Tag: 275.2998

Development of a Highly Potent D₂/D₃ Agonist and a Partial Agonist from Structure-Activity Relationship Study of N⁶-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N⁶-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson’s Disease was written by Das, Banibrata;Vedachalam, Seenuvasan;Luo, Dan;Antonio, Tamara;Reith, Maarten E. A.;Dutta, Aloke K.. And the article was included in Journal of Medicinal Chemistry in 2015.Product Details of 324756-80-1 This article mentions the following:

The structure-activity relationship studies with N⁶-(2-(4-(1H-indol-5-yl)piperazin-1-yl)ethyl)-N⁶-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine derivatives led to development of a lead compound I which exhibited very high affinity (K_i, D₂ = 16.4 nM, D₃ = 1.15 nM) and full agonist activity (EC₅₀ (GTP纬S); D₂ = 3.23 and D₃ = 1.41 nM) at both D₂ and D₃ receptors. A partial agonist mol. II (EC₅₀ (GTP纬S); D₂ = 21.6 (E_max = 27%) and D₃ = 10.9 nM) was also identified. In a Parkinson’s disease (PD) animal model, I was highly efficacious in reversing hypolocomotion in reserpinized rats with a long duration of action, indicating its potential as an anti-PD drug. Compound II was also able to elevate locomotor activity in the above PD animal model significantly, implying its potential application in PD therapy. Furthermore, I was shown to be neuroprotective in protecting neuronal PC12 from toxicity of 6-OHDA. This report, therefore, underpins the notion that a multifunctional drug like I might have the potential not only to ameliorate motor dysfunction in PD patients but also to modify disease progression by protecting DA neurons from progressive degeneration. In the experiment, the researchers used many compounds, for example, tert-Butyl 3-formyl-5-methoxy-1H-indole-1-carboxylate (cas: 324756-80-1Product Details of 324756-80-1).

tert-Butyl 3-formyl-5-methoxy-1H-indole-1-carboxylate (cas: 324756-80-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Product Details of 324756-80-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Development of a Highly Potent D₂/D₃ Agonist and a Partial Agonist from Structure-Activity Relationship Study of N⁶-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N⁶-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson’s Disease was written by Das, Banibrata;Vedachalam, Seenuvasan;Luo, Dan;Antonio, Tamara;Reith, Maarten E. A.;Dutta, Aloke K.. And the article was included in Journal of Medicinal Chemistry in 2015.Product Details of 324756-80-1 This article mentions the following:

The structure-activity relationship studies with N⁶-(2-(4-(1H-indol-5-yl)piperazin-1-yl)ethyl)-N⁶-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine derivatives led to development of a lead compound I which exhibited very high affinity (K_i, D₂ = 16.4 nM, D₃ = 1.15 nM) and full agonist activity (EC₅₀ (GTPγS); D₂ = 3.23 and D₃ = 1.41 nM) at both D₂ and D₃ receptors. A partial agonist mol. II (EC₅₀ (GTPγS); D₂ = 21.6 (E_max = 27%) and D₃ = 10.9 nM) was also identified. In a Parkinson’s disease (PD) animal model, I was highly efficacious in reversing hypolocomotion in reserpinized rats with a long duration of action, indicating its potential as an anti-PD drug. Compound II was also able to elevate locomotor activity in the above PD animal model significantly, implying its potential application in PD therapy. Furthermore, I was shown to be neuroprotective in protecting neuronal PC12 from toxicity of 6-OHDA. This report, therefore, underpins the notion that a multifunctional drug like I might have the potential not only to ameliorate motor dysfunction in PD patients but also to modify disease progression by protecting DA neurons from progressive degeneration. In the experiment, the researchers used many compounds, for example, tert-Butyl 3-formyl-5-methoxy-1H-indole-1-carboxylate (cas: 324756-80-1Product Details of 324756-80-1).

tert-Butyl 3-formyl-5-methoxy-1H-indole-1-carboxylate (cas: 324756-80-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Product Details of 324756-80-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Development of a Highly Potent D₂/D₃ Agonist and a Partial Agonist from Structure-Activity Relationship Study of N⁶-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N⁶-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson’s Disease was written by Das, Banibrata;Vedachalam, Seenuvasan;Luo, Dan;Antonio, Tamara;Reith, Maarten E. A.;Dutta, Aloke K.. And the article was included in Journal of Medicinal Chemistry in 2015.Product Details of 324756-80-1 This article mentions the following:

The structure-activity relationship studies with N⁶-(2-(4-(1H-indol-5-yl)piperazin-1-yl)ethyl)-N⁶-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine derivatives led to development of a lead compound I which exhibited very high affinity (K_i, D₂ = 16.4 nM, D₃ = 1.15 nM) and full agonist activity (EC₅₀ (GTPγS); D₂ = 3.23 and D₃ = 1.41 nM) at both D₂ and D₃ receptors. A partial agonist mol. II (EC₅₀ (GTPγS); D₂ = 21.6 (E_max = 27%) and D₃ = 10.9 nM) was also identified. In a Parkinson’s disease (PD) animal model, I was highly efficacious in reversing hypolocomotion in reserpinized rats with a long duration of action, indicating its potential as an anti-PD drug. Compound II was also able to elevate locomotor activity in the above PD animal model significantly, implying its potential application in PD therapy. Furthermore, I was shown to be neuroprotective in protecting neuronal PC12 from toxicity of 6-OHDA. This report, therefore, underpins the notion that a multifunctional drug like I might have the potential not only to ameliorate motor dysfunction in PD patients but also to modify disease progression by protecting DA neurons from progressive degeneration. In the experiment, the researchers used many compounds, for example, tert-Butyl 3-formyl-5-methoxy-1H-indole-1-carboxylate (cas: 324756-80-1Product Details of 324756-80-1).

tert-Butyl 3-formyl-5-methoxy-1H-indole-1-carboxylate (cas: 324756-80-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Product Details of 324756-80-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles