Tag: M.W:100-200

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, ACS Medicinal Chemistry Letters called Amide-Amine Replacement in Indole-2-carboxamides Yields Potent Mycobactericidal Agents with Improved Water Solubility, Author is Tan, Yu Jia; Li, Ming; Gunawan, Gregory Adrian; Nyantakyi, Samuel Agyei; Dick, Thomas; Go, Mei-Lin; Lam, Yulin, which mentions a compound: 21778-81-4, SMILESS is O=CC(N1)=CC2=C1C=CC(OC)=C2, Molecular C10H9NO2, Recommanded Product: 21778-81-4.

Indolecarboxamides are potent but poorly soluble mycobactericidal agents. Here, it was found that modifying the incipient scaffold by amide-amine substitution and replacing the indole ring with benzothiophene or benzoselenophene led to striking (10-20-fold) improvements in solubility Potent activity could be achieved without the carboxamide linker but not in the absence of the indole ring. The indolylmethylamine, N-cyclooctyl-6-trifluoromethylindol-2-ylmethylamine (MIC90Mtb 0.13μM, MBC99.9Mtb 0.63μM), exemplifies a promising member that is more soluble and equipotent to its carboxamide equivalent It is also an inhibitor of the mycolate transporter MmpL3, a property shared by the methylamines of benzothiophene and benzoselenophene.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Application In Synthesis of (R)-(-)-3-Fluoropyrrolidine Hydrochloride. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Discovery of novel 4-phenyl-2-(pyrrolidinyl)nicotinamide derivatives as potent Nav1.1 activators. Author is Miyazaki, Tohru; Kawasaki, Masanori; Suzuki, Atsushi; Ito, Yuki; Imanishi, Akio; Maru, Takamitsu; Kawamoto, Tomohiro; Koike, Tatsuki.

The voltage-gated sodium channel, Nav1.1, is predominantly expressed in parvalbumin-pos. fast spiking interneurons and has been genetically linked to Dravet syndrome. Starting from a high throughput screening hit isoxazole derivative 5, modifications of 5 via combinations of IonWorks and Q-patch assays successfully identified the nicotinamide derivative 4. Its increasing decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6 and acceptable brain exposure in mice was observed Compound 4 is a promising Nav1.1 activator that can be used to analyze pathophysiol. functions of the Nav1.1 channel towards treating various central nervous system diseases.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 21778-81-4, is researched, SMILESS is O=CC(N1)=CC2=C1C=CC(OC)=C2, Molecular C10H9NO2Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called 2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists, Author is Spadoni, Gilberto; Balsamini, Cesarino; Bedini, Annalida; Diamantini, Giuseppe; Di Giacomo, Barbara; Tontini, Andrea; Tarzia, Giorgio; Mor, Marco; Plazzi, Pier Vincenzo; Rivara, Silvia; Nonno, Romolo; Pannacci, Marilou; Lucini, Valeria; Fraschini, Franco; Stankov, Bojidar Michaylov, the main research direction is melatonin receptor antagonist agonist.Electric Literature of C10H9NO2.

The synthesis of several novel indole melatonin analogs substituted at the 2-position with acylaminomethyl, acylaminoethyl, or acylaminopropyl side chains is reported. Using a novel in vitro functional assay (specific binding of [35S]GTPγS), the authors showed that several of these compounds exhibited partial agonist, antagonist, and inverse agonist activity. Binding and functional assays were performed on cloned human MT1 receptor. Structure-activity relation considerations indicate that N-[1-aryl-2-(4-methoxy-1H-indol-2-yl)(C1-C2)alkyl]alkanamides represent a lead structure for this type of ligands.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Kuwano, Satoru; Suzuki, Takumi; Yamanaka, Masahiro; Tsutsumi, Ryosuke; Arai, Takayoshi researched the compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ).Application of 21778-81-4.They published the article 《Catalysis based on C-I···π halogen bonds: electrophilic activation of 2-alkenylindoles by cationic halogen-bond donors for [4+2] cycloadditions》 about this compound( cas:21778-81-4 ) in Angewandte Chemie, International Edition. Keywords: alkenylindole iodoimidazolium triflate catalyst diastereoselective cycloaddition; indolyl tetrahydrocarbazole preparation; cycloaddition; density-functional calculations; halogen bonding; heterocycles; noncovalent bonds. We’ll tell you more about this compound (cas:21778-81-4).

Homo- and cross-[4+2] cycloadditions of 2-alkenylindoles catalyzed by cationic halogen-bond donors were developed. Under mild reaction conditions, 3-indolyl-substituted tetrahydrocarbazole derivatives were obtained in good to excellent yields. Exptl. and quantum calculation studies revealed that the electrophilic activation of 2-alkenylindoles was achieved by C-I···π halogen bonds.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Highly fluorescent 1,2-dihydropyrimido[1,6-α]indoles: an efficient metal-free synthesis and photophysical study, the main research direction is dihydropyrimidoindole preparation; indole carboxaldehyde ethyl arylideneglycinate aldol Mannich reaction.Computed Properties of C10H9NO2.

