Month: October 2022

Kim, Chaewon’s team published research in Archives of Pharmacal Research in 2015 | CAS: 5788-60-3

3-Chloro-6-propoxypyridazine(cas: 5788-60-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Product Details of 5788-60-3

Product Details of 5788-60-3On May 31, 2015, Kim, Chaewon; Lee, Jihee; Park, Myung-Sook published an article in Archives of Pharmacal Research. The article was 《Synthesis of new diorganodiselenides from organic halides: their antiproliferative effects against human breast cancer MCF-7 cells》. The article mentions the following:

A new series of bis(aryl or aralkyl) diselenides was synthesized by selenylation from aryl halide (or aralkyl halide) for development of new anticancer agents. The process involves the reaction of aryl halides (or aralkyl halides) with selenium, hydrazine hydrate under atm. pressure in the presence of sodium hydroxide, to afford diorganodiselenides. These new compounds showed antiproliferative activities against breast cancer (MCF-7) cells in CCK-8 assays, and could be promising candidates for chemotherapy of carcinomas. Among 17 synthesized compounds for inhibiting the growth of these cell lines, 1,2-bis(chloropyridazinyl) diselenide I showed the highest potency. This result suggests the potential anticancer activity of compound I. The experimental process involved the reaction of 3-Chloro-6-propoxypyridazine(cas: 5788-60-3Product Details of 5788-60-3)

3-Chloro-6-propoxypyridazine(cas: 5788-60-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Product Details of 5788-60-3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Siegrist, Romain’s team published research in Journal of Medicinal Chemistry in 2016 | CAS: 1445-56-3

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Computed Properties of C5H2ClN3

Siegrist, Romain; Pozzi, Davide; Jacob, Gael; Torrisi, Caterina; Colas, Kilian; Braibant, Bertrand; Mawet, Jacques; Pfeifer, Thomas; de Kanter, Ruben; Roch, Catherine; Kessler, Melanie; Corminboeuf, Olivier; Bezencon, Olivier published their research in Journal of Medicinal Chemistry on December 8 ,2016. The article was titled 《Structure-Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers》.Computed Properties of C5H2ClN3 The article contains the following contents:

Despite the availability of numerous antiepileptic drugs, 20-30% of epileptic patients are pharmacoresistant with seizures not appropriately controlled. Consequently, new strategies to address this unmet medical need are required. T-type calcium channels play a key role in neuronal excitability and burst firing and selective triple T-type calcium channel blockers could offer a new way to treat various CNS disorders, in particular epilepsy. Herein the authors describe the identification of new 1,4-benzodiazepines as brain penetrant and selective triple T-type calcium channel blockers. From racemic hit 4 ((±)-N,1-dibenzyl-3,5-cis-dimethyl-1,2,3,5-tetrahydro-4H-benzo[e][1,4]diazepine-4-carboxamide), optimization work led to the preparation of pyridodiazepine 31c with improved physicochem. properties, solubility and metabolic stability. The racemic mixture was separated by chiral preparative HPLC and the resulting lead compound (3R,5S)-31c ((3R,5S)-N,1-dibenzyld-3,5-dimethyl-1,2,3,5-tetrahydro-4,5-pyrido[3,4-e][1,4]diazepine-4-carboxamide) showed promising efficacy in the WAG/Rij-rat model of generalized non-convulsive absence-like epilepsy. In the experiment, the researchers used many compounds, for example, 3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3Computed Properties of C5H2ClN3)

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Computed Properties of C5H2ClN3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Trofymchuk, Serhii’s team published research in Journal of Organic Chemistry in 2020 | CAS: 244268-34-6

5-(Trifluoromethyl)pyridazin-3(2H)-one(cas: 244268-34-6) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Reference of 5-(Trifluoromethyl)pyridazin-3(2H)-one

Reference of 5-(Trifluoromethyl)pyridazin-3(2H)-oneOn March 6, 2020, Trofymchuk, Serhii; Bugera, Maksym Ya.; Klipkov, Anton A.; Razhyk, Bohdan; Semenov, Sergey; Tarasenko, Karen; Starova, Viktoriia S.; Zaporozhets, Olga A.; Tananaiko, Oksana Yu.; Alekseenko, Anatoliy N.; Pustovit, Yurii; Kiriakov, Oleksandr; Gerus, Igor I.; Tolmachev, Andrei A.; Mykhailiuk, Pavel K. published an article in Journal of Organic Chemistry. The article was 《Deoxofluorination of (Hetero)aromatic Acids》. The article mentions the following:

Diverse trifluoromethyl-substituted compounds were synthesized by deoxofluorination of cinnamic and (hetero)aromatic carboxylic acids with sulfur tetrafluoride. The obtained products were used as starting materials in the preparation of novel fluorinated amino acids, anilines, and aliphatic amines – valuable building blocks for medicinal chem. and agrochem. Of note, sulfur tetrafluoride (SF4) and hydrogen fluoride (HF) are toxic, therefore, safety and addnl. tech. training must be taken before working with them. The experimental part of the paper was very detailed, including the reaction process of 5-(Trifluoromethyl)pyridazin-3(2H)-one(cas: 244268-34-6Reference of 5-(Trifluoromethyl)pyridazin-3(2H)-one)

5-(Trifluoromethyl)pyridazin-3(2H)-one(cas: 244268-34-6) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Reference of 5-(Trifluoromethyl)pyridazin-3(2H)-one

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Haider, Norbert’s team published research in Journal of Heterocyclic Chemistry in 1988 | CAS: 1445-56-3

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Product Details of 1445-56-3

Haider, Norbert; Heinisch, Gottfried; Lassnigg, Doris published their research in Journal of Heterocyclic Chemistry on February 29 ,1988. The article was titled 《Pyridazines. XXXV. Preparation of some novel pyrimido[4,5-c]pyridazine derivatives from 3-(alkylamino)- and 3-(arylamino)-4-pyridazinecarboxamides》.Product Details of 1445-56-3 The article contains the following contents:

Pyrimido[4,5-c]pyridazinediones I (R = Ph, PhCH2; R1R2 = O), pyrimido[4,5-c]pyridazinones II (R = Ph, PhCH2; R3 = H, Me, Et), and dihydropyrimido[4,5-c]pyridazinones I (R = Ph, PhCH2, Me2CH; R1 = H, R2 = Ph, 3-pyridyl) were prepared from 3-chloro-4-pyridazinecarbonitrile III (R4 = Cl) via amino carbonitriles III (R4 = NHR) and amino carboxamides. In addition, III (R4 = NH2) was prepared from III (R4 = Cl), via the tetrazolo[1,5-b]pyridazine IV as the key intermediate.3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3Product Details of 1445-56-3) was used in this study.

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Product Details of 1445-56-3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Yanai, Mitsuji’s team published research in Journal of Heterocyclic Chemistry in 1970 | CAS: 27427-66-3

3,6-Dichloropyridazine-4-carboxamide(cas: 27427-66-3) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Formula: C5H3Cl2N3O

In 1970,Journal of Heterocyclic Chemistry included an article by Yanai, Mitsuji; Kuraishi, Tsukasa; Kinoshita, Toshio; Nishimura, Masakuni. Formula: C5H3Cl2N3O. The article was titled 《Recyclization of 3-amino-6-chloroimidazo[4,5-c]pyridazine》. The information in the text is summarized as follows:

3-Benzylideneamino-6-chloroimidazo[4,5-c]pyridazine refluxed with HCl or AcOH gave 5-chloro-8-amino-s-triazolo-[4,5-b]pyridazine and 3-benzylid enehydrazino-4-amino-6-chloropyridazine.3,6-Dichloropyridazine-4-carboxamide(cas: 27427-66-3Formula: C5H3Cl2N3O) was used in this study.

3,6-Dichloropyridazine-4-carboxamide(cas: 27427-66-3) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Formula: C5H3Cl2N3O

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Yanai, Mitsuji’s team published research in Chemical & Pharmaceutical Bulletin in 1977 | CAS: 1445-56-3

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Category: pyridazine

In 1977,Chemical & Pharmaceutical Bulletin included an article by Yanai, Mitsuji; Takeda, Shigeko; Mitsuoka, Tamao. Category: pyridazine. The article was titled 《Studies on heterocyclic compounds. XX. The reaction of 4-cyano-3,6-dichloropyridazine with amines》. The information in the text is summarized as follows:

4-Cyano-3,6-dichloropyridazine (I) was treated with primary amines in MeOH under mild conditions (stirring at 0-5°) to give the corresponding 5-amino derivatives II (R = NHCH2CH2OH, NH2, PhCH2NH, NHMe, etc.) resulting from nuclear amination. When I was treated with secondary amines, the corresponding 3- or 6-amino derivatives were obtained.3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3Category: pyridazine) was used in this study.

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Category: pyridazine

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Fulep, Gunther’s team published research in Molecules [Electronic Publication] in 1998 | CAS: 1445-56-3

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Synthetic Route of C5H2ClN3

In 1998,Molecules [Electronic Publication] included an article by Fulep, Gunther; Haider, Norbert. Synthetic Route of C5H2ClN3. The article was titled 《Synthesis and intramolecular [4+2] cycloaddition reactions of 4-pyridazinecarbonitriles with alkyne side chains》. The information in the text is summarized as follows:

Title compounds I (X = O, R = H, Me; X = NH, R = H) were prepared I underwent thermally induced intramol. Diels-Alder reactions with inverse electron demand, affording fused benzonitriles (II). Incorporation of a 1,2-phenylene unit into the side chain, as in III (X = O, NAc), resulted in a more favorable conformation of the dienophilic substructure and thus in a pronounced acceleration of the [4+2] cycloaddition reaction. In the experiment, the researchers used 3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3Synthetic Route of C5H2ClN3)

3-Chloropyridazine-4-carbonitrile(cas: 1445-56-3) belongs to pyridazine derivatives.The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazines are also important because of their utility in synthetic organic chemistry and in physical organic chemistry.There are reports available for the synthesis of pyridazine and their derivatives by using 2-oxoaldehyes.Synthetic Route of C5H2ClN3

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Yu, Jianjun’s team published research in European Journal of Medicinal Chemistry in 2019-01-01 | 20744-39-2

European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Related Products of 20744-39-2.

Yu, Jianjun; Xu, Lei; Hong, Duidui; Zhang, Xiaotuan; Liu, Jieyu; Li, Daqiang; Li, Jia; Zhou, Yubo; Liu, Tao published the artcile< Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors>, Related Products of 20744-39-2, the main research area is phenol ether preparation proteasome inhibitor antitumor SAR mol docking; Non-covalent; Non-peptide; Phenol ether; Proteasome inhibitor; Solid cancers.

A series of novel phenol ether derivatives I (n = 1, 2; R1 = Me, methoxy, n-Pr, etc.; R2 = 4-FC6H4, 2-naphthyl, 3-pyridinyl, etc.) were designed, synthesized, and evaluated as non-covalent proteasome inhibitors. Most compounds exhibited moderate to excellent proteasome inhibitory activity. In particular, compound I (n = 1; R1 = n-Bu; R2 = pyridazine-4-yl) proved to be the most potent compound (chymotrypsin-like: IC50 = 49 nM), exhibiting a 2-fold higher potency compared to the reported PI-1840. Besides, compound I (n = 1; R1 = n-Bu; R2 = pyridazine-4-yl) exhibited excellent metabolic stability and selective anti-proliferative activity against solid cancer cell lines including HepG2 and HGC27, providing incentive for the further development as a potential anticancer agent against solid cancers.

European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Related Products of 20744-39-2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Abdelaziz, Ahmed M’s team published research in Bioorganic & Medicinal Chemistry Letters in 2019-09-15 | 20744-39-2

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Electric Literature of 20744-39-2.

Abdelaziz, Ahmed M.; Basnet, Sunita K. C.; Islam, Saiful; Li, Manjun; Tadesse, Solomon; Albrecht, Hugo; Gerber, Cobus; Yu, Mingfeng; Wang, Shudong published the artcile< Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors>, Electric Literature of 20744-39-2, the main research area is spiro cyclohexane imidazopyridine dione preparation chemoselective antitumor Mnk inhibitor; Anti-cancer; Inhibitor; Mnk; eFT508; eIF4E.

A series of 2’H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione derivatives I (R = pyridin-4-yl, pyrimidin-4-yl, oxazol-2-yl, etc.) is presented as Mnk inhibitors. Some of them showed sub-micromolar to low nanomolar inhibitory activities against Mnk1/2 with a high level of selectivity for both kinases over CDKs. Biochem. assays revealed that compounds I (R = pyridin-4-yl, pyrimidin-4-yl) are non-ATP-competitive inhibitors of Mnks. Lead compound I (R = pyrimidin-4-yl) demonstrated a high selectivity for Mnk1/2 over a selection of 51 kinases, and displayed anti-proliferative activities against a panel of cancer cell lines. However, this compound in combination with our inhouse CDK4/6 inhibitor 83 did not show a synergistic effect in A2780 ovarian cancer cells, suggesting that caution be exercised in the selection of an agent to be combined with an Mnk inhibitor.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Electric Literature of 20744-39-2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

 

Venkatesan, Aranapakam M’s team published research in Journal of Medicinal Chemistry in 2010-03-25 | 20744-39-2

Journal of Medicinal Chemistry published new progress about Antitumor agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Synthetic Route of 20744-39-2.

Venkatesan, Aranapakam M.; Dehnhardt, Christoph M.; Delos Santos, Efren; Chen, Zecheng; Dos Santos, Osvaldo; Ayral-Kaloustian, Semiramis; Khafizova, Gulnaz; Brooijmans, Natasja; Mallon, Robert; Hollander, Irwin; Feldberg, Larry; Lucas, Judy; Yu, Ker; Gibbons, James; Abraham, Robert T.; Chaudhary, Inder; Mansour, Tarek S. published the artcile< Bis(morpholino-1,3,5-triazine) Derivatives: Potent Adenosine 5'-Triphosphate Competitive Phosphatidylinositol-3-kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of Compound 26 (PKI-587), a Highly Efficacious Dual Inhibitor>, Synthetic Route of 20744-39-2, the main research area is PI3K mTOR inhibitor dimorpholinotriazine preparation; triazine dimorpholino preparation PI3K mTOR inhibitor.

The PI3K/Akt signaling pathway is a key pathway in cell proliferation, growth, survival, protein synthesis, and glucose metabolism It has been recognized recently that inhibiting this pathway might provide a viable therapy for cancer. A series of bis(morpholino-1,3,5-triazine) derivatives were prepared and optimized to provide the highly efficacious PI3K/mTOR inhibitor 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea (PKI-587). This compound has shown excellent activity in vitro and in vivo, with antitumor efficacy in both s.c. and orthotopic xenograft tumor models when administered i.v. The structure-activity relationships and the in vitro and in vivo activity of analogs in this series are described.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Synthetic Route of 20744-39-2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem