Category: 159326-69-9

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.Reference of 1-Aminopyrrole-2-carboxamide.Xiang, Haoyue; Chen, Yanhong; He, Qian; Xie, Yuyuan; Yang, Chunhao published the article 《Pot, atom and step economic synthesis: a diversity-oriented approach to construct 2-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones》 about this compound( cas:159326-69-9 ) in RSC Advances. Keywords: pyrrolecarboxamide chromonecarboxaldehyde amidine heterocyclization; pyrimidinyl aryl pyrrolotriazinone preparation; chromonecarboxaldehyde pyrrolecarboxamide hydrazine heterocyclization; pyrazolyl aryl pyrrolotriazinone preparation. Let’s learn more about this compound (cas:159326-69-9).

A diversity-oriented approach to the synthesis of pyrimidinyl-/pyrazolyl-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones, e.g., I and II, via copper-promoted two-step one-pot reaction of chromones with pyrrolecarboxamides and amidines/hydrazines was developed. Pot, atom and step economy were combined in these sequential reactions, and at least six bonds were formed in one pot.

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

Quality Control of 1-Aminopyrrole-2-carboxamide. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 1-Aminopyrrole-2-carboxamide, is researched, Molecular C5H7N3O, CAS is 159326-69-9, about Synthesis of pyrrolo[2,1-f][1,2,4]triazine congeners of nucleic acid purines via the N-amination of 2-substituted pyrroles. Author is Patil, Shirish A.; Otter, Brian A.; Klein, Robert S..

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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Thiazole | C3H3NS – PubChem,
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Recommanded Product: 1-Aminopyrrole-2-carboxamide. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-Aminopyrrole-2-carboxamide, is researched, Molecular C5H7N3O, CAS is 159326-69-9, about Pot, atom and step economic synthesis: a diversity-oriented approach to construct 2-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones.

A diversity-oriented approach to the synthesis of pyrimidinyl-/pyrazolyl-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones, e.g., I and II, via copper-promoted two-step one-pot reaction of chromones with pyrrolecarboxamides and amidines/hydrazines was developed. Pot, atom and step economy were combined in these sequential reactions, and at least six bonds were formed in one pot.

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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.Category: thiazole.Jia, Hong; Dai, Guangxiu; Su, Weiguo; Xiao, Kun; Weng, Jianyang; Zhang, Zhulin; Wang, Qing; Yuan, Tianhai; Shi, Fuying; Zhang, Zheng; Chen, Wei; Sai, Yang; Wang, Jian; Li, Xiong; Cai, Yu; Yu, Jun; Ren, Ping; Venable, Jennifer; Rao, Tadimeti; Edwards, James P.; Bembenek, Scott D. published the article 《Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors》 about this compound( cas:159326-69-9 ) in Journal of Medicinal Chemistry. Keywords: pyrrolotriazinone synthesis SAR pharmacokinetics PI3K rheumatoid arthritis autoimmune disorders. Let’s learn more about this compound (cas:159326-69-9).

An electronic d. model was developed and used to identify a novel pyrrolotriazinone replacement for a quinazolinone, a commonly used moiety to impart selectivity in inhibitors for PI3Kγ and PI3Kδ. Guided by mol. docking, this new specificity piece was then linked to the hinge-binding region of the inhibitor using a novel cyclic moiety. Further structure-activity relationship optimization around the hinge region led to the discovery of candidate 26, a highly potent and selective PI3Kγ-PI3Kδ dual inhibitor with favorable drug metabolism and pharmacokinetic properties in preclin. species.

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Thiazole | C3H3NS – PubChem,
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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 159326-69-9, is researched, Molecular C5H7N3O, about Discovery of the Pyrrolo[2,1-f][1,2,4]triazine Nucleus as a New Kinase Inhibitor Template, the main research direction is pyrrolotriazine derivative preparation structure activity VEGF EGFR kinase antitumor.Reference of 1-Aminopyrrole-2-carboxamide.

The pyrrolo[2,1-f][1,2,4]triazine nucleus was identified as a novel kinase inhibitor template which effectively mimics the well-known quinazoline kinase inhibitor scaffold. Attachment of a 4-((3-chloro-4-fluorophenyl)amino) substituent to the template provided potent biochem. inhibitors of the tyrosine kinase activity of EGFR, as well as inhibition of cellular proliferation of the human colon tumor cell line DiFi. Attachment of a 4-((3-hydroxy-4-methylphenyl)amino) substituent provided potent inhibitors of VEGFR-2 which also showed effects on the VEGF-dependent proliferation of human umbilical vein endothelial cells. Biol. activity was maintained with substitution at positions 5 or 6, but not 7, suggesting that the former positions are promising sites for introducing side chains which modulate physicochem. properties. Preliminary inhibition studies with varying ATP concentrations suggest that, like the quinazoline-based kinase inhibitors, the pyrrolotriazine-based inhibitors bind in the ATP pocket.

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

Quality Control of 1-Aminopyrrole-2-carboxamide. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 1-Aminopyrrole-2-carboxamide, is researched, Molecular C5H7N3O, CAS is 159326-69-9, about Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors. Author is Jia, Hong; Dai, Guangxiu; Su, Weiguo; Xiao, Kun; Weng, Jianyang; Zhang, Zhulin; Wang, Qing; Yuan, Tianhai; Shi, Fuying; Zhang, Zheng; Chen, Wei; Sai, Yang; Wang, Jian; Li, Xiong; Cai, Yu; Yu, Jun; Ren, Ping; Venable, Jennifer; Rao, Tadimeti; Edwards, James P.; Bembenek, Scott D..

An electronic d. model was developed and used to identify a novel pyrrolotriazinone replacement for a quinazolinone, a commonly used moiety to impart selectivity in inhibitors for PI3Kγ and PI3Kδ. Guided by mol. docking, this new specificity piece was then linked to the hinge-binding region of the inhibitor using a novel cyclic moiety. Further structure-activity relationship optimization around the hinge region led to the discovery of candidate 26, a highly potent and selective PI3Kγ-PI3Kδ dual inhibitor with favorable drug metabolism and pharmacokinetic properties in preclin. species.

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

Synthetic Route of C5H7N3O. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. 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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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

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 published an article about the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9,SMILESS:O=C(C1=CC=CN1N)N ).Application In Synthesis 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 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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Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Xin, Minhang; Zhang, Liandi; Tang, Feng; Tu, Chongxing; Wen, Jun; Zhao, Xinge; Liu, Zhaoyu; Cheng, Lingfei; Shen, Han published an article about the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9,SMILESS:O=C(C1=CC=CN1N)N ).Safety 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.

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

Safety of 1-Aminopyrrole-2-carboxamide. 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 Discovery of the Pyrrolo[2,1-f][1,2,4]triazine Nucleus as a New Kinase Inhibitor Template. Author is Hunt, John T.; Mitt, Toomas; Borzilleri, Robert; Gullo-Brown, Johnni; Fargnoli, Joseph; Fink, Brian; Han, Wen-Ching; Mortillo, Steven; Vite, Gregory; Wautlet, Barri; Wong, Tai; Yu, Chiang; Zheng, Xiaoping; Bhide, Rajeev.

The pyrrolo[2,1-f][1,2,4]triazine nucleus was identified as a novel kinase inhibitor template which effectively mimics the well-known quinazoline kinase inhibitor scaffold. Attachment of a 4-((3-chloro-4-fluorophenyl)amino) substituent to the template provided potent biochem. inhibitors of the tyrosine kinase activity of EGFR, as well as inhibition of cellular proliferation of the human colon tumor cell line DiFi. Attachment of a 4-((3-hydroxy-4-methylphenyl)amino) substituent provided potent inhibitors of VEGFR-2 which also showed effects on the VEGF-dependent proliferation of human umbilical vein endothelial cells. Biol. activity was maintained with substitution at positions 5 or 6, but not 7, suggesting that the former positions are promising sites for introducing side chains which modulate physicochem. properties. Preliminary inhibition studies with varying ATP concentrations suggest that, like the quinazoline-based kinase inhibitors, the pyrrolotriazine-based inhibitors bind in the ATP pocket.

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