Accession Number : ADB109523

Title :   Antiradiation Drugs without Amino Groups.

Descriptive Note : Annual summary rept. no. 1, 1 Jun 85-31 May 86,

Corporate Author : VANDERBILT UNIV NASHVILLE TN DEPT OF CHEMISTRY

Personal Author(s) : Chandra, R. ; Field, L. ; Lee, C. ; Macke, J. D. ; Singh, P. K.

Report Date : JUN 1986

Pagination or Media Count : 38

Abstract : In synthetic work aimed at the synthesis of novel antiradiation agents that contain no nitrogen, 21 submissions have been made for biological testing. These included representative alkanesulfinates terminated by a variety of polar, non-polar, and sulfur-containing functions. With RSS(CH2)nSO2Na as the formulation of this broad class, five compounds each were propanesulfinates (n=3) and pentanesulfinates (n=5); R (n=3 or 5) was NaO2S(CH2)nS-,HO2C(CH2)2-, p-CH3C6H4-, C6H5- and NaO2S(CH2)nSS (CH2)4. These 10 compounds, with similar ones where n was 4 should afford a good basis for conclusions about structure-activity relations in this promising series. 1-Adamantyl and 9-fluorenyl p-toluenesulfinates were submitted as models for crystalline esters which are desired of sulfinates like the foregoing. A disulfide-sulfinate of the structure R superscript 1 SS(CH2)2S(O)R superscript 2 was submitted to determine whether sulfoxide functions can be desirable substitutes for sulfinate functions in exercising the postulated neighboring-group effect on -S sub n- functions in the same molecule. Studies in process are described in efforts to develop unsaturated counterparts of active agents as well as counterparts containing aromatic rings and a promising aminoalkyl type of R group.

Descriptors :   *RADIOPROTECTIVE AGENTS, SYNTHESIS(CHEMISTRY), ALKANES, PROPANE, PENTANES, TOLUENES, SULFOXIDES, AMINES, BIOLOGY, TEST METHODS, NITROGEN, AROMATIC COMPOUNDS, RINGS, CRYSTALS, ESTERS, SULFINATES.

Subject Categories : Pharmacology
      Organic Chemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE