34000-31-2

Upstream product

• 118-93-4 o-hydroxyacetophenone 
• 123-08-0 4-hydroxy-benzaldehyde 
• 111391-32-3 (E)-3-(4-(benzyloxy)phenyl)-1-(2-hydroxyphenyl)prop-2-en-1-one 
• 100-52-7 benzaldehyde 
• 100-83-4 meta-hydroxybenzaldehyde 
• 582-24-1 1-phenyl-2-hydroxyethanone 
• 18962-05-5 4-isopropoxybenzaldehyde 
• 204703-70-8 1-(2-(tetrahydro-2H-pyran-2-yloxy)phenyl)ethanone 
• 74189-56-3 4-(tetrahydropyran-2-yloxy)benzaldehyde 
• 6515-21-5 4-methoxymethoxy-benzaldehyde 
• 4397-53-9 p-benzyloxybenzaldehyde 
• 928634-31-5 (E)-1-(2-hydroxyphenyl)-3-[4-(methoxymethoxy)phenyl]-2-propen-1-one 
• 6515-18-0 1-[2-(methoxymethoxy)phenyl]ethanone 
• 130600-79-2 (E)-1-(2-Hydroxy-phenyl)-3-[4-(tetrahydro-pyran-2-yloxy)-phenyl]-propenone 

Downstream Products

• 112980-31-1 (2Z)-2-[(4-hydroxyphenyl)methylidene]benzofuran-3-one 
• 6515-37-3 2-(4-hydroxyphenyl)chroman-4-one 
• 4143-63-9 4'-hydroxyflavone 
• 71809-05-7 1-(2-hydroxyphenyl)-3-(4-hydroxyphenyl)propane 
• 421573-08-2 3-(2-hydroxyphenyl)-5-(4-hydroxyphenyl)-4,5-dihydro-1H-pyrazole 
• 1250377-70-8 4-(2-fluorophenyl)-1-[1-(2-hydroxyphenyl)-3-phenylallylidene]semicarbazide 
• 7508-30-7 2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromen-4-ol 
• 201424-65-9 3-(4-hydroxybenzyl)-chroman-4-one 
• 24271-94-1 1-(2-hydroxyphenyl)-3-(4-hydroxyphenyl)-propan-1-one 
• 24389-48-8 2-(4-hydroxybenzylidene)benzofuran-3(2H)-one 

Relevant academic research and scientific papers

Glycolytic inhibition and antidiabetic activity on synthesized flavanone scaffolds with computer aided drug designing tools

Background: Diabetes mellitus is a challengeable metabolic disorder that leads to a group of complications when the HbA1c level is not maintained. Most of the existing drugs avail-able in the market in long-term use may lead to serious adverse effects. He

Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition

In this study, we have designed and synthesized pyrazoline analogues that partially mimic the structure of mycobactin, to address the requirement of novel therapeutics to tackle the emerging global challenge of antimicrobial resistance (AMR). Our investigation resulted in the identification of novel lead compounds 44 and 49 as potential mycobactin biosynthesis inhibitors against mycobacteria. Moreover, candidates efficiently eradicated intracellularly surviving mycobacteria. Thermofluorimetric analysis and molecular dynamics simulations suggested that compounds 44 and 49 bind to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway. To the best of our knowledge, these are the first rationally designed mycobactin inhibitors to demonstrate an excellent in vivo pharmacokinetic profile. In addition, these compounds also exhibited more potent whole-cell efflux pump inhibition than known efflux pump inhibitors verapamil and chlorpromazine. Results from this study pave the way for the development of 3-(2-hydroxyphenyl)-5-(aryl)-pyrazolines as a new weapon against superbug-associated AMR challenges.

A Convenient One-Pot Synthesis of Chalcones and Their Derivatives and Their Antimicrobial Activity

Abstract: A series of chalcones were synthesized by base-catalyzed Clasien-Schmidtcondensation of substituted benzaldehydes and substituted acetophenones at roomtemperature. The addition of hydrazine hydrate and hydroxylamine hydrochlorideacross the double bond of the obtained chalcones gave pyrazole and isoxazolederivatives, respectively. All the synthesized compounds were characterized by1H and 13C NMR andFT-IR spectroscopy and screened for their in vitro antimicrobial activityagainst two bacterial strains, Pseudomonasaeruginosa and Pseudomonasoryzihabitans using Ciprofloxacin as standard drug.1-(2-Methoxyphenyl)-3-phenylprop-2-en-1-one and1-(4-chlorophenyl)-3-phenylprop-2-en-1-one showed significant activity againstboth bacterial strains and hence proved to be potent antimicrobialagents.

Natural product-based design, synthesis and biological evaluation of 2′,3,4,4′-tetrahydrochalcone analogues as antivitiligo agents

A bioactive component, 2′,3,4,4′-tetrahydrochalcone (RY3-a) was first isolated from Vernohia anthelmintica (L.) willd seeds, and a set of its analogs, RY3-a-1–RY3-a-15 and RY3-c were designed and synthesized. Biological activity assays showed that RY3-c exhibited better melanogenesis and antioxidant activity and lower toxicity in comparison with RY3-a and butin. Further study tests showed that RY3-c exhibited better melanogenesis activity compared with the positive control 8-methoxypsoralan (8-MOP) in a vitiligo mouse model, suggesting that RY3-c is a good candidate antivitiligo agent. Mechanistic studies showed that RY3-c could repair cell damage induced by excessive oxidative stress and may exert melanin synthesis activity in the mouse melanoma B16F10 cell line by activating the mitogen-activated protein kinase (MAPK) pathway and the upregulation of c-kit.

