[Synthesis and bioactivity of 2-arylimino-4-thiazolidones].
OBJECTIVE
To synthesize a series of 2-arylimino-4-thiazolidone derivatives and 2-imidazolino [2,3-b]-4-thiazolidone in order to get some novel potent compounds with nitric oxide synthases (NOS) inhibitory activity.


METHODS
The target compounds were prepared by reaction of N-chloroacetyl-1,2,3,4-tetrahydroisoquinoline or N-chloroacetylphthalimide with substituted thioureas, their NOS inhibitory activity were measured.


CONCLUSIONS
The 15 new compounds were synthesized and most of the reaction yields were over 65%. The structures of new compounds were identified by IR, 1H NMR, MS and elemental analyses. Bioassay indicated that, most of 15 new compounds synthesized had confirmed bioactivities inhibition against NOS.
Zhang
Da-yong
DY
School of Chemistry and Environment Science, Nanjing Normal University, Nanjing 210097, China. zhngdayong@yahoo.com
Xiang
Hua
H
Xu
Yun-gen
YG
Hua
Wei-yi
WY
D015394:Molecular Structure; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013890:Thiourea / Q000031:analogs & derivatives
D013844:Thiazoles; D019001:Nitric Oxide Synthase; D013890:Thiourea