154419-89-3

Upstream product

• 136786-72-6 5-(4-Methoxy-phenyl)-3-thiophen-2-yl-4,5-dihydro-1H-pyrazole 
• 79-04-9 chloroacetyl chloride 
• 88-15-3 2-Acetylthiophene 
• 123-11-5 4-methoxy-benzaldehyde 
• 6028-93-9 (2E)-3-(4-methoxyphenyl)-1-(thiophen-2-yl) prop-2-en-1-one 

Relevant academic research and scientific papers

Fighting against alzheimer’s disease: Synthesis of new pyrazoline and benzothiazole derivatives as new acetylcholinesterase and MAO inhibitors

Background: Alzheimer’s Disease (AD) is a complicated neurodegenerative disorder with a multifaceted pathogenesis.AD, characterized by gradual memory loss, falling in language ability and other cognitive deterioration, and has been a prominent risk to ageing population. This means that there is an urgent need to find new lead compounds for controlling and fighting against (AD). In this way, a new thiophene-2-pyrazoline derivatives (A1-A5) and benzothiazole derivatives (A6-A13) have been synthesized to give beneficial compounds to controlling and battling against (AD). Results: Compounds A5 and A13 showed the most remarkable activity with an 18.53 μM and 15.26 μM IC50 values against AChE enzyme. In like manner, compound A4 was active with a 20.34 μM IC50 value against MAO-A. These active compounds are in fact non-toxic making them very attractive for additional future studies. Enzyme kinetic was analyzed and the Lineweaver-Burk plot reveals that compound A13 was typically mixed AChE inhibitors, which showed significant similarity to donepezil. In addition, the best docking pose was done by analyzing the docking pattern of the most active compound A13 which was very compatible with the gorge and in interaction with both CAS and PAS. Conclusion: The synthesis of new thiophene-2-pyrazoline and benzothiazole derivatives targeting AChE/(MAO-A)/(MAO-B) enzymes was described. The selection of enzyme-kinetic analysis, molecular docking and toxicity test was led to good understanding to the therapeutic potential for the active derivatives. Therefore, these compounds may be accepted as promising leads for future research efforts in fighting against AD.

Synthesis of some 1-[(N,N-disubstituted thiocarbamoylthio)acetyl]-3-(2- thienyl)-5-aryl-2-pyrazoline derivatives and investigation of their antibacterial and antifungal activities

Fourteen new 1-[(N,N-disubstituted thiocarbamoylthio)acetyl]-3-(2-thienyl)- 5-aryl-2-pyrazoline derivatives (7a-n) were synthesised by reacting 1-(chloroacetyl)-3-(2-thienyl)-5-aryl-2-pyrazolines (5a-g) and appropriate sodium salts of N,N-disubstituted dithiocarbamoic acids (6a, b). The structures of the synthesised compounds were confirmed by elemental analyses, UV, IR, 1H-NMR and FAB+-MS spectral data. Their antibacterial activities against Proteus vulgaris (NRRL B-123), Escherichia coli (NRRL B-3704), Aeromonas hydrophila (Ankara University, Faculty of Veterinary Sciences), Salmonella typhimurium (NRRL B-4420), Streptococcus feacalis (NRRL B-14617), Micrococcus luteus (NRLL B-4375) were investigated and in this investigation, a significant level of activity was illustrated. Antifungal activities of the compounds against Candida albicans and Candida globrata (isolates obtained from Osmangazi Uni. Fac. of Medicine) were found to be inactive. Compounds 7c-n were also evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system and BACTEC 12B medium. The preliminary results indicated that all of the tested compounds were inactive against the test organism.

N-Derivatisation of some 3-(2-furyl)- and 3-(2-thienyl)-5-aryl-2-pyrazolines

A series of twenty six N-derivatised 3-(2-furyl)- and 3-(2-thienyl)-5-arylpyrazolines of general structure 2 has been prepared by the reactions of 2 (X=O,S) with suitable reagents.The structures of the compounds have been established by elemental analyses and spectral (IR, PMR) data.