Tag: 200.2795

Zhang, Jiantao et al. published their research in Scientific Reports in 2018 | CAS: 17403-09-7

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Product Details of 17403-09-7

Exploring Ugi-Azide Four-Component Reaction Products for Broad-Spectrum Influenza Antivirals with a High Genetic Barrier to Drug Resistance was written by Zhang, Jiantao;Hu, Yanmei;Foley, Christopher;Wang, Yuanxiang;Musharrafieh, Rami;Xu, Shuting;Zhang, Yongtao;Ma, Chunlong;Hulme, Christopher;Wang, Jun. And the article was included in Scientific Reports in 2018.Product Details of 17403-09-7 This article mentions the following:

Influenza viruses are respiratory pathogens that are responsible for seasonal influenza and sporadic influenza pandemic. The therapeutic efficacy of current influenza vaccines and small mol. antiviral drugs is limited due to the emergence of multidrug-resistant influenza viruses. In response to the urgent need for the next generation of influenza antivirals, we utilized a fast-track drug discovery platform by exploring multi-component reaction products for antiviral drug candidates. Specifically, mol. docking was applied to screen a small mol. library derived from the Ugi-azide four-component reaction methodol. for inhibitors that target the influenza polymerase PAC-PB1N interactions. One hit compound 5 was confirmed to inhibit PAC-PB1N interactions in an ELISA assay and had potent antiviral activity in an antiviral plaque assay. Subsequent structure-activity relationship studies led to the discovery of compound 12a, which had broad-spectrum antiviral activity and a higher in vitro genetic barrier to drug resistance than oseltamivir. Overall, the discovery of compound 12a as a broad-spectrum influenza antiviral with a high in vitro genetic barrier to drug resistance is significant, as it offers a second line of defense to combat the next influenza epidemics and pandemics if vaccines and oseltamivir fail to confine the disease outbreak. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Product Details of 17403-09-7).

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Product Details of 17403-09-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Herold, Franciszek et al. published their research in European Journal of Medicinal Chemistry in 2010 | CAS: 17403-09-7

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole

Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity. part 3 was written by Herold, Franciszek;Chodkowski, Andrzej;Izbicki, Lukasz;Turlo, Jadwiga;Dawidowski, Maciej;Kleps, Jerzy;Nowak, Gabriel;Stachowicz, Katarzyna;Dybala, Malgorzata;Siwek, Agata;Mazurek, Aleksander P.;Mazurek, Andrzej;Plucinski, Franciszek. And the article was included in European Journal of Medicinal Chemistry in 2010.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole This article mentions the following:

A number of 4-aryl-5,6,7,8-tetrahydropyrido[1,2-c]pyrimidines with 3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole or 2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole residues were synthesized for further investigation of SAR in a group of pyrido[1,2-c]pyrimidine derivatives with dual 5-HT1A/SERT activity. Synthesized compounds were found to be potent ligands for both 5-HT1A and SERT with Ki ranging from 28.3 to 642 nM and 42.4 nM to 1.8 渭M, resp. Moreover some compounds were found to be selective agonists, while compound I as an antagonist of 5-HT1A presynaptic receptors in the inducible hypothermia test in mice. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole).

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Santos, Sofia A. et al. published their research in European Journal of Medicinal Chemistry in 2015 | CAS: 17403-09-7

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 17403-09-7

Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype was written by Santos, Sofia A.;Lukens, Amanda K.;Coelho, Lis;Nogueira, Fatima;Wirth, Dyann F.;Mazitschek, Ralph;Moreira, Rui;Paulo, Alexandra. And the article was included in European Journal of Medicinal Chemistry in 2015.Application of 17403-09-7 This article mentions the following:

A series of 3-piperidin-4-yl-1H-indoles with building block diversity was synthesized based on a hit derived from an HTS whole-cell screen against Plasmodium falciparum. Thirty-eight compounds were obtained following a three-step synthetic approach and evaluated for antiparasitic activity. The SAR shows that 3-piperidin-4-yl-1H-indole is intolerant to most N-piperidinyl modifications. Nevertheless, the authors were able to identify a new compound with lead-like properties (MW = 305; cLogP = 2.42), showing antimalarial activity against drug-resistant and sensitive strains (EC50 values 鈭?3 渭M), selectivity for malaria parasite and no cross-resistance with chloroquine, thus representing a potential new chemotype for further optimization towards novel and affordable antimalarial drugs. The synthesis of the target compounds was achieved using 3-(4-piperidinyl)-1H-indole and 4,6-dichloroquinoline as key reactants. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Application of 17403-09-7).

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 17403-09-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Herold, Franciszek et al. published their research in European Journal of Medicinal Chemistry in 2010 | CAS: 17403-09-7

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole

Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity. part 3 was written by Herold, Franciszek;Chodkowski, Andrzej;Izbicki, Lukasz;Turlo, Jadwiga;Dawidowski, Maciej;Kleps, Jerzy;Nowak, Gabriel;Stachowicz, Katarzyna;Dybala, Malgorzata;Siwek, Agata;Mazurek, Aleksander P.;Mazurek, Andrzej;Plucinski, Franciszek. And the article was included in European Journal of Medicinal Chemistry in 2010.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole This article mentions the following:

A number of 4-aryl-5,6,7,8-tetrahydropyrido[1,2-c]pyrimidines with 3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole or 2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole residues were synthesized for further investigation of SAR in a group of pyrido[1,2-c]pyrimidine derivatives with dual 5-HT1A/SERT activity. Synthesized compounds were found to be potent ligands for both 5-HT1A and SERT with Ki ranging from 28.3 to 642 nM and 42.4 nM to 1.8 μM, resp. Moreover some compounds were found to be selective agonists, while compound I as an antagonist of 5-HT1A presynaptic receptors in the inducible hypothermia test in mice. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole).

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Santos, Sofia A. et al. published their research in European Journal of Medicinal Chemistry in 2015 | CAS: 17403-09-7

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 17403-09-7

Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype was written by Santos, Sofia A.;Lukens, Amanda K.;Coelho, Lis;Nogueira, Fatima;Wirth, Dyann F.;Mazitschek, Ralph;Moreira, Rui;Paulo, Alexandra. And the article was included in European Journal of Medicinal Chemistry in 2015.Application of 17403-09-7 This article mentions the following:

A series of 3-piperidin-4-yl-1H-indoles with building block diversity was synthesized based on a hit derived from an HTS whole-cell screen against Plasmodium falciparum. Thirty-eight compounds were obtained following a three-step synthetic approach and evaluated for antiparasitic activity. The SAR shows that 3-piperidin-4-yl-1H-indole is intolerant to most N-piperidinyl modifications. Nevertheless, the authors were able to identify a new compound with lead-like properties (MW = 305; cLogP = 2.42), showing antimalarial activity against drug-resistant and sensitive strains (EC50 values ∼ 3 μM), selectivity for malaria parasite and no cross-resistance with chloroquine, thus representing a potential new chemotype for further optimization towards novel and affordable antimalarial drugs. The synthesis of the target compounds was achieved using 3-(4-piperidinyl)-1H-indole and 4,6-dichloroquinoline as key reactants. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Application of 17403-09-7).

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 17403-09-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Herold, Franciszek et al. published their research in European Journal of Medicinal Chemistry in 2010 | CAS: 17403-09-7

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole

Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity. part 3 was written by Herold, Franciszek;Chodkowski, Andrzej;Izbicki, Lukasz;Turlo, Jadwiga;Dawidowski, Maciej;Kleps, Jerzy;Nowak, Gabriel;Stachowicz, Katarzyna;Dybala, Malgorzata;Siwek, Agata;Mazurek, Aleksander P.;Mazurek, Andrzej;Plucinski, Franciszek. And the article was included in European Journal of Medicinal Chemistry in 2010.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole This article mentions the following:

A number of 4-aryl-5,6,7,8-tetrahydropyrido[1,2-c]pyrimidines with 3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole or 2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole residues were synthesized for further investigation of SAR in a group of pyrido[1,2-c]pyrimidine derivatives with dual 5-HT1A/SERT activity. Synthesized compounds were found to be potent ligands for both 5-HT1A and SERT with Ki ranging from 28.3 to 642 nM and 42.4 nM to 1.8 μM, resp. Moreover some compounds were found to be selective agonists, while compound I as an antagonist of 5-HT1A presynaptic receptors in the inducible hypothermia test in mice. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole).

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application In Synthesis of 3-(Piperidin-4-yl)-1H-indole

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Santos, Sofia A. et al. published their research in European Journal of Medicinal Chemistry in 2015 | CAS: 17403-09-7

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 17403-09-7

Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype was written by Santos, Sofia A.;Lukens, Amanda K.;Coelho, Lis;Nogueira, Fatima;Wirth, Dyann F.;Mazitschek, Ralph;Moreira, Rui;Paulo, Alexandra. And the article was included in European Journal of Medicinal Chemistry in 2015.Application of 17403-09-7 This article mentions the following:

A series of 3-piperidin-4-yl-1H-indoles with building block diversity was synthesized based on a hit derived from an HTS whole-cell screen against Plasmodium falciparum. Thirty-eight compounds were obtained following a three-step synthetic approach and evaluated for antiparasitic activity. The SAR shows that 3-piperidin-4-yl-1H-indole is intolerant to most N-piperidinyl modifications. Nevertheless, the authors were able to identify a new compound with lead-like properties (MW = 305; cLogP = 2.42), showing antimalarial activity against drug-resistant and sensitive strains (EC50 values ∼ 3 μM), selectivity for malaria parasite and no cross-resistance with chloroquine, thus representing a potential new chemotype for further optimization towards novel and affordable antimalarial drugs. The synthesis of the target compounds was achieved using 3-(4-piperidinyl)-1H-indole and 4,6-dichloroquinoline as key reactants. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Application of 17403-09-7).

3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 17403-09-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem