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novel tricyclic system

An efficient two-steps strategy for the regioselective synthesis of the benzo[f]pyrimido[4,5-b][1,5]oxazocine as a novel tricyclic system has been developed via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 2-aminobenzylalcohol in room temperature and short reaction times under mild conditions, followed amination with some secondary amines.

Fast and efficient regioselective synthesis of a novel eight membered ring system, 5H-benzo[f]pyrimido[4,5-b][1,5]oxazocine

novel tricyclic system

ABSTRACT Several derivatives of the novel tricyclic system ‘dipyrimido[2,1-b:4′,5′-d][1,3]thiazine’ were synthesized via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile in short reaction times under mild conditions.

Regioselective synthesis of new 5H,10H-dipyrimido[2,1-b:4′,5′-d][1,3]thiazine: a combined experimental and computational study

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novel tricyclic derivative

All the novel tricyclic derivatives were evaluated for inhibitory activity against herpes simplex virus 1 and 2 (HSV-1, HSV-2) and thymidine kinase deficient (ACV resistant) HSV-1.

Synthesis and anti-HSV activity of tricyclic penciclovir and hydroxybutylguanine derivatives

novel tricyclic derivative

Antithrombotic activity of a novel tricyclic derivative of diazepino[1,2-α]benzimidazole (DAB-15) was examined on the model of arterial thrombosis developed in rats without concomitant pathology and in rats with experimental myocardial infarction.

Antithrombotic Activity of a Novel Diazepino[1,2-α] Benzimidazole Derivative on Arterial Thrombosis Model in Rats without Concomitant Pathology and in Rats with Experimental Myocardial Infarction

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10.1021/acs.orglett.1c01167

The protocol proceeds under operationally simple conditions and provides novel tricyclic and tetracyclic scaffolds such as 3,4-dihydroindolo[1,2-c]quinazoline-1,6(2H,5H)-dione and 1H-[1,3]oxazino[3,4-a]indol-1-one derivatives with a broad range of functional group tolerance and moderate to excellent yields.

Rh(III)-Catalyzed Chemodivergent Annulations between Indoles and Iodonium Carbenes: A Rapid Access to Tricyclic and Tetracyclic N-Heterocylces.

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10.2298/jsc210416068k

The synthetic route toward novel tricyclic, nitrogen-containing system is disclosed.

Synthetic route towards 1,2,3,4-tetrahydroquinoxaline/piperidine combined tricyclic ring system

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10.1021/acs.joc.1c01315

A new domino mode of assembly was discovered from the one-pot three-component reactions of pyrrole derivatives, active methylene compounds (malononitrile, methyl cyanoacetate, or ethyl cyanoacetate), and sodium cyanide in the presence of piperidinium acetate in EtOH at room temperature, leading to a novel tricyclic skeleton in excellent yield under mild and eco-friendly conditions.

Diastereoselective Synthesis of Densely Functionalized 3a,8a-Dihydro-8H-furo[3,2-a]pyrrolizines through One-Pot Three-Component Assembly.

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10.1016/j.ejmech.2021.113750

To develop a selective TRPM2 inhibitor, three-dimensional similarity-based screening strategy was employed using the energy-minimized conformation of non-selective TRPM2 inhibitor 2-APB as the query structure, which resulted in the discovery of a novel tricyclic TRPM2 inhibitor Z-4 with benzo[d]imidazo[1,2-a]imidazole skeleton.

Design, synthesis and biological activities of benzo[d]imidazo[1,2-a]imidazole derivatives as TRPM2-specfic inhibitors.

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10.1007/s00706-021-02758-y

An efficient two-steps strategy for the regioselective synthesis of the benzo[f]pyrimido[4,5-b][1,5]oxazocine as a novel tricyclic system has been developed via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 2-aminobenzylalcohol in room temperature and short reaction times under mild conditions, followed amination with some secondary amines.

Fast and efficient regioselective synthesis of a novel eight membered ring system, 5H-benzo[f]pyrimido[4,5-b][1,5]oxazocine

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10.1155/2021/5597003

Purpose To evaluate efficacy and safety of novel tricyclic corneal stroma injection (TCSI) voriconazole for the treatment of fungal keratitis.

Efficacy of Voriconazole Corneal Intrastromal Injection for the Treatment of Fungal Keratitis

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10.1080/17415993.2019.1576685

ABSTRACT Several derivatives of the novel tricyclic system ‘dipyrimido[2,1-b:4′,5′-d][1,3]thiazine’ were synthesized via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile in short reaction times under mild conditions.

Regioselective synthesis of new 5H,10H-dipyrimido[2,1-b:4′,5′-d][1,3]thiazine: a combined experimental and computational study

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10.1038/s41589-019-0365-8

Here we show that WEHI-9625, a novel tricyclic sulfone small molecule, binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK.

A small molecule interacts with VDAC2 to block mouse BAK-driven apoptosis

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10.1002/anie.201903488

Cyclobutene alcohols undergo Prins cyclisations to generate single diastereomers of novel tricyclic heterocycles with five contiguous stereocentres.

Sequential Photochemical and Prins Reactions for the Diastereoselective Synthesis of Tricyclic Scaffolds.

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10.1016/j.carres.2019.04.002

A series of novel tricyclic quinazolinone-iminosugars 1 (a-c) were synthesized from the benzyl protected sugars through three steps.

Synthesis of tricyclic quinazolinone-iminosugars as potential glycosidase inhibitors via a Mitsunobu reaction.

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10.1016/j.bmc.2019.02.005

All the novel tricyclic derivatives were evaluated for inhibitory activity against herpes simplex virus 1 and 2 (HSV-1, HSV-2) and thymidine kinase deficient (ACV resistant) HSV-1.

Synthesis and anti-HSV activity of tricyclic penciclovir and hydroxybutylguanine derivatives

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10.3987/com-19-14093

– The synthesis of novel tricyclic fused furo[2,3-b]pyridine derivatives is described.

A Convenient Approach to the Synthesis of Novel Tricyclic Fused Furo[2,3-b]pyridine Derivatives

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10.1007/s10517-019-04432-0

Antithrombotic activity of a novel tricyclic derivative of diazepino[1,2-α]benzimidazole (DAB-15) was examined on the model of arterial thrombosis developed in rats without concomitant pathology and in rats with experimental myocardial infarction.

Antithrombotic Activity of a Novel Diazepino[1,2-α] Benzimidazole Derivative on Arterial Thrombosis Model in Rats without Concomitant Pathology and in Rats with Experimental Myocardial Infarction

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10.1021/ACS.ORGANOMET.9B00356

Interestingly, the latter was seen to undergo facile reductive elimination, affording a novel tricyclic monodentate NHC ligand.

Accessing Chelating Extended Linker Bis(NHC) Palladium(II) Complexes: Sterically Triggered Divergent Reaction Pathways

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10.1016/j.bmcl.2019.06.032

Medicinal chemistry design efforts yielded two novel tricyclic cores that enhanced M4 PAM potency, regained CNS penetration, displayed favorable DMPK properties and afforded robust in vivo efficacy in reversing amphetamine-induced hyperlocomotion in rats.

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.

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10.1080/09205071.2019.1605940

A novel tricyclic nested electromagnetic bandgap (TN-EBG) structure has been proposed to restrain the simultaneous switching noise (SSN) in high-speed digital systems.

Tricyclic nested electromagnetic bandgap structure characterized with broad stopband bandwidth and deep noise suppression

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10.1021/acschemneuro.8b00311

This Letter describes the chemical optimization of a new series of muscarinic acetylcholine receptor subtype 1 (M1) positive allosteric modulators (PAMs) based on novel tricyclic triazolo- and imidazopyridine lactam cores, devoid of M1 agonism, e.

Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators.

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10.1016/J.OPTMAT.2019.05.006

A novel tricyclic heterocyclic compound, 5,5’-(furan-2,5-diyl)bis (1,3,4- thiadiazol-2-amine) (3), was easily synthesized, which has an excellent fluorescence performance and could be a chemical sensor of Pd2+ at a very broad pH range.

A novel tricyclic heterocyclic fluorescent probe for Pd2+ in aqueous solution: Synthesis, properties and theoretical calculations

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10.3390/molecules24050921

A series of novel tricyclic matrinic derivatives with 11-adamantyl substitution were designed, synthesized, and evaluated for their activities against Influenza A H3N2 virus, based on the privileged structure strategy.

Evolution and Biological Evaluation of Matrinic Derivatives with Amantadine Fragments As New Anti-Influenza Virus Agents

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10.1007/s00259-019-4268-4

F-GE180 is a novel tricyclic indole compound that binds to TSPO with high affinity [3], and has been used with satisfactory results in a variety of preclinical models [4–6].

The validity of 18F-GE180 as a TSPO imaging agent

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10.1002/cbdv.201900012

Upon the prenylation, side reactions were observed, resulting in the formation of nucleolipids with a novel tricyclic nucleobase (→4a, 4b).

