Combinatorial approaches to inhibitors of VLA-4: piperazine-peptoid-bisarylureas.
A combinatorial approach towards identifying inhibitors of VALA-4 was investigated. A library of piperazine-peptoid-bisarylureas was assembled in solid phase and screening in the novel v-well assay enabled the identification of active compounds.
Lewis
I
I
Transplantation Research Chemistry Unit, S-507.3.03, Novartis Pharma, CH-4002 Basel, Switzerland. ian.lewis@pharma.novartis.com
Rohde
B
B
Mengus
M
M
Weetall
M
M
Maida
S
S
Hugo
R
R
Lake
P
P
D002851:Chromatography, High Pressure Liquid; D020650:Combinatorial Chemistry Techniques; D019992:Databases as Topic; D004121:Dimethyl Sulfoxide / Q000737:chemistry; D004126:Dimethylformamide / Q000737:chemistry; D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013058:Mass Spectrometry; D008956:Models, Chemical; D019151:Peptide Library; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry*; D034444:Peptoids; D000077489:Piperazine; D010879:Piperazines / Q000494:pharmacology*; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D012984:Software; D014230:Triazoles / Q000737:chemistry
D039041:Integrin alpha4beta1; D016023:Integrins; D019151:Peptide Library; D010455:Peptides; D034444:Peptoids; D010879:Piperazines; D016201:Receptors, Lymphocyte Homing; D014230:Triazoles; D000077489:Piperazine; D004126:Dimethylformamide; C011852:1-hydroxybenzotriazole; D004121:Dimethyl Sulfoxide