Synthesis and biological activity of N-substituted aminocarbonyl-1,3-dioxolanes as VLA-4 antagonists.
A novel set of compounds with a 1,3-dioxolane ring which acts as a proline bioisostere have been successfully designed as VLA-4 receptor antagonists. Compounds (18e), (28j), and (35g) were shown to have high receptor affinities.
Rehman
Abdul
A
Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Research Laboratories, Plot 20, Sector 18, Gurgaon 122015, Haryana, India. ab_rehman@rediffmail.com
Soni
Ajay
A
Naik
Keshav
K
Nair
Sreeji
S
Palle
Venkata P
VP
Dastidar
Sunanda
S
Ray
Abhijit
A
Alam
M S
MS
Salman
Mohammad
M
Cliffe
Ian A
IA
Sattigeri
Viswajanani
V
D002460:Cell Line; D004148:Dioxolanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D039041:Integrin alpha4beta1 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D008958:Models, Molecular; D011485:Protein Binding / Q000187:drug effects; D013329:Structure-Activity Relationship
D004148:Dioxolanes; D039041:Integrin alpha4beta1; C010962:formal glycol