Exploration of synthetic antioxidant flavonoid analogs as acetylcholinesterase inhibitors: an approach towards finding their quantitative structure–activity relationship

The binding interactions between acetylcholinesterase (AChE) and a series of antioxidant flavonoid analogs were studied by fluorescence spectroscopic assay. The present study incorporated different classes of naturally occurring and synthetic flavonoid compounds like flavones, isoflavones, and chalcones as well as a few standard antioxidants. The AChE inhibitory (AChEI) activity of these compounds was further analyzed using in silico techniques, namely pharmacophore mapping, quantitative structure–activity relationship (QSAR) analysis, and molecular docking studies. We have also compared the AChE inhibitory and radical scavenging antioxidant activities of these compounds. Both the AChE inhibitory and antioxidant activities of these compounds were found to be highly dependent on their structural patterns. However, it was observed that, in general, flavones are comparatively better AChE inhibitors as well as antioxidants compared to chalcones. [Figure not available: see fulltext.].

Phototransformations of some 3-cyclohexenyloxychromenones: Synthesis of Spirocyclic compounds

The phototransformation of the 3-cyclohexenyloxychromenones by irradiation with a pyrex-filtered light from a 125 W Hg vapor lamp under an inert atmosphere into the spirocyclic fused xanthenones was described. The efficacy of the protocol depended upon th

Synthesis, characterization and antimicrobial evaluation of cobalt(III) complexes of 4-(2-substituted phenylimino)-2-(4-substituted phenyl)-4H-chromen-3-ol

A series of eight Co(III) complexes [CoL1-8(H2O)2Cl] (I-1 to I-8) incorporating 4-(2-substituted phenylimino)-2-(4-substituted phenyl)-4H-chromen-3-ol, as a tridentate imino flavone ligands (L1 to L8, 2-sub. = NH2, SH, 4-sub. = OMe, OH, Cl, NMe2) have been synthesized, characterized and the geometry of the complexes were optimized by DFT. The chemical structure of synthesized imino flavone ligands and their complexes were characterized by elemental analysis, 1H NMR, 13C NMR, UV-visible, IR, ESI-mass spectral data, conductometric and magnetic measurements. The synthesized compounds have been screened for their in vitro antibacterial activities against bacteria Vibrio cholerae, Salmonella typhi, Staphylococcus aureus, Escherichia coli and antifungal activities against fungi Candida albicans and Aspergillus flavus by paper disc diffusion method. The complexes I-3, I-4, I-7 and I-8 showed good antimicrobial activities against pathogens.

Synthesis, Structure, and Anti-Inflammatory Activity of Functionally Substituted Chalcones and Their Derivatives

Functionally substituted chalcones, pyrazolines, and flavonones have been synthesized. Their structure has been studied by means of 1H and 13C NMR spectroscopy, including COSY and HMQC experiments. Anti-inflammatory activity of the s

Design, synthesis and biological evaluation of novel dihydropyrimidine-2-thione derivatives as potent antimicrobial agents: Experimental and molecular docking approach

Introduction: Dihydropyrimidine scaffold represent an important class of pharmacologically active nitrogen containing heterocyclic compounds. A wide range of molecules with dihydropyrimidine moieties have important role in medicinal chemistry on account of their potential biological activities. Methodology: A series of 3,4-dihydropyrimidine-2(1H)-thione derivatives have been designed and synthesized in a concise way through condensation of variously substituted chalcones with thiourea in alkaline alcoholic solutions. In order to investigate their biological significance, these compounds were tested for their in vitro antimicrobial potential against various bacterial and fungal strains. Moreover, the experimental results were supported by molecular docking studies. Results and Discussion: The newly synthesized compounds were characterized by the usual spectroscopic techniques In case of antibacterial activity, the compounds 5 (40.3±0.44 mm), 12 and 13 (almost 35 mm) exhibited highest zone of inhibitions against Methicillin-resistant Staphylococcus auerus (MRSA) bacterial strain as compared to the standard drug Cefixime. These compounds displayed moderate to good activities against all attempted fungal strains. In docking analysis, it has been observed that compounds 8 (-6.4017 Kcal/mol) and 10 (-6.1319 Kcal/mol) revealed significant binding affinity against penicillin binding protein (PDB ID: 1VQQ), while compounds 1 (-143.23 Kcal/mol) and 2 (-146.99 Kcal/mol) showed best activity for shikimate dehydrogenase (PDB ID: 3DON). Conclusion: In conclusion, we have designed, synthesized and characterized an interesting series of biologically active dihydropyrimidine derivatives. Remarkably, most of the synthesized compounds were found more active against all tested bacterial strains in comparison to the standard drug Cefixime as manifested by experimental as well as theoretical results.

NOTCH INHIBITORS FOR USE IN THE TREATMENT OF T-CELL ACUTE LYMPHOBLASTIC LEUKEMIA

Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL).