Adechlorin, a new adenosine deaminase inhibitor containing chlorine production, isolation and properties.
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 C11H15N4O4Cl. 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 1.0 mg/ml. The Ki values for adechlorin, coformycin and 2'-deoxycoformycin against adenosine deaminase were determined to be 5.3 X 10(-10) M, 2.1 X 10(-10) M and 7.6 X 10(-11) M, 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.
D000192:Actinomycetales / Q000145:classification / Q000378:metabolism; D058892:Adenosine Deaminase Inhibitors; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002713:Chlorine / Q000032:analysis; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D009700:Nucleoside Deaminases / Q000037:antagonists & inhibitors*; D009705:Nucleosides / Q000302:isolation & purification* / Q000494:pharmacology; D015649:Pentostatin / Q000031:analogs & derivatives*; D014740:Vidarabine / Q000494:pharmacology
D058892:Adenosine Deaminase Inhibitors; D009705:Nucleosides; D015649:Pentostatin; D002713:Chlorine; C046686:adechlorin; D009700:Nucleoside Deaminases; D014740:Vidarabine