Adechlorin, a new adenosine deaminase inhibitor containing chlorine production, isolation and properties

Abstract

Adechlorin exhibiting a potent inhibitory activity against calf intestinal adenosine deaminase was isolated from the cultured broth of Actinomadura sp. OMR-37. The molecular formula was C11H15N4O4C1. The aglycone of adechlorin was identical with that of the known adenosine deaminase inhibitors coformycin and 2'-deoxycoformycin. Adechlorin did not exhibit inhibitory activity against various bacteria and fungi at 1.0mg/ml. The Ki values for adechlorin, coformycin and 2'-deoxycoformycin against adenosine deaminase were determined to be 5.3X10-10M, 2.1X10-10M and 7.6X10-11M, respectively. Adechlorin as well as coformycin and 2'-deoxycoformycin enhanced the antiviral activity of Ara-A. The acute toxicity of adechlorin in mice was less than those of coformycin and 2'-deoxycoformycin. © 1985, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.