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Literature summary for 3.4.21.37 extracted from

  • Shreder, K.R.; Cajica, J.; Du, L.; Fraser, A.; Hu, Y.; Kohno, Y.; Lin, E.C.; Liu, S.J.; Okerberg, E.; Pham, L.; Wu, J.; Kozarich, J.W.
    Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase (2009), Bioorg. Med. Chem. Lett., 19, 4743-4746.
    View publication on PubMed
Search for more literature for 3.4.21.37

Inhibitors

Inhibitors Comment Organism Structure
(3R)-1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-3-carboxylic acid
-
 Homo sapiens
(3S)-1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-3-carboxylic acid
-
 Homo sapiens
1-[3-(5-cyclobutyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
 Homo sapiens
1-[3-(5-cyclopropyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
 Homo sapiens
1-[3-(5-ethyl-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
 Homo sapiens
1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
 Homo sapiens
1-[3-(5-methyl-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
 Homo sapiens
1-[3-(7-methoxy-4-oxo-5-propyl-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
-
 Homo sapiens
1-[3-[7-methoxy-4-oxo-5-(propan-2-yl)-4H-3,1-benzoxazin-2-yl]pyridin-2-yl]piperidine-4-carboxylic acid
-
 Homo sapiens
2-(2-methoxypyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
2-(2-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]pyridin-3-yl)-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
2-(2-[[2-(dimethylamino)ethyl](methyl)amino]pyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
2-(2-[[2-(dimethylamino)ethyl]amino]pyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
2-[2-(1H-imidazol-1-yl)pyridin-3-yl]-5-methyl-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
2-[2-(4-butylpiperazin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
2-[2-(4-cyclopentylpiperazin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
2-[2-[4-(cyclopropylmethyl)piperazin-1-yl]pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
3-[4-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperazin-1-yl]propanenitrile
-
 Homo sapiens
4-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperazine-1-carboxylic acid
-
 Homo sapiens
5-chloro-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-cyclobutyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-cyclobutyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-cyclopropyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-cyclopropyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-ethyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-ethyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-ethyl-2-[2-[4-(2-hydroxyethyl)piperazin-1-yl]pyridin-3-yl]-7-methoxy-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-ethyl-7-methoxy-2-(2-[4-[2-(morpholin-4-yl)ethyl]piperazin-1-yl]pyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-ethyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-ethyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-ethyl-7-methoxy-2-[2-[4-(2-methoxyethyl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-ethyl-7-methoxy-2-[2-[4-(2-methylpropyl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methoxy-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methyl-2-(2-methylpyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methyl-2-(2-phenoxy-pyridin-3-yl)-benzo[d][1,3]oxazin-4-one development and synthesis, overview Homo sapiens
5-methyl-2-(2-phenoxyphenyl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methyl-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methyl-2-(2-[[2-(morpholin-4-yl)ethyl]amino]pyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methyl-2-(6-methylpyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methyl-2-(pyridin-3-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-methyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
5-tert-butyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
7-(dimethylamino)-5-ethyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
7-(dimethylamino)-5-ethyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-5-(propan-2-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-5-propyl-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-5-(propan-2-yl)-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-5-propyl-4H-3,1-benzoxazin-4-one
-
 Homo sapiens
additional information 2-[2-(4-methyl-piperazin-1-yl)-pyridin-3-yl] derivative inhibitor development and synthesis, structure-activity relationship study, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
neutrophil
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O
-
 Homo sapiens N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline
-
 ?

Synonyms

Synonyms Comment Organism
neutrophil elastase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000015
-
 pH 7.4, 22°C Homo sapiens 5-tert-butyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.000016
-
 pH 7.4, 22°C Homo sapiens 5-ethyl-7-methoxy-2-[2-[4-(2-methoxyethyl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.000016
-
 pH 7.4, 22°C Homo sapiens 5-ethyl-2-[2-[4-(2-hydroxyethyl)piperazin-1-yl]pyridin-3-yl]-7-methoxy-4H-3,1-benzoxazin-4-one
0.000019
-
 pH 7.4, 22°C Homo sapiens (3S)-1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-3-carboxylic acid
0.00002
-
 pH 7.4, 22°C Homo sapiens 5-ethyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.000021
-
 pH 7.4, 22°C Homo sapiens 5-ethyl-7-methoxy-2-[2-[4-(2-methylpropyl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.000021
-
 pH 7.4, 22°C Homo sapiens 2-(2-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]pyridin-3-yl)-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
0.000022
-
 pH 7.4, 22°C Homo sapiens 5-ethyl-7-methoxy-2-(2-[4-[2-(morpholin-4-yl)ethyl]piperazin-1-yl]pyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.000023
-
 pH 7.4, 22°C Homo sapiens 4-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperazine-1-carboxylic acid
0.000024
-
 pH 7.4, 22°C Homo sapiens 3-[4-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperazin-1-yl]propanenitrile
0.000025
-
 pH 7.4, 22°C Homo sapiens (3R)-1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-3-carboxylic acid
0.000027
-
 pH 7.4, 22°C Homo sapiens 2-[2-(4-butylpiperazin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
0.000028
-
 pH 7.4, 22°C Homo sapiens 5-ethyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.000028
-
 pH 7.4, 22°C Homo sapiens 1-[3-(5-ethyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
0.000028
-
 pH 7.4, 22°C Homo sapiens 2-[2-[4-(cyclopropylmethyl)piperazin-1-yl]pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
0.000034
-
 pH 7.4, 22°C Homo sapiens 2-[2-(4-cyclopentylpiperazin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-3,1-benzoxazin-4-one
0.000061
-
 pH 7.4, 22°C Homo sapiens 5-methyl-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.000064
-
 pH 7.4, 22°C Homo sapiens 2-[2-(1H-imidazol-1-yl)pyridin-3-yl]-5-methyl-4H-3,1-benzoxazin-4-one
0.000071
-
 pH 7.4, 22°C Homo sapiens 7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-5-propyl-4H-3,1-benzoxazin-4-one
0.000074
-
 pH 7.4, 22°C Homo sapiens 5-methyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.000079
-
 pH 7.4, 22°C Homo sapiens 1-[3-(5-methyl-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
0.000085
-
 pH 7.4, 22°C Homo sapiens 2-(2-methoxypyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
0.000087
-
 pH 7.4, 22°C Homo sapiens 5-methyl-2-(2-methylpyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.00011
-
 pH 7.4, 22°C Homo sapiens 5-cyclopropyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.00011
-
 pH 7.4, 22°C Homo sapiens 2-(2-[[2-(dimethylamino)ethyl](methyl)amino]pyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
0.00012
-
 pH 7.4, 22°C Homo sapiens 5-cyclopropyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.00014
-
 pH 7.4, 22°C Homo sapiens 7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-5-(propan-2-yl)-4H-3,1-benzoxazin-4-one
0.00014
-
 pH 7.4, 22°C Homo sapiens 1-[3-(5-cyclopropyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
0.00015
-
 pH 7.4, 22°C Homo sapiens 5-cyclobutyl-7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.00016
-
 pH 7.4, 22°C Homo sapiens 5-chloro-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.00017
-
 pH 7.4, 22°C Homo sapiens 5-methyl-2-(2-phenoxyphenyl)-4H-3,1-benzoxazin-4-one
0.00018
-
 pH 7.4, 22°C Homo sapiens 1-[3-(7-methoxy-4-oxo-5-propyl-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
0.00021
-
 pH 7.4, 22°C Homo sapiens 7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-5-(propan-2-yl)-4H-3,1-benzoxazin-4-one
0.00025
-
 pH 7.4, 22°C Homo sapiens 7-methoxy-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-5-propyl-4H-3,1-benzoxazin-4-one
0.00033
-
 pH 7.4, 22°C Homo sapiens 1-[3-[7-methoxy-4-oxo-5-(propan-2-yl)-4H-3,1-benzoxazin-2-yl]pyridin-2-yl]piperidine-4-carboxylic acid
0.00039
-
 pH 7.4, 22°C Homo sapiens 5-methoxy-2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.00071
-
 pH 7.4, 22°C Homo sapiens 5-methyl-2-(6-methylpyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.00085
-
 pH 7.4, 22°C Homo sapiens 5-cyclobutyl-7-methoxy-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.0009
-
 pH 7.4, 22°C Homo sapiens 5-methyl-2-(pyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.00093
-
 pH 7.4, 22°C Homo sapiens 5-methyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.0013
-
 pH 7.4, 22°C Homo sapiens 1-[3-(5-cyclobutyl-7-methoxy-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid
0.0026
-
 pH 7.4, 22°C Homo sapiens 7-(dimethylamino)-5-ethyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.0053
-
 pH 7.4, 22°C Homo sapiens 7-(dimethylamino)-5-ethyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.006
-
 pH 7.4, 22°C Homo sapiens 5-methyl-2-(2-[[2-(morpholin-4-yl)ethyl]amino]pyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.0081
-
 pH 7.4, 22°C Homo sapiens 2-(2-[[2-(dimethylamino)ethyl]amino]pyridin-3-yl)-5-methyl-4H-3,1-benzoxazin-4-one
0.0093
-
 pH 7.4, 22°C Homo sapiens 2-(2-phenoxypyridin-3-yl)-4H-3,1-benzoxazin-4-one
0.04055
-
 pH 7.4, 22°C Homo sapiens 5-ethyl-2-[2-(4-methylpiperazin-1-yl)pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.04067
-
 pH 7.4, 22°C Homo sapiens 5-ethyl-2-[2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]pyridin-3-yl]-4H-3,1-benzoxazin-4-one
0.0407
-
 pH 7.4, 22°C Homo sapiens 1-[3-(5-ethyl-4-oxo-4H-3,1-benzoxazin-2-yl)pyridin-2-yl]piperidine-4-carboxylic acid