A metal-free route to highly fluorescent 1,2-dihydropyrimido[1,6-α]indole derivatives I (R = H, OCH3, CH3, Br; Ar = C6H5, naphth-1-yl, furan-2-yl, etc.) has been developed via base catalyzed aldol followed by the Mannich reaction of indole-2-carboxaldehydes II with Et N-arylideneglycinates ArHC=NCH2COOEt at room temperature This transformation consists of the sequential formation of two new bonds to afford highly functionalized pyrimidoindole derivatives under mild reaction conditions.. Photophys. properties of the products have also been reported.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ) is researched.Computed Properties of C10H9NO2.Lena, Gersande; Trapani, Joseph A.; Sutton, Vivien R.; Ciccone, Annette; Browne, Kylie A.; Smyth, Mark J.; Denny, William A.; Spicer, Julie A. published the article 《Dihydrofuro[3,4-c]pyridinones as Inhibitors of the Cytolytic Effects of the Pore-Forming Glycoprotein Perforin》 about this compound( cas:21778-81-4 ) in Journal of Medicinal Chemistry. Keywords: furopyridinone dihydro arylmethylidene preparation inhibitor cytolytic effect glycoprotein perforin; pyrrolopyridinone arylmethylidene heteroarylmethylidene preparation inhibitor cytolytic effect glycoprotein perforin. Let’s learn more about this compound (cas:21778-81-4).

Dihydrofuro[3,4-c]pyridinones are the first class of small mols. reported to inhibit the cytolytic effects of the lymphocyte toxin perforin. A lead structure was identified from a high throughput screen, and a series of analogs I (X = O, S; Y = O, NH; R = Ph, 4-FC6H4, 2-furyl, 5-methyl-2-thienyl, 3-thienyl, 2-benzofuryl, 3-benzothienyl, 3-indolyl, etc.) were designed and prepared to explore structure-activity relationships around the core bicyclic ring and pendant aryl(heteroaryl) ring. This resulted in the identification of a submicromolar inhibitor of the perforin-induced lysis of Jurkat T-lymphoma cells.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 39977-42-9, is researched, SMILESS is O=C(OC)C1=NC=C(CO)C=C1, Molecular C8H9NO3Journal, Tetrahedron Letters called Simultaneous dehalogenation and hydrogenation reduction of halogen-heteroaromatic aldehydes, Author is Chen, Xi-Bo; Hu, Qiu-Peng; Yuan, Qian-Jia; Ding, Wei; Ren, Jiangmeng; Zeng, Bu-Bing, the main research direction is halogenated heteroaromatic aldehyde dehalogenation hydrogenation; heteroaralkyl alc preparation.Quality Control of Methyl 5-(hydroxymethyl)picolinate.

Treatment of halo-heteroaromatic aldehydes with a catalytic amount of PdCl2 under atm. pressure of H2 in base medium (NaOAc) leads to the corresponding dehalogenated primary alcs. The reaction system was especially effective for heteroaromatic compounds bearing aldehyde groups and halides (Br or Cl).

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Synthesis of indole-2-carbaldehydes, 2-(2-aminoethyl) – and 2-(2-aminopropyl)indoles, the main research direction is indolecarboxaldehydes aminoalkyl; aminoalkyl indolecarboxaldehydes.Synthetic Route of C10H9NO2.

Et indole-2-carboxylate derivatives (e.g. I) were reduced by LiAlH4 to indole-2-methanol derivatives (e.g. II). These were oxidized by MnO2 to indole-2-carboxaldehyde derivatives (e.g. III), which were also prepared from the indole-2-carboxylates by the McFadyen-Stevens reaction. The aldehydes reacted with MeNO2 and EtNO2, and the condensation products (e.g. IV and V) were reduced by LiAlH4 to 2-(2-aminoethyl)indoles (e.g. VI) and 2-(2-aminopropyl)indoles (e.g. VII), resp.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Spadoni, Gilberto; Balsamini, Cesarino; Bedini, Annalida; Diamantini, Giuseppe; Di Giacomo, Barbara; Tontini, Andrea; Tarzia, Giorgio; Mor, Marco; Plazzi, Pier Vincenzo; Rivara, Silvia; Nonno, Romolo; Pannacci, Marilou; Lucini, Valeria; Fraschini, Franco; Stankov, Bojidar Michaylov researched the compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ).Application of 21778-81-4.They published the article 《2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists》 about this compound( cas:21778-81-4 ) in Journal of Medicinal Chemistry. Keywords: melatonin receptor antagonist agonist. We’ll tell you more about this compound (cas:21778-81-4).

The synthesis of several novel indole melatonin analogs substituted at the 2-position with acylaminomethyl, acylaminoethyl, or acylaminopropyl side chains is reported. Using a novel in vitro functional assay (specific binding of [35S]GTPγS), the authors showed that several of these compounds exhibited partial agonist, antagonist, and inverse agonist activity. Binding and functional assays were performed on cloned human MT1 receptor. Structure-activity relation considerations indicate that N-[1-aryl-2-(4-methoxy-1H-indol-2-yl)(C1-C2)alkyl]alkanamides represent a lead structure for this type of ligands.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Application of 21778-81-4. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about N-heterocyclic carbene catalyzed domino reactions of formylcyclopropane 1,1-diesters: construction of a 6-5-5 tricyclic pyrrolo[1,2-a]indole. Author is Li, Linxia; Du, Ding; Ren, Jun; Wang, Zhongwen.

Catalyzed by N-heterocyclic carbenes (NHCs), a domino ring-opening/redox amidation/Knoevenagel condensation of readily available formylcyclopropane 1,1-diesters with 1H-indole-2-carbaldehydes is reported. This methodol. provides a new and direct method for the construction of a 6-5-5 tricyclic pyrrolo[1,2-a]indole skeleton I (R1 = H, 5-Me, 5-MeO, 5-Et, 5-iPr, 5-Cl, R2 = CO2Et, R3 = Et, R4 = H; R1 = R4 = H, R2 = CO2Me, R3 = Me; R1 = R4 = H,R2 = CO2iPr, R3 = Et; R1 = H, R2 = CO2Et, R3 = Et, R4 = Me; R1 = H, 5-Me, 5-Cl, R2 = H, R3 = Et, R4 = H).

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem