Category: 75341-23-0

Yamamoto, H. published the artcileOrally active cephalosporins. Part 3: synthesis, structure-activity relationships and oral absorption of novel C-3 heteroarylmethylthio cephalosporins, Synthetic Route of 75341-23-0, the publication is Bioorganic & Medicinal Chemistry (2001), 9(2), 465-475, database is CAplus and MEDLINE.

A series of 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3-(heteroarylmethylthio)cephalosporins was designed, synthesized and evaluated for antibacterial activity and oral absorption in rats. Antibacterial activity was markedly influenced by the structure of the heteroaromatic ring moiety. Oral absorption was influenced by the heteroaromatic ring moiety as well as by the arrangement of heteroatoms. Among these compounds, FK041, 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-(hydroxyimino)acetamido]-3-[(pyrazol-3-yl)methylthio]-3-cephem-4-carboxylic acid, showed potent antibacterial activity against both Gram-pos. and Gram-neg. bacteria including Haemophilus influenzae. Further, it showed higher oral absorption than CFDN.

Bioorganic & Medicinal Chemistry published new progress about 75341-23-0. 75341-23-0 belongs to chlorides-buliding-blocks, auxiliary class Thiadiazole,Chloride, name is 2-(Chloromethyl)-5-methyl-1,3,4-thiadiazole, and the molecular formula is C17H14N2O2, Synthetic Route of 75341-23-0.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Waszkowycz, Bohdan published the artcileCell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides, Name: 2-(Chloromethyl)-5-methyl-1,3,4-thiadiazole, the publication is Journal of Medicinal Chemistry (2018), 61(23), 10767-10792, database is CAplus and MEDLINE.

DNA damage repair enzymes are promising targets in the development of new therapeutic agents for a wide range of cancers and potentially other diseases. The enzyme poly(ADP-ribose) glycohydrolase (PARG) plays a pivotal role in the regulation of DNA repair mechanisms; however, the lack of potent drug-like inhibitors for use in cellular and in vivo models has limited the investigation of its potential as a novel therapeutic target. Using the crystal structure of human PARG in complex with the weakly active and cytotoxic anthraquinone 8a, novel quinazolinedione sulfonamides PARG inhibitors have been identified by means of structure-based virtual screening and library design. 1-Oxetan-3-ylmethyl derivatives 33d and 35d were selected for preliminary investigations in vivo. X-ray crystal structures help rationalize the observed structure-activity relationships of these novel inhibitors.

Journal of Medicinal Chemistry published new progress about 75341-23-0. 75341-23-0 belongs to chlorides-buliding-blocks, auxiliary class Thiadiazole,Chloride, name is 2-(Chloromethyl)-5-methyl-1,3,4-thiadiazole, and the molecular formula is C15H20O6, Name: 2-(Chloromethyl)-5-methyl-1,3,4-thiadiazole.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Liu, Tian published the artcileA crystal structure-guided rational design switching non-carbohydrate inhibitors’ specificity between two β-GlcNAcase homologs, Product Details of C4H5ClN2S, the publication is Scientific Reports (2014), 6188, database is CAplus and MEDLINE.

Selective inhibition of function-specific β-GlcNAcase has great potential in terms of drug design and biol. research. The sym. bis-naphthalimide M-31850 was previously obtained by screening for specificity against human glycoconjugate-lytic β-GlcNAcase. Using protein-ligand co-crystallization and mol. docking, we designed an unsym. dyad of naphthalimide and thiadiazole, Q2, that changes naphthalimide specificity from against a human glycoconjugate-lytic β-GlcNAcase to against insect and bacterial chitinolytic β-GlcNAcases. The crystallog. and in silico studies reveal that the naphthalimide ring can be utilized to bind different parts of these enzyme homologs, providing a new starting point to design specific inhibitors. Moreover, Q2-induced closure of the substrate binding pocket is the structural basis for its 13-fold increment in inhibitory potency. Q2 is the first non-carbohydrate inhibitor against chitinolytic β-GlcNAcases. This study provides a useful example of structure-based rationally designed inhibitors as potential pharmaceuticals or pesticides.

Scientific Reports published new progress about 75341-23-0. 75341-23-0 belongs to chlorides-buliding-blocks, auxiliary class Thiadiazole,Chloride, name is 2-(Chloromethyl)-5-methyl-1,3,4-thiadiazole, and the molecular formula is C4H5ClN2S, Product Details of C4H5ClN2S.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics