Category: 159326-69-9

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 Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology, Author is Johannes, Jeffrey W.; Almeida, Lynsie; Barlaam, Bernard; Boriack-Sjodin, P. Ann; Casella, Robert; Croft, Rosemary A.; Dishington, Allan P.; Gingipalli, Lakshmaiah; Gu, Chungang; Hawkins, Janet L.; Holmes, Jane L.; Howard, Tina; Huang, Jian; Ioannidis, Stephanos; Kazmirski, Steven; Lamb, Michelle L.; McGuire, Thomas M.; Moore, Jane E.; Ogg, Derek; Patel, Anil; Pike, Kurt G.; Pontz, Timothy; Robb, Graeme R.; Su, Nancy; Wang, Haiyun; Wu, Xiaoyun; Zhang, Hai-Jun; Zhang, Yue; Zheng, Xiaolan; Wang, Tao, which mentions a compound: 159326-69-9, SMILESS is O=C(C1=CC=CN1N)N, Molecular C5H7N3O, Name: 1-Aminopyrrole-2-carboxamide.

The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ss-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is known to inhibit the Wnt pathway via increased stabilization of Axin. In order to explore the consequences of tankyrase and Wnt pathway inhibition in preclin. models of cancer and its impact on normal tissue, the authors sought a small mol. inhibitor of TNKS1/2 with suitable physicochem. properties and pharmacokinetics for hypothesis testing in vivo. Starting from a 2-Ph quinazolinone hit I, the authors discovered the pyrrolopyrimidinone compound II (AZ6102), which is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. Moreover, compound II can be formulated well in a clin. relevant i.v. solution at 20 mg/mL, has demonstrated good pharmacokinetics in preclin. species, and shows low Caco2 efflux to avoid possible tumor resistance mechanisms.

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Chen, Yanhong; Xiang, Haoyue; Tan, Cun; Xie, Yuyuan; Yang, Chunhao published the article 《A tandem copper (II)-promoted synthesis of 2-substituted pyrrolo[2,1-f][1,2,4] triazin-4(3H)-ones》. Keywords: aldehyde aminopyrroleamide annulation cupric chloride catalyst; acetal aminopyrroleamide annulation cupric chloride catalyst; pyrrolotriazinone preparation.They researched the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ).Application of 159326-69-9. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:159326-69-9) here.

Annulation of 1-amino-1H-pyrrole-2-amides with various substituted benzaldehydes, heteroaryl aldehydes, alkyl aldehydes or even acetals, promoted by cupric chloride, to synthesize 2-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones was carried out. This approach provides a useful method for constructing the privileged structure in medicinal chem. Electron-donating groups on both partners could accelerate the reaction.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Synthesis of pyrrolo[2,1-f][1,2,4]triazine congeners of nucleic acid purines via the N-amination of 2-substituted pyrroles, published in 1994-08-31, which mentions a compound: 159326-69-9, Name is 1-Aminopyrrole-2-carboxamide, Molecular C5H7N3O, Application In Synthesis of 1-Aminopyrrole-2-carboxamide.

The synthesis of several new 4-mono- and 2,4-disubstituted pyrrolo[2,1-f][1,2,4]triazines is described. Key intermediates 1-aminopyrrole-2-carbonitrile (3) and 1-amino-5-ethylpyrrole-2-carbonitrile (15) were obtained by N-amination of the corresponding pyrrole-2-carboxaldehyde followed by CHO → CN conversion with either hydroxylamine-O-sulfonic acid for 3 or O-mesitylenesulfonylhydroxylamine for 15. Cyclization of 3 or 15 with a variety of amidine reagents or, after conversion of 3 to its corresponding amide, base-catalyzed annulation completed the synthesis of the title products.

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Patil, Shirish A.; Otter, Brian A.; Klein, Robert S. published an article about the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9,SMILESS:O=C(C1=CC=CN1N)N ).Quality Control of 1-Aminopyrrole-2-carboxamide. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:159326-69-9) through the article.

The synthesis of several new 4-mono- and 2,4-disubstituted pyrrolo[2,1-f][1,2,4]triazines is described. Key intermediates 1-aminopyrrole-2-carbonitrile (3) and 1-amino-5-ethylpyrrole-2-carbonitrile (15) were obtained by N-amination of the corresponding pyrrole-2-carboxaldehyde followed by CHO → CN conversion with either hydroxylamine-O-sulfonic acid for 3 or O-mesitylenesulfonylhydroxylamine for 15. Cyclization of 3 or 15 with a variety of amidine reagents or, after conversion of 3 to its corresponding amide, base-catalyzed annulation completed the synthesis of the title products.

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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, Synthesis called Synthesis of Novel Hydroxymethyl-Substituted Fused Heterocycles, Author is Holmes, Jane L.; Almeida, Lynsie; Barlaam, Bernard; Croft, Rosemary A.; Dishington, Allan P.; Gingipalli, Laksmaiah; Hassall, Lorraine A.; Hawkins, Janet L.; Ioannidis, Stephanos; Johannes, Jeffrey W.; McGuire, Thomas M.; Moore, Jane E.; Patel, Anil; Pike, Kurt G.; Pontz, Timothy; Wu, Xiaoyun; Wang, Tao; Zhang, Hai-Jun; Zheng, Xiaolan, which mentions a compound: 159326-69-9, SMILESS is O=C(C1=CC=CN1N)N, Molecular C5H7N3O, Related Products of 159326-69-9.

Examples of hydroxymethylated analogs of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones were sparse or non-existent in the scientific literature. Synthesis of such compounds by using standard procedures from readily available raw materials was demonstrated.

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Product Details of 159326-69-9. 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: 1-Aminopyrrole-2-carboxamide, is researched, Molecular C5H7N3O, CAS is 159326-69-9, about Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology. Author is Johannes, Jeffrey W.; Almeida, Lynsie; Barlaam, Bernard; Boriack-Sjodin, P. Ann; Casella, Robert; Croft, Rosemary A.; Dishington, Allan P.; Gingipalli, Lakshmaiah; Gu, Chungang; Hawkins, Janet L.; Holmes, Jane L.; Howard, Tina; Huang, Jian; Ioannidis, Stephanos; Kazmirski, Steven; Lamb, Michelle L.; McGuire, Thomas M.; Moore, Jane E.; Ogg, Derek; Patel, Anil; Pike, Kurt G.; Pontz, Timothy; Robb, Graeme R.; Su, Nancy; Wang, Haiyun; Wu, Xiaoyun; Zhang, Hai-Jun; Zhang, Yue; Zheng, Xiaolan; Wang, Tao.

The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ss-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is known to inhibit the Wnt pathway via increased stabilization of Axin. In order to explore the consequences of tankyrase and Wnt pathway inhibition in preclin. models of cancer and its impact on normal tissue, the authors sought a small mol. inhibitor of TNKS1/2 with suitable physicochem. properties and pharmacokinetics for hypothesis testing in vivo. Starting from a 2-Ph quinazolinone hit I, the authors discovered the pyrrolopyrimidinone compound II (AZ6102), which is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. Moreover, compound II can be formulated well in a clin. relevant i.v. solution at 20 mg/mL, has demonstrated good pharmacokinetics in preclin. species, and shows low Caco2 efflux to avoid possible tumor resistance mechanisms.

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Thiazole | C3H3NS – PubChem,
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Chen, Jianyang; Liu, Bo; Chen, Yanhong; He, Qian; Yang, Chunhao published an article about the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9,SMILESS:O=C(C1=CC=CN1N)N ).COA of Formula: C5H7N3O. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:159326-69-9) through the article.

A copper(II)-catalyzed coupling-cyclization reaction that allowed a facile access to an impressive variety of pyrrolo[2,1-f][1,2,4]triazine-fused isoquinolines, e.g., I, in good to excellent yields has been developed. The reaction proceeded with high 6-endo-dig regioselectivity, and the product was confirmed by x-ray crystallog. study. This method appeared to be compatible with different substituted starting materials that have different electronic properties, increasing its applicability to various functional groups.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ) is researched.Application In Synthesis of 1-Aminopyrrole-2-carboxamide.Xin, Minhang; Zhang, Liandi; Tang, Feng; Tu, Chongxing; Wen, Jun; Zhao, Xinge; Liu, Zhaoyu; Cheng, Lingfei; Shen, Han published the article 《Design, synthesis, and evaluation of pyrrolo[2,1-f][1,2,4]triazine derivatives as novel hedgehog signaling pathway inhibitors》 about this compound( cas:159326-69-9 ) in Bioorganic & Medicinal Chemistry. Keywords: pyrrolotriazine derivative preparation SAR hedgehog signaling inhibitor cancer; Hedgehog signaling pathway; Inhibitors; Novel; Pyrrolo[2,1-f][1,2,4]triazine. Let’s learn more about this compound (cas:159326-69-9).

A novel series of Hh signaling pathway inhibitors were designed by replacing the pyrimidine skeleton of our earlier reported lead compound with pyrrolo[2,1-f][1,2,4]triazine scaffold. Starting from this new scaffold, SAR exploration was investigated based on structural modification on A-ring, C-ring and D-ring. And several much potent compounds were studies in vivo to profile their pharmacokinetic properties. Finally, optimization leads to the identification of compound (I), a potent Hh signaling pathway inhibitor with superior potency in vitro and satisfactory pharmacokinetic properties in vivo.

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Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ) is researched.Product Details of 159326-69-9.Chen, Yanhong; Xiang, Haoyue; Tan, Cun; Xie, Yuyuan; Yang, Chunhao published the article 《A tandem copper (II)-promoted synthesis of 2-substituted pyrrolo[2,1-f][1,2,4] triazin-4(3H)-ones》 about this compound( cas:159326-69-9 ) in Tetrahedron. Keywords: aldehyde aminopyrroleamide annulation cupric chloride catalyst; acetal aminopyrroleamide annulation cupric chloride catalyst; pyrrolotriazinone preparation. Let’s learn more about this compound (cas:159326-69-9).

Annulation of 1-amino-1H-pyrrole-2-amides with various substituted benzaldehydes, heteroaryl aldehydes, alkyl aldehydes or even acetals, promoted by cupric chloride, to synthesize 2-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones was carried out. This approach provides a useful method for constructing the privileged structure in medicinal chem. Electron-donating groups on both partners could accelerate the reaction.

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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ) is researched.Electric Literature of C5H7N3O.Sampognaro, Anthony J.; Wittman, Mark D.; Carboni, Joan M.; Chang, Chiehying; Greer, Ann F.; Hurlburt, Warren W.; Sack, John S.; Vyas, Dolatrai M. published the article 《Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase》 about this compound( cas:159326-69-9 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: isosteric proline replacement pyrrolo triazine inhibitor IGF1R kinase structure. Let’s learn more about this compound (cas:159326-69-9).

Pyrrolidine, pyrrolidinone, carbocyclic, and acyclic groups were used as isosteric proline replacements in a series of insulin-like growth factor I receptor kinase/insulin receptor kinase inhibitors. Examples that were similar in potency to proline-containing reference compounds were shown to project a key fluoropyridine amide into a common space, while less potent compounds were not able to do so for reasons of stereochem. or structural rigidity.

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