41931-13-9

Usage

Uses

LCS 1 is an inhibitor of Superoxide Dismutase 1 (SOD1).

Biochem/physiol Actions

LCS-1 is an inhibitor of superoxide dismutase (SOD1). LCS-1 inhibits the proliferation of lung adendocarcinoma cell lines.

InChI:InChI=1/C11H8Cl2N2O/c1-7-3-2-4-8(5-7)15-11(16)10(13)9(12)6-14-15/h2-6H,1H3

Upstream product

• 90351-49-8 mucochloric acid 
• 536-89-0 m-tolylhydrazine 
• 766-40-5 Mucochloric acid 

Downstream Products

• 1035450-98-6 5-chloro-4-(diethylamino)-2-(3-methylphenyl)pyridazin-3(2H)-one 
• 1035451-00-3 4-chloro-5-(diethylamino)-2-(3-methylphenyl)pyridazin-3(2H)-one 
• 1035451-05-8 4-chloro-5-ethoxy-2-(3-methylphenyl)pyridazin-3(2H)-one 
• 1035451-09-2 5-iodo-2-(3-methylphenyl)pyridazin-3(2H)-one 
• 1035451-07-0 4,5-diiodo-2-(3-methylphenyl)pyridazin-3(2H)-one 
• 1035451-02-5 5-azido-4-chloro-2-(3-methylphenyl)pyridazin-3(2H)-one 
• 1415356-22-7 C₁₈H₁₅ClN₂O₃ 

Relevant academic research and scientific papers

Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7)

Novel small molecule antagonists of NPBWR1 (GPR7) are herein reported. A high-throughput screening (HTS) of the Molecular Libraries-Small Molecule Repository library identified 5-chloro-4-(4-methoxyphenoxy)-2-(p-tolyl) pyridazin-3(2H)-one as a NPBWR1 hit antagonist with micromolar activity. Design, synthesis and structure-activity relationships study of the HTS-derived hit led to the identification of 5-chloro-2-(3,5-dimethylphenyl)-4-(4-methoxyphenoxy) pyridazin-3(2H)-one lead molecule with submicromolar antagonist activity at the target receptor and high selectivity against a panel of therapeutically relevant off-target proteins. This lead molecule may provide a pharmacological tool to clarify the molecular basis of the in vivo physiological function and therapeutic utility of NPBWR1 in diverse disease areas including inflammatory pain and eating disorders.

Discovery and structure-activity relationship analysis of Staphylococcus aureus sortase A inhibitors

Methicillin resistant Staphylococcus aureus (MRSA) is a major health problem that has created a pressing need for new antibiotics. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Using high-throughput screening, we have identified several compounds that inhibit the enzymatic activity of the SrtA. A structure-activity relationship (SAR) analysis led to the identification of several pyridazinone and pyrazolethione analogs that inhibit SrtA with IC50 values in the sub-micromolar range. Many of these molecules also inhibit the sortase enzyme from Bacillus anthracis suggesting that they may be generalized sortase inhibitors.

PYRIDAZINONES AND FURAN-CONTAINING COMPOUNDS

The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.