Non-steroidal pregnancy-terminating agents: design, synthesis and structure-activity relationships of 2-aryl-1,2,4-triazolo[1,5-a]pyridine.
The syntheses and the pregnancy-terminating activity relationships of compounds -n are reported. Compounds 5b and are found to be more potent than DL-111-a known drug having effective pregnancy-terminating activity in vitro. Further research shows compounds 5b and have the same activity as DL-111 in vivo. We also found an exciting result that they have excellent anti-implantation activity after oral administration.
Liu
Tao
T
Zhejiang University, Department of Medicinal Chemistry, College of Pharmacy, Hangzhou 310031, PR China.
Hu
Yongzhou
Y
D000020:Abortifacient Agents, Nonsteroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D015195:Drug Design; D010064:Embryo Implantation / Q000187:drug effects; D004622:Embryo, Mammalian / Q000187:drug effects; D003341:Luteolysis / Q000187:drug effects; D008186:Luteolytic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology
D000020:Abortifacient Agents, Nonsteroidal; D008186:Luteolytic Agents; D011725:Pyridines; D014230:Triazoles; C030266:3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1,2,4-triazole