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: EC:2.1.1.69 (
BMT
)
2,655
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The metabotropic glutamate receptor 5 (mGluR5) is an attractive target for the treatment of schizophrenia due to its role in regulating glutamatergic signaling in association with the
N
-methyl-d-aspartate receptor (NMDAR). We describe the synthesis of 1
H
-pyrazolo[3,4-
b
]pyridines and their utility as mGluR5 positive allosteric modulators (PAMs) without inherent agonist activity. A facile and convergent synthetic route provided access to a structurally diverse set of analogues that contain neither the aryl-acetylene-aryl nor aryl-methyleneoxy-aryl elements, the predominant structural motifs described in the literature. Binding studies suggest that members of our new chemotype do not engage the receptor at the MPEP and CPPHA mGluR5 allosteric sites.
SAR
studies culminated in the first non-MPEP site PAM, 1
H
-pyrazolo[3,4-
b
]pyridine
31
(
BMT
-145027), to improve cognition in a preclinical rodent model of learning and memory.
...
PMID:Development of 1
H
-Pyrazolo[3,4-
b
]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators. 2799 42
