Synthesis and Physico-chemical Properties of 1-(2-Chloroethyl)-3-(4-substituted-2, 3-dioxo-1-piperazinylalkyl)-1-nitrosourea

1-(2-Chloroethyl)-3-(4-substituted-2, 3-dioxo-1-piperazinylalkyl)-1-nitrosourea (Ia-r) were synthesized and their physico-chemical properties were examined. Along with an increase of the carbon number n between the nitrosourea moiety and the 2, 3-dioxopiperazine ring, the alkylating activity was red...

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Published inYAKUGAKU ZASSHI Vol. 99; no. 7; pp. 730 - 737
Main Authors HORI, TAKAKO, MOMONOI, KAISHU, KIBA, YASUO, YOSHIDA, CHOSAKU, SAKAI, HIROSHI, TAKENO, RYUKO, OHASHI, TOSHINORI, KISHIMOTO, SUMIKO, SAIKAWA, ISAMU
Format Journal Article
LanguageEnglish
Japanese
Published Japan The Pharmaceutical Society of Japan 01.07.1979
Subjects
2, 3-dioxopiperazinyl moiety
alkylating activity
antitumor agent
Chemical Phenomena
Chemistry
Chemistry, Physical
N-chloroethyl-N-nitrosourea derivatives
Nitrosourea Compounds - chemical synthesis
physico-chemical property
stability in aqueous solution
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Summary:1-(2-Chloroethyl)-3-(4-substituted-2, 3-dioxo-1-piperazinylalkyl)-1-nitrosourea (Ia-r) were synthesized and their physico-chemical properties were examined. Along with an increase of the carbon number n between the nitrosourea moiety and the 2, 3-dioxopiperazine ring, the alkylating activity was reduced, the stability in aqueous solution at pH 7-8 was increased, and the NH proton of the nuclear magnetic resonance spectrum was shifted to a higher field. They were not related to the 4-substitutent R of the 2, 3-dioxopiperazine ring.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0031-6903
1347-5231
DOI:10.1248/yakushi1947.99.7_730