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A number of 6-chloro-3-(pyrazol-1?-yl) pyridazines were prepared from 3,6-dichloropyridazine via either reaction with hydrazine followed I by reaction with appropriate reagents to develop the pyrazole or through a nucleophilic reaction with a pyrazole. Some electrophilic reactions gave the corresponding 4?-substituted pyrazolylpyridazines. All the compounds were tested for their in vitro antibacterial as well as their antioxidant properties.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1601 – PubChem

 

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This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had improved selectivity versus the IKr channel; poor selectivity against IKr had been a liability of earlier analogs in this series.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1854 – PubChem

 

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A mild, practical method for direct arylation of unactivated C(sp3)-H bonds with heteroarenes has been achieved via photochemistry. Selectfluor is used as a hydrogen atom transfer reagent under visible light irradiation. A diverse range of chemical feedstocks, such as alkanes, ketones, esters, and ethers, and complex molecules readily undergo intermolecular C(sp3)-C(sp2) bond formation. Moreover, a broad array of heteroarenes, including pharmaceutically useful scaffolds, can be alkylated effectively by the protocol presented here.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1979 – PubChem

 

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Structure-activity relationship (SAR) investigations of a novel class of triazolopyridazinone p38alpha mitogen activated protein kinase (MAPK) inhibitors are disclosed. From these studies, increased in vitro potency was observed for 2,6-disubstituted phenyl moieties and N-ethyl triazolopyridazinone cores due to key contacts with Leu108, Ala157 and Val38. Further investigation led to the identification of three compounds, 3g, 3j and 3m that are highly potent inhibitors of LPS-induced MAPKAP kinase 2 (MK2) phosphorylation in 50% human whole blood (hWB), and possess desirable in vivo pharmacokinetic and kinase selectivity profiles.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1730 – PubChem

 

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A series of novel Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors 8a-f was synthesized; the substances were characterized by the presence of a 2,5-dimethylpyrazin-3-yl moiety at one end and a 3-heptylamino-5- phenylpyridazine system at the other one, linked through linear alkyl spacers of different length. The new derivatives were designed based on the hypothesis that the 3-amino-5-phenylpyridazine moiety could mimic the aryl substituted urea, which was present in a number of ACAT inhibitors previously described. The choice of the 2,5-dimethylpyrazin-3-yl substituent was supported by a preliminary investigation, which indicated that this moiety is the most powerful in conferring ACAT inhibitory properties to the new series. The pharmacological results proved the idea to be sound. Finally, compounds 9a-c, lacking the phenylpyridazine moiety were prepared and tested to further strengthen our hypothesis.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1704 – PubChem

 

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A series of new 3-alkylamino-6-allylthio-pyridazine derivatives was synthesized through allythiolation and amino-de-halogenation and were expected to have anti-proliferative activity. 6-Allylthio-3-chloropyridazine was prepared from the reaction of 3,6-dichloropyridazine with allylmercaptan and sodium hydroxide. The alkylamines such as methylamine and the dialkylamines such as dimethylamine were introduced into the 3- position of the pyridazine ring. These new compounds showed anti-proliferative activities against MCF-7 human breast cancer cells in CCK-8 assays. These compounds are thus promising candidates for chemotherapy of breast cancer. Two compounds, 14 and 15, showed higher potencies for inhibiting growth of breast cancer cells than did 5FU. This suggests the potential anti-proliferative activity of these compounds.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1767 – PubChem

 

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Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1426 – PubChem

 

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We report herein the design and synthesis of a series of novel ciprofloxacin (CPFX) derivatives with remarkable improvement in lipophilicity by introducing a substituted benzyl moiety to the N atom on the C-7 piperazine ring of CPFX. Antimycobacterial and antibacterial activity of the newly synthesized compounds was evaluated. Results reveal that compound 4f has good in vitro activity against all of the tested Gram-positive strains including MRSA and MRSE (MICs: 0.06-32 mug/mL) which is two to eightfold more potent than or comparable to the parent drug CPFX (MICs: 0.25-128 mug/mL), Gram-negative bacteria P. aeruginosa (MICs: 0.5-4 mug/mL) and M. tuberculosis H37Rv ATCC 27294 (MIC: 1 mug/mL).

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1949 – PubChem

 

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The reactions of methylhydrazine and hydrazine hydrate with chlorinated pyridazines and pyridazones were studied.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1606 – PubChem

 

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Nuclear magnetic resonance (NMR) and magnetic resonance imaging (MRI) are two extremely important techniques with applications ranging from molecular structure determination to human imaging. However, in many cases the applicability of NMR and MRI are limited by inherently poor sensitivity and insufficient nuclear spin lifetime. Here we demonstrate a cost-efficient and fast technique that tackles both issues simultaneously. We use the signal amplification by reversible exchange (SABRE) technique to hyperpolarize the target1H nuclei and store this polarization in long-lived singlet (LLS) form after suitable radiofrequency (rf) pulses. Compared to the normal scenario, we achieve three orders of signal enhancement and one order of lifetime extension, leading to1H NMR signal detection 15 minutes after the creation of the detected states. The creation of such hyperpolarized long-lived polarization reflects an important step forward in the pipeline to see such agents used as clinical probes of disease.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1880 – PubChem