Accession Number : ADB101203

Title :   Synthesis of Potential Prophylactic Antiradiation Agents.

Descriptive Note : Annual progress rept. 1 Jul 83-30 Jun 84,

Corporate Author : SOUTHERN RESEARCH INST BIRMINGHAM AL

Personal Author(s) : Piper, James R. ; Kussner, Conrard L.

Report Date : MAY 1985

Pagination or Media Count : 55

Abstract : This report consists of accounts of efforts to identify improved antiradiation agents. The primary goal remains to find modifications fo S-2-(3-aminopropyl-amino)ethyl dihydrogen phosphorothioate (WR-2721) and related radioprotective compounds that will be less toxic, longer lasting, and effective when administered orally. The work done during this report period dealt with compounds from two broad areas, phosphorothioates and thiazolidines, each of which may be regarded as latentiated derivatives of aminothiols. Seven potential radioprotectants of the phosphorothioate class whose syntheses were completed represented a continuation of structure-activity-relationship studies on carboxy- and also hydroxy-substituted analogues of WR-2721 and additional S-omega-aminoalkylamino) alkyl dihydrogen phosphorothioates. Thiazolidine derivatives were prepared from four selected diaminothiols and two carbonyl compounds, formaldehyde and D-glucose. The diaminothiols used were prepared via their phosphorothioates, which were selected for this purpose from among the best of the known radioprotective agents. The antiradiation test results provided by Walter Reed Army Institute of Research revealed some activity among phosphorothioates administered intraperitoneally, but no activity was observed in the thiazolidines.

Descriptors :   *RADIOPROTECTIVE AGENTS, *PHARMACOLOGY, CARBONYL COMPOUNDS, FORMALDEHYDE, PHOSPHOROTHIOATES, RADIATION, SYNTHESIS, ORAL DOSAGE, SYNTHESIS(CHEMISTRY), PREVENTIVE MEDICINE, ARMY RESEARCH, MEDICAL RESEARCH, MILITARY MEDICINE.

Subject Categories : Pharmacology
      Organic Chemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE