90649-68-6

Upstream product

• 21900-53-8 2-chloro-4-methyl-benzoyl chloride 
• 1007476-32-5 sodium ethyl acetylacetate enolate 
• 108-41-8 1-chloro-3-methylbenzene 
• 75-36-5 acetyl chloride 
• 75-15-0 carbon disulfide 
• 7446-70-0 aluminium trichloride 
• 116632-42-9 2-chloro-1-iodo-4-methylbenzene 
• 21423-84-7 2-chloro-4-methylbenzonitrile 
• 75-16-1 methylmagnesium bromide 
• 7697-25-8 2-chloro-4-methylbenzoic acid 
• 108-24-7 acetic anhydride 

Downstream Products

• 134365-28-9 2-chloro-4-methyl-5-nitroacetophenone 
• 1967-31-3 2-chloroterephthalic acid 
• 1256373-61-1 1-(2-chloro-4-methylphenyl)-3-hydroxyprop-2-en-1-one 
• 871476-79-8 2-bromo-1-(2-chloro-4-methylphenyl)ethanone 
• 2043-83-6 2-chloro-4-methylphenylacetic acid 
• 86308-74-9 [2-(2-Chloro-4-methyl-phenoxy)-4-methyl-phenyl]-acetic acid 
• 51676-74-5 1-chloro-5-methyl-2,4-dinitrobenzene 

Relevant academic research and scientific papers

Design, Synthesis, and Pharmacological Evaluation of Novel β2/3 Subunit-Selective γ-Aminobutyric Acid Type A (GABAA) Receptor Modulators

Subunit-selective modulation of γ-aminobutyric acid type A receptors (GABAAR) is considered to exert fewer side effects compared to unselective clinically used drugs. Here, the β2/3 subunit-selective GABAAR modulators valerenic acid (VA) and loreclezole (LOR) guided the synthesis of novel subunit-selective ligands with simplified structures. We studied their effects on GABAARs expressed in Xenopus laevis oocytes using two-microelectrode voltage clamp technique. Five compounds showed significantly more efficacious modulation of GABA-evoked currents than VA and LOR with retained potency and selectivity. Compound 18 [(E)-2-Cyano-3-(2,4-dichlorophenyl)but-2-enamide] induced the highest maximal modulation of GABA-induced chloride currents (Emax: 3114 ± 242%), while 12 [(Z)-3-(2,4-dichlorophenyl)but-2-enenitrile] displayed the highest potency (EC50: 13 ± 2 μM). Furthermore, in hippocampal neurons 12 facilitated phasic and tonic GABAergic inhibition, and in vivo studies revealed significantly more potent protection against pentylenetetrazole (PTZ)-induced seizures compared to VA and LOR. Collectively, compound 12 constitutes a novel, simplified, and subunit-selective GABAAR modulator with low-dose anticonvulsant activity.

Anti-Malarial Agents

The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.

ANTI-MALARIAL AGENTS

The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.

Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases

The role of the tetrazole moiety in the binding of aryl thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases was explored. Different acyclic, cyclic and heterocyclic replacements were investigated in order t