Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0024312 (
lymphopenia
)
4,859
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Agonism of S1P
1
receptor has been proven to be responsible for peripheral blood
lymphopenia
and elicts the identification of various S1P
1
modulators. In this paper we described a series of oxadiazole-based S1P
1
direct-acting agonists disubstituted on terminal
benzene
ring, with high potency for S1P
1
receptor and favorable selectivity against S1P
3
receptor. In addition, two representative agents named 16-3b and 16-3g demonstrated impressive efficacy in lymphocyte reduction along with reduced effect on heart rate when orally administered. Furthermore, these compounds have been shown to possess desired pharmacokinetic (PK) and physicochemical profiles. The binding mode between 16-3b and the activated S1P
1
model was also studied.
...
PMID:Identification and Structure-Activity Relationship (SAR) of potent and selective oxadiazole-based agonists of sphingosine-1-phosphate receptor (S1P
1
). 3026 73
<< Previous
1
2
