Health College)
  • 이종달 (영남대학교 약학대학 약학과) ;
  • 도성탁 (대구보건전문대학 임상병리과)
  • Published : 1997.12.01
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Abstract

Conformational analyses on thromboxane $A_2$ (Tx$A_2$) and thromboxane $A_2$ receptor antagonists (TxRA) were carried out by molecular mechanics method. Based on the assumption that active conformer is the nonintrahydrogen bonding and more stable former of Tx$A_2$ and TxRA, the molecular structural requirements for potent TxA2 receptor antagonists are like below: 1) The distance is 5.0-5.6${\AA}$ between C atom of carboxyl group and S atom of sulfonyl group or C atom which is bonded to hydroxyl group in the active conformers. 2) The putative active conformers of Tx$A_2$and TxRAs are hairpin-like forms.

Keywords

References

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