Tag: 197.25

Synthesis of thieno[2,3-d]oxazines and thieno[2,3-d]thiazines as subtype specific kainate receptor antagonists was written by Briel, D.;Rybak, A.;Mann, S.;Kronbach, C.;Unverferth, K.. And the article was included in Current Medicinal Chemistry in 2009.Computed Properties of C9H11NO2S This article mentions the following:

For the development of new antiepileptics the kainate receptors, GluR6 and GluR5, are important targets. Based on the anticonvulsant effects of chinazolines and thieno[2,3-d]pyrimidines that are known from the literature, thieno[2,3-d][1.3]oxazines were synthesized and studied for their inhibitory properties at GluR6 and GluR5 receptors. The strongest inhibitor activity was observed with 5-methyl-6-phenyl-thieno[2,3-d][1.3]oxazines with Cl or C3-substituents in position 2. The 2-trihalide-methyl-substituted compounds were the most active inhibitors at the GluR5-receptor (IC₅₀ = 23.4 μmol, 16 μl). The 2-isopropyl-substituted compound displayed the strongest activity at the GluR6-receptor (IC₅₀ = 8.7 μmol). A number of thieno[2,3-d][1.3]thiazines and thieno[2,3-d]pyrimidines that were synthesized from the thieno[2,3][1.3]oxazines did not show any activity. In the experiment, the researchers used many compounds, for example, 2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid (cas: 5936-58-3Computed Properties of C9H11NO2S).

2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid (cas: 5936-58-3) belongs to benzothiophene derivatives. Benzothiophene scaffolds are of great importance due to its increased presence in bioactive molecules. It is also used in the manufacturing of dyes such as thioindigo.Computed Properties of C9H11NO2S

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Thiophene/thiazole-benzene replacement on guanidine derivatives targeting α₂-Adrenoceptors was written by Flood, Aoife;Trujillo, Cristina;Sanchez-Sanz, Goar;Kelly, Brendan;Muguruza, Carolina;Callado, Luis F.;Rozas, Isabel. And the article was included in European Journal of Medicinal Chemistry in 2017.Reference of 5936-58-3 This article mentions the following:

Searching for improved antagonists of α₂-adrenoceptors, a thorough theor. study comparing the aromaticity of phenyl-, pyridinyl-, thiophenyl- and thiazolylguanidinium derivatives were carried out [at M06-2X/6-311++G(p,d) computational level] confirming that thiophene and thiazole were good ‘ring equivalent’ to benzene in these guanidinium systems. Based on these results, a small but chem. diverse library of guanidine derivatives were synthesized to explore the effect that the bioisosteric change has on affinity and activity at α₂-adrenoceptors in comparison with our previously studied Ph derivatives All compounds were tested for their α₂-adrenoceptor affinity and unsubstituted guanidinothiophenes displayed the strongest affinities in the same range as the Ph analogs. In the case of cycloalkyl systems, thiophenes with 6-membered rings showed the largest affinities, while for the thiazoles the 5-membered analog presented the strongest affinity. From all the compounds tested for noradrenergic activity, only one compound exhibited agonistic activity, while two compounds showed very promising antagonism of α₂-adrenoceptors. In the experiment, the researchers used many compounds, for example, 2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid (cas: 5936-58-3Reference of 5936-58-3).

2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid (cas: 5936-58-3) belongs to benzothiophene derivatives. Benzothiophene is a fused ring compound of thiophene ring and benzene ring, which is an important class of heterocycles with advantageous structures. It is found within the chemical structures of pharmaceutical drugs such as zileuton, raloxifene, and sertaconazole, and also BTCP.Reference of 5936-58-3

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Thiophene bioisosteres. Synthesis of 2-methyl-4-oxothieno [2,3-d] pyrimidines was written by Noverola, Salvador Vega. And the article was included in Anales de la Real Academia de Farmacia in 1976.Computed Properties of C9H11NO2S This article mentions the following:

Thienopyrimidinones I [RR1 = (CH2)4, R = Me, R1 = H; R2 = (CH2)3OCHMe2, NHCO2Et, NHCOCH2Ph, NHBz, (CH2)nNR3R4, n = 2, 3, NR3R4 = NMe2, NEt2, morpholino, pyrrolidino] were prepared by treating cyclohexanone and S or HSCH2COMe with NCCH2CO2Et, acetylating II (R5 = H, R6 = Et), hydrolyzing, cyclizing II (R5 = Ac, R6 = H) with Ac2O, and treating the oxazines III with R2NH2 with prolonged heating. Intermediates IV of the reaction of III with R2NH2 were isolated at shorter reaction times. In the experiment, the researchers used many compounds, for example, 2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid (cas: 5936-58-3Computed Properties of C9H11NO2S).

2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid (cas: 5936-58-3) belongs to benzothiophene derivatives. Benzothiophenes are valuable heterocycles that are widely used in medicines, agrochemicals, and materials science. It is found within the chemical structures of pharmaceutical drugs such as raloxifene, zileuton, sertaconazole, and also BTCP.Computed Properties of C9H11NO2S

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem