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Literature summary for 2.5.1.47 extracted from

  • Jean Kumar, V.U.; Poyraz, O.; Saxena, S.; Schnell, R.; Yogeeswari, P.; Schneider, G.; Sriram, D.
    Discovery of novel inhibitors targeting the Mycobacterium tuberculosis O-acetylserine sulfhydrylase (CysK1) using virtual high-throughput screening (2013), Bioorg. Med. Chem. Lett., 23, 1182-1186.
    View publication on PubMed
Search for more literature for 2.5.1.47

Crystallization (Commentary)

Crystallization (Comment) Organism
identification of inhibitors by docking into crystal structure, PDB entry 2Q3C Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
4-(2-methylphenyl)-8-nitro-2-thioxo-2,3,4,4a-tetrahydro-5H-pyrimido[5,4-e][1,3]thiazolo[3,2-a]pyrimidin-5-one minimum inhibitory concentration against Mycobacterium tuberculosis 0.0335 mM, cytotoxicity against HEK 293T cell 3.6% at 0.025 mM Mycobacterium tuberculosis
4-(4-methoxyphenyl)-8-nitro-2-thioxo-2,3,4,4a-tetrahydro-5H-pyrimido[5,4-e][1,3]thiazolo[3,2-a]pyrimidin-5-one minimum inhibitory concentration against Mycobacterium tuberculosis 0.0321 mM, cytotoxicity against HEK 293T cell 0.2% at 0.025 mM Mycobacterium tuberculosis
8-nitro-4-(2-nitrophenyl)-2-thioxo-2,3,4,4a-tetrahydro-5H-pyrimido[5,4-e][1,3]thiazolo[3,2-a]pyrimidin-5-one minimum inhibitory concentration against Mycobacterium tuberculosis 0.0309 mM, cytotoxicity against HEK 293T cell 1% at 0.025 mM Mycobacterium tuberculosis
8-nitro-4-[2-(trifluoromethyl)phenyl]-4,4a-dihydro-2H-pyrimido[5,4-e][1,3]thiazolo[3,2-a]pyrimidine-2,5(3H)-dione minimum inhibitory concentration against Mycobacterium tuberculosis 0.0076 mM, cytotoxicity against HEK 293T cell 5.7% at 0.025 mM Mycobacterium tuberculosis

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WP55
-
-
Mycobacterium tuberculosis H37Rv P9WP55
-
-

Synonyms

Synonyms Comment Organism
CysK1
-
 Mycobacterium tuberculosis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0177
-
 pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 4-(2-methylphenyl)-8-nitro-2-thioxo-2,3,4,4a-tetrahydro-5H-pyrimido[5,4-e][1,3]thiazolo[3,2-a]pyrimidin-5-one
0.0177
-
 pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 8-nitro-4-[2-(trifluoromethyl)phenyl]-4,4a-dihydro-2H-pyrimido[5,4-e][1,3]thiazolo[3,2-a]pyrimidine-2,5(3H)-dione
0.0227
-
 pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 4-(4-methoxyphenyl)-8-nitro-2-thioxo-2,3,4,4a-tetrahydro-5H-pyrimido[5,4-e][1,3]thiazolo[3,2-a]pyrimidin-5-one
0.0303
-
 pH not specified in the publication, temperature not specified in the publication Mycobacterium tuberculosis 8-nitro-4-(2-nitrophenyl)-2-thioxo-2,3,4,4a-tetrahydro-5H-pyrimido[5,4-e][1,3]thiazolo[3,2-a]pyrimidin-5-one