199938-23-3

Upstream product

• 79-04-9 chloroacetyl chloride 
• 5933-32-4 4-bromobenzoic acid hydrazide 
• 79-11-8 chloroacetic acid 
• 5798-75-4 Ethyl 4-bromobenzoate 
• 586-76-5 4-Bromobenzoic acid 
• 619-42-1 4-methoxycarbonylphenyl bromide 

Downstream Products

• 568544-04-7 2-(4-bromophenyl)-5-(chloromethyl)-1,3,4-oxadiazole 
• 871583-96-9 benzyl{[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]methyl}[(6-methoxy-3-nitropyridin-2-yl)methyl]amine 
• 911062-10-7 3-(4-bromophenyl)-4-(4-methoxyphenyl)-5-(1H-pyrazol-1-ylmethyl)-4H-1,2,4-triazole 
• 911062-06-1 5-[3-(4-bromophenyl)-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl]-2-methoxypyridine 
• 911061-99-9 2-(4-bromophenyl)-5-(1H-pyrazol-1-ylmethyl)-1,3,4-oxadiazole 
• 911061-96-6 2-(4-bromophenyl)-5-(methoxymethyl)-1,3,4-oxadiazole 
• 871583-86-7 1-(4-bromophenyl)-8-methoxy-4H,6H-[1,2,4]triazolo[4,3-a][4,1]benzoxazepine 
• 871583-95-8 2-benzylaminomethyl-5-(4-bromophenyl)-1,3,4-oxadiazole 

Relevant academic research and scientific papers

Synthesis and biological evaluation of honokiol derivatives bearing 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)oxazol-2(3h)-ones as potential viral entry inhibitors against sars-cov-2

The 2019 coronavirus disease (COVID-19) caused by SARS-CoV-2 virus infection has posed a serious danger to global health and the economy. However, SARS-CoV-2 medications that are specific and effective are still being developed. Honokiol is a bioactive component from Magnoliae officinalis Cortex with damp-drying effect. To develop new potent antiviral molecules, a series of novel honokiol analogues were synthesized by introducing various 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)oxazol-2(3H)-ones to its molecule. In a SARS-CoV-2 pseudovirus model, all honokiol derivatives were examined for their antiviral entry activities. As a result, 6a and 6p demonstrated antiviral entry effect with IC50 values of 29.23 and 9.82 μM, respectively. However, the parental honokiol had a very weak antiviral activity with an IC50 value more than 50 μM. A biolayer interfero-metry (BLI) binding assay and molecular docking study revealed that 6p binds to human ACE2 protein with higher binding affinity and lower binding energy than the parental honokiol. A competitive ELISA assay confirmed the inhibitory effect of 6p on SARS-CoV-2 spike RBD’s binding with ACE2. Importantly, 6a and 6p (TC50 > 100 μM) also had higher biological safety for host cells than honokiol (TC50 of 48.23 μM). This research may contribute to the discovery of potential viral entrance inhibitors for the SARS-CoV-2 virus, although 6p’s antiviral efficacy needs to be validated on SARS-CoV-2 viral strains in a biosafety level 3 facility.

OXADIAZINONE COMPOUNDS FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES

The present invention includes name compounds of general formula (I) in which R1, Y, and R3 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compos

One-potCuAAC synthesis of (1H-1,2,3-triazol-1-yl)methyl-1,3,4/1,2,4-oxadiazoles starting from available chloromethyl-1,3,4/1,2,4-oxadiazoles

The one-pot CuAAC synthesis of (1H-1,2,3-triazol-1-yl)methyl-1,3,4-oxadiazole and (1H-1,2,3-triazol-1-yl)methyl-1,2,4-oxadiazole derivatives via three-component reaction of consequent nucleophilic substitution of chlorine, with azide, and its further “cli

Design and synthesis of new norfloxacin-1,3,4-oxadiazole hybrids as antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA)

Toward the search of new antibacterial agents to control methicillin-resistant Staphylococcus aureus (MRSA), a class of new norfloxacin-1,3,4-oxadiazole hybrids were designed and synthesized. Antibacterial activities against drug-sensitive bacteria S. aureus and clinical drug resistant isolates of MRSA were evaluated. Compound 5k exhibited excellent antibacterial activities against S. aureus (MIC: 2 μg/mL) and MRSA1–3 (MIC: 0.25–1 μg/mL). The time-kill kinetics demonstrated that compound 5k had an advantage over commonly used antibiotics vancomycin in killing S. aureus and MRSA. Moreover, compound 5k could inhibit the bacteria and destroy their membranes in a short time, and showed very low cytotoxicity to NRK-52E cells. Some interesting structure-activity relationships (SARs) were also discussed. These results indicated that these norfloxacin-1,3,4-oxadiazole hybrids could be further developed into new antibacterial agents against MRSA.

Synthesis of pyrimidones and evaluation of their xanthine oxidase inhibitory and antioxidant activities

The increasing prevalence of gout has been accompanied by a growing number of patients intolerant to or with disease refractory to the available urate-lowering therapies. This metabolic disease is a common disease with a higher prevalence in men older than 30 years and in women older than 50 years. These findings highlight the need for emerging treatments to effectively lower urate levels. In this view, we describe the xanthine oxidase (XO) inhibitory activities of the synthesized compounds 5a-j and also their antioxidant activities. Compounds 5c, 5d, 5f, 5h, and 5j exhibited good inhibitory activities against XO. On the other hand, compounds 5g and 5j exhibited moderate antioxidant activity. In order to find new urate-lowering compounds, the xanthine oxidase (XO) inhibitory and antioxidant activities of the newly synthesized pyrimidones 5a-j were evaluated. Compounds 5c, 5d, 5f, 5h, and 5j exhibited good inhibitory activities against XO. In addition, compounds 5g and 5j showed moderate antioxidant activity.

Versatile synthesis of fused tricyclic 1,2,4-triazole derivatives

(Chemical Equation Presented) The synthesis of a small series of fused tricyclic 1,2,4-triazoles is described. The key reaction is an intramolecular two-stage, one-pot reduction/cyclization sequence of a nitropyridine/oxadiazole substrate to give the key tricyclic triazole. Further standard transformations convert this template into a series of final target compounds. Copyright Pfizer Ltd.

SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS

The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytoci antagonists, uses thereof, processes for the preparation thereof and compositions containing sai inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction particularly premature ejaculation (P.E.).

SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS

This invention relates to compounds of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).