Toward the development of chemoprevention agents (III): synthesis and anti-inflammatory activities of a new class of 5-glycylamino-2-substituted-phenyl-1,3-dioxacycloalkanes.
A new series of 5-glycylamino-2-substituted-phenyl-1,3-dioxacycloalkanes were designed and synthesized. The anti-inflammatory activities of these compounds were tested using the xylene-induced mouse ear edema model. Sixteen of these new compounds exhibited comparable or better anti-inflammatory activities than aspirin suggesting that they can be further developed as potential anti-inflammatory drug leads. In addition, treatment with these anti-inflammatory agents did not prolong tail bleeding time in mice. The structure/activity relationships were also analyzed among these compounds. Considering their good efficacy and safety profiles, some 5-glycylamino-2-substituted-phenyl-1,3-dioxacycloalkanes are worthy to be explored further in assessing the possible link between anti-inflammation and cancer prevention.
College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.
Lanrong
L
Bi
Ming
M
Zhao
Keli
K
Gu
Chao
C
Wang
Jingfang
J
Ju
Shiqi
S
Peng
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001555:Benzene Derivatives; D018890:Chemoprevention / Q000379:methods; D007249:Inflammation / Q000188:drug therapy*; D051379:Mice; D013329:Structure-Activity Relationship; D016896:Treatment Outcome
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001555:Benzene Derivatives