Nucleolipids of the Nucleoside Antibiotics Formycins A and B: Synthesis and Biomedical Characterization Particularly Using Glioblastoma Cells

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Novel Tricyclic - The protocol proceeds under operationally simple conditions and provides novel tricyclic and tetracyclic scaffolds such as 3,4-dihydroindolo[1,2-c]quinazoline-1,6(2H,5H)-dione and 1H-[1,3]oxazino[3,4-a]indol-1-one derivatives with a broad range of functional group tolerance and moderate to excellent yields. [1] The synthetic route toward novel tricyclic, nitrogen-containing system is disclosed. [2] A new domino mode of assembly was discovered from the one-pot three-component reactions of pyrrole derivatives, active methylene compounds (malononitrile, methyl cyanoacetate, or ethyl cyanoacetate), and sodium cyanide in the presence of piperidinium acetate in EtOH at room temperature, leading to a novel tricyclic skeleton in excellent yield under mild and eco-friendly conditions. [3] To develop a selective TRPM2 inhibitor, three-dimensional similarity-based screening strategy was employed using the energy-minimized conformation of non-selective TRPM2 inhibitor 2-APB as the query structure, which resulted in the discovery of a novel tricyclic TRPM2 inhibitor Z-4 with benzo[d]imidazo[1,2-a]imidazole skeleton. [4] An efficient two-steps strategy for the regioselective synthesis of the benzo[f]pyrimido[4,5-b][1,5]oxazocine as a novel tricyclic system has been developed via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 2-aminobenzylalcohol in room temperature and short reaction times under mild conditions, followed amination with some secondary amines. [5] Purpose To evaluate efficacy and safety of novel tricyclic corneal stroma injection (TCSI) voriconazole for the treatment of fungal keratitis. [6] ABSTRACT Several derivatives of the novel tricyclic system ‘dipyrimido[2,1-b:4′,5′-d][1,3]thiazine’ were synthesized via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile in short reaction times under mild conditions. [7] Here we show that WEHI-9625, a novel tricyclic sulfone small molecule, binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. [8] Cyclobutene alcohols undergo Prins cyclisations to generate single diastereomers of novel tricyclic heterocycles with five contiguous stereocentres. [9] A series of novel tricyclic quinazolinone-iminosugars 1 (a-c) were synthesized from the benzyl protected sugars through three steps. [10] All the novel tricyclic derivatives were evaluated for inhibitory activity against herpes simplex virus 1 and 2 (HSV-1, HSV-2) and thymidine kinase deficient (ACV resistant) HSV-1. [11] – The synthesis of novel tricyclic fused furo[2,3-b]pyridine derivatives is described. [12] Antithrombotic activity of a novel tricyclic derivative of diazepino[1,2-α]benzimidazole (DAB-15) was examined on the model of arterial thrombosis developed in rats without concomitant pathology and in rats with experimental myocardial infarction. [13] Interestingly, the latter was seen to undergo facile reductive elimination, affording a novel tricyclic monodentate NHC ligand. [14] Medicinal chemistry design efforts yielded two novel tricyclic cores that enhanced M4 PAM potency, regained CNS penetration, displayed favorable DMPK properties and afforded robust in vivo efficacy in reversing amphetamine-induced hyperlocomotion in rats. [15] A novel tricyclic nested electromagnetic bandgap (TN-EBG) structure has been proposed to restrain the simultaneous switching noise (SSN) in high-speed digital systems. [16] This Letter describes the chemical optimization of a new series of muscarinic acetylcholine receptor subtype 1 (M1) positive allosteric modulators (PAMs) based on novel tricyclic triazolo- and imidazopyridine lactam cores, devoid of M1 agonism, e. [17] A novel tricyclic heterocyclic compound, 5,5’-(furan-2,5-diyl)bis (1,3,4- thiadiazol-2-amine) (3), was easily synthesized, which has an excellent fluorescence performance and could be a chemical sensor of Pd2+ at a very broad pH range. [18] A series of novel tricyclic matrinic derivatives with 11-adamantyl substitution were designed, synthesized, and evaluated for their activities against Influenza A H3N2 virus, based on the privileged structure strategy. [19] F-GE180 is a novel tricyclic indole compound that binds to TSPO with high affinity [3], and has been used with satisfactory results in a variety of preclinical models [4–6]. [20] Upon the prenylation, side reactions were observed, resulting in the formation of nucleolipids with a novel tricyclic nucleobase (→4a, 4b). [21]

novel tricyclic system

An efficient two-steps strategy for the regioselective synthesis of the benzo[f]pyrimido[4,5-b][1,5]oxazocine as a novel tricyclic system has been developed via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 2-aminobenzylalcohol in room temperature and short reaction times under mild conditions, followed amination with some secondary amines. [1] ABSTRACT Several derivatives of the novel tricyclic system ‘dipyrimido[2,1-b:4′,5′-d][1,3]thiazine’ were synthesized via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile in short reaction times under mild conditions. [2]

novel tricyclic derivative

All the novel tricyclic derivatives were evaluated for inhibitory activity against herpes simplex virus 1 and 2 (HSV-1, HSV-2) and thymidine kinase deficient (ACV resistant) HSV-1. [1] Antithrombotic activity of a novel tricyclic derivative of diazepino[1,2-α]benzimidazole (DAB-15) was examined on the model of arterial thrombosis developed in rats without concomitant pathology and in rats with experimental myocardial infarction. [2]