Studies on the Development of New Angiotensin II Receptor Antagonist as the Treatment of Hypertensives

Kang-Yeoun Jung; Kun-Ho Lee

Journal of Industrial and Engineering Chemistry, Vol.3, No.1, 46-50, March, 1997

Department of Industrial Chemistry, Kangnung National University Kangnung, Kangwondo 210-702, Korea
¹Cheil Jedang Research and Development Center, 522-1 Tokpyong-ri, Majang-myon, Inchon-gun, Kyonggi-do 467-810, Korea

As the life span of mankind increases, the occurrence of various adult diseases also increases dramatically. Hypertension among them, which is being fatal for a human life, required usually a long time to treat effectively and safely. The purpose of this study is to synthesize new nonpeptide angiotensin Ⅱ receptor antagonists used for a treatment of hypertensives and to find out their biological activities. On the basis of the structure-activity relationship (SAR) of the nonpeptide angiotensin Ⅱ receptor antagonists obtained in other studies, we are trying to get a leading compound for the synthesis of new angiotensin Ⅱ receptor antagonists, specially imidazopyridine derivatives, which are showing an excellent biological activity and low toxicity in the treatment of hypertensives.

[References]

Duncia JV, Chiu AT, Carini D, Johnson AL, Price WA, Wong PC, Wexler RR, Timmermans PBMWM, Med. Res. Rev., 12, 149 (1992)
Inada Y, Wada T, Shibouta Y, Ojima M, Sanada T, Ohtsuki K, Itoh K, Kubo K, Kohara Y, Naka T, Nishikawa K, J. Pham. Experimental Therapeutics, 268, 1540 (1994)
Chang RSL, Siegl PKS, Clineschmidt BV, Mantlo NB, Chakravarty PK, Greenlee WJ, Patchett AA, Lotti VJ, J. Pham. Experimental Therapeutics, 262, 133 (1992)
Peach MJ, Physiol. Rev., 57, 313 (1977)
Furakawa Y, Kishimoto S, Nishikawa K, U.S. Patent, 4,340,598 (1982)
Furakawa Y, Kishimoto S, Nishikawa K, U.S. Patent, 4,355,040 (1982)
De B, Winn M, Zydowsky TM, Kerkman DJ, Debernardis JF, Lee J, Buckneer S, Warner R, Brune M, Hancock A, Opgenorth T, Marsh K, J. Med. Chem., 35, 3714 (1992)
Wisansky WA, Ansbacher S, Org. Synth., 138 (1955)
Moriarty RM, J. Org. Chem., 29, 2748 (1964)
The synthetic procedureand authentic sample were obtained from Cheil Jedang Research Center. Representative method for the biphenyltetrazole bromide (BPT-Br) is described in experimental section
Experimental data was obtained from the pharmacology team of Cheil Jedang Research Center
Synthetic material were obtained and tested at Cheil Jedang Research Center

[Related Articles]

[1] Duncia JV, Chiu AT, Carini D, Johnson AL, Price WA, Wong PC, Wexler RR, Timmermans PBMWM, Med. Res. Rev., 12, 149 (1992)

[2] Inada Y, Wada T, Shibouta Y, Ojima M, Sanada T, Ohtsuki K, Itoh K, Kubo K, Kohara Y, Naka T, Nishikawa K, J. Pham. Experimental Therapeutics, 268, 1540 (1994)

[3] Chang RSL, Siegl PKS, Clineschmidt BV, Mantlo NB, Chakravarty PK, Greenlee WJ, Patchett AA, Lotti VJ, J. Pham. Experimental Therapeutics, 262, 133 (1992)

[4] Peach MJ, Physiol. Rev., 57, 313 (1977)

[5] Furakawa Y, Kishimoto S, Nishikawa K, U.S. Patent, 4,340,598 (1982)

[6] Furakawa Y, Kishimoto S, Nishikawa K, U.S. Patent, 4,355,040 (1982)

[7] De B, Winn M, Zydowsky TM, Kerkman DJ, Debernardis JF, Lee J, Buckneer S, Warner R, Brune M, Hancock A, Opgenorth T, Marsh K, J. Med. Chem., 35, 3714 (1992)

[8] Wisansky WA, Ansbacher S, Org. Synth., 138 (1955)

[9] Moriarty RM, J. Org. Chem., 29, 2748 (1964)

[10] The synthetic procedureand authentic sample were obtained from Cheil Jedang Research Center. Representative method for the biphenyltetrazole bromide (BPT-Br) is described in experimental section

[11] Experimental data was obtained from the pharmacology team of Cheil Jedang Research Center

[12] Synthetic material were obtained and tested at Cheil Jedang Research Center