hmao-b

hMAO-B-IN-4 is a selective, reversible and blood–brain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B, IC50=0.067 μM, Ki= 0.03 μM, hMAO-A, IC50= 33.82 μM).

hMAO-B-IN-5 is a potent reversible and selective human monoamine oxidase hMAO-B inhibitor (IC50:0.12μM). hMAO-B-IN-5 can cross the blood-brain barrier and can be used in the study of Parkinson's disease. It is a promising compound in the treatment and diagnosis of central nervous system diseases.

TB5 is a potent, selective, and reversible inhibitor of hMAO-B.

hMAO-B-IN-32 is a potent hMAO-B selective inhibitor with an IC50 of 45.52 μM.

hMAO-B-IN-10 (compound 7) is an inhibitor of MAO-A B with IC50 values of 424.1 nM and 177.9 nM, respectively. It has demonstrated neuroprotective effects in the MPTP-induced mouse model of Parkinson's Disease (PD).

hMAO-B-IN-11 (Compound 12) is a selective and reversible inhibitor of human monoamine oxidase B (hMAO-B) with an IC50 value of 0.11 µM. It operates by competitively binding to the active site of hMAO-B, thereby preventing the oxidative deamination of monoamines and reducing hydrogen peroxide production. Additionally, hMAO-B-IN-11 inhibits pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia. This compound holds potential for research in neurodegenerative diseases such as Parkinson's and Alzheimer's.

Nrf2-ARE hMAO-B QR2 modulator 1, a resveratrol derivative and multi-target-directed ligand (mtdl), activated the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibited hMAO-B and QR2（quinone reductase-2，NQO2) (IC 50 = 8.05 and 0.57 μM), and was able to promote hippocampal neurogenesis and exert neuroprotective and antioxidant effects in an Alzheimer's disease model.

hMAO-B MB-COMT-IN-1 is a dual MAO-B MB-COMT inhibitor with IC50s of 2.5 μΜ for hMAO-B and 3.84 μΜ for MB-COMT. hMAO-B MB-COMT-IN-1 protects cells from oxidative damage and can be utilized in neurodegenerative disease research, such as Parkinson's Disease (PD) [1].

hMAO-B MB-COMT-IN-2 is a dual inhibitor of MAO-B MB-COMT with IC50s of 4.27 μM and 2.69 μM for hMAO-B and MB-COMT, respectively. hMAO-B MB-COMT-IN-2 protects cells from oxidative damage and can be used in neurodegeneration disease research, such as Parkinson's Disease (PD) [1].

hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective, BBB-penetrating, and competitively reversible inhibitor of hMAO-B (IC50 = 4 nM) used in Alzheimer's disease research. hMAO-B-IN-2 exhibits good neuroprotective effects and low toxicity in SH-SY5Y cells [1].

MAO-B-IN-17 is a selective and potent monoamine oxidase B (MAO-B) inhibitor (IC50: 5.08 μM) used in the study of central nervous system disorders, including Parkinson's.

hMAO-B-IN-3 (Compound 15) is a potent hMAO-B inhibitor (IC50 = 47.4 nM) with favorable drug-like properties and a broad safety window, making it a suitable candidate for lead optimization and multitarget-directed ligand development [1].

Compound 17d (hMAO-B-IN-6) is an effective and selective hMAO-B inhibitor, demonstrating an IC 50 of 67.02 nM. It significantly ameliorates cognitive deficits induced by Scopolamine in Alzheimer's disease (AD) mice [1].

Compound 11n (hMAO-B-IN-7) is a potent inhibitor of human monoamine oxidase-B (hMAO-B) that can cross the blood-brain barrier (BBB). It demonstrates an IC 50 value of 0.79±0.05 μM and is useful in research related to Alzheimer's disease (AD) and Parkinson's disease (PD) [1].

hMAO-B-IN-9 (Compound 25c) acts as a non-competitive inhibitor of monoamine oxidase B (MAO-B), with an IC50 value of 1.58 µM (hMAO-B). Additionally, it functions as a chelator, forming complexes with iron ions which suppress ferroptosis induced by erastin. This compound exhibits antioxidant activity through the downregulation of reactive oxygen species (ROS) levels. It has also been shown to improve cognitive functions in mice without significant toxicity at a dose of 30 mg kg. Computer predictions suggest that hMAO-B-IN-9 is permeable to the blood-brain barrier.

CHBO4 is an hMAO-B inhibitor that is potent, reversible, competitive and selective.The IC50 value of CHBO4 against hMAO-B in the CHBO assay was 0.031 μM, and the Ki value was 0.010 ± 0.005 μM.CHBO4 reduces cellular damage by scavenging intracellular reactive oxygen species (ROS), and can be used to study Parkinson's disease (PD).

AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. It inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC50 values of 0.072, 9.81, 14.52, 0.024, and 2.42 μM, respectively. Additionally, AChE-IN-82 inhibits COX-1, COX-2, and 5-LOX with IC50 values of 60.41, 0.187, and 0.18 μM, respectively. The compound also demonstrates strong neuroprotective effects by significantly reducing H2O2-induced oxidative stress.

MAO-B-IN-43 (4) is a potent inhibitor of hMAO-B and a mild inhibitor of GSK3β kinase, with Ki values for hMAO-A and hMAO-B of 0.044 μM and 0.004 μM, respectively. This compound is applicable in the study of neurodegenerative diseases.

8-CSC is a dual agent endowed with good hMAO-B inhibitory activity (Ki: 235 nM in baboon liver mitochondria) and A2A affinity (Ki: 36 nM in rat brain striatal membranes receptor).

AChE BChE MAO-B-IN-1 is a reversible, non-time-dependent inhibitor of AChE, BChE, and MAO-B that crosses the blood-brain barrier, exhibiting inhibitory effects on hAChE, hBChE, and hMAO-B with IC50s of 7.31, 0.56, and 26.1 μM, respectively. [AChE BChE MAO-B-IN-1] had a neuroprotective effect and was not significantly cytotoxic.

H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor antagonist with inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B) with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. With a Ki of 170 nM for hH3R, it demonstrates favorable anti-neuropathic pain and memory-enhancing effects and can cross the blood-brain barrier (BBB) [1].

MAO-B-IN-18 is a potent, selective inhibitor of MAO B with IC50 values of 52 nM for hMAO B and 14 μM for hMAO A. It exhibits cytoprotective effects against hydrogen peroxide-induced damage in neuroblastoma and astrocyte cultures [1].

MAO-B-IN-27 (Compound 12c), a monoamine oxidase B (MAO-B) inhibitor, exhibits a potent and selective inhibitory effect on hMAO-B with an IC50 value of 8.9 nM, and is utilized in Parkinson's disease (PD) research [1].

NDs-IN-1 (Compound 3g) is a novel non-covalent multi-target inhibitor that inhibits the activities of key enzymes such as hBACE-1, hAChE, and hMAO-B, and is primarily used in the study of neurodegenerative diseases [1].