Category: 87-63-8

Formula: C7H8ClN. In 2020 SYNTHETIC COMMUN published article about DERIVATIVES; BENZOTHIAZOLE; 2-MERCAPTO; DESIGN in [Tung, Truong Thanh; Huy, Luong Xuan] PHENIKAA Univ, Fac Pharm, Hanoi 12116, Vietnam; [Tung, Truong Thanh; Huy, Luong Xuan] PHENIKAA Univ, PHENIKAA Inst Adv Study PIAS, Hanoi, Vietnam in 2020, Cited 17. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8.

A simple, efficient, and metal-free methodology for the preparation of 2-mercaptobenzothiazole and derivatives in excellent yields via microwave-assisted pathway is reported. Our condition provides a convenient protocol for the synthesis of a diverse collection of 2-mercaptobenzothiazoles and 6-(4-substituted-1H-1,2,3-triazol-1-yl)-2-mercaptobenzothiazoles with a very simple purification process. This report provides an alternative protocol for fast access to the wide range of compounds for sequence synthesis and biological studies.

Welcome to talk about 87-63-8, If you have any questions, you can contact Tung, TT; Huy, LX or send Email.. Formula: C7H8ClN

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

An article Chemical conversion of nicotinamide into type I positive allosteric modulator of alpha 7 nAChRs WOS:000471750200013 published article about ACETYLCHOLINE-RECEPTOR AGONIST; PHARMACOLOGICAL CHARACTERIZATION; IDENTIFICATION; APOPTOSIS; SUBUNIT; RELEASE in [Li, Xin; Xie, Wenjun; Huang, Zongze; Sun, Qi] Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China; [Xie, Wenjun; Wang, Xintong; Bian, Xiling; Wang, KeWei] Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China; [Wang, KeWei] Qingdao Univ, Sch Pharm, Dept Pharmacol, Qingdao 266021, Shandong, Peoples R China in 2019, Cited 38. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8. Category: chlorides-buliding-blocks

Structural modifications of nicotinamide, a form of vitamin B3, gave rise to a series of compounds (8aa-8ce) that exhibit activities as type I positive allosteric modulators (PAMs) of human alpha 7 nAChR expressed in Xenopus oocytes in two-electrode voltage clamp assay. The compound 8ai was a potent and efficacious PAM with an EC50 = 3.34 +/- 1.13 mu M and the maximum activation effect of alpha 7 current over 1474 +/- 246% in the presence of acetylcholine (100 mu M). It is highly specific to alpha 7 nAChR over other subtypes of nAChR and 5-HT3A receptors. The structure-activity relationship analysis identified a key skeleton of nicotinamide nucleus critical for biological activity. Taken together, the 8ai as a type I PAM of alpha 7 nAChR may be beneficial for improvement of cognitive deficit.

Category: chlorides-buliding-blocks. Welcome to talk about 87-63-8, If you have any questions, you can contact Li, X; Xie, WJ; Wang, XT; Huang, ZZ; Bian, XL; Wang, KW; Sun, Q or send Email.

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Authors Zhang, P; Zhao, XM in CHINESE JOURNAL STRUCTURAL CHEMISTRY published article about MESENCHYMAL STEM-CELLS; ADIPOSE-TISSUE; DENTAL-PULP; REGENERATION in [Zhang Peng; Zhao Xiao-Mei] Shaanxi Univ Chinese Med, Sch Pharm, Xianyang 712046, Shaanxi, Peoples R China in 2020, Cited 15. Name: 2-Chloro-6-methylaniline. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8

The heterocyclic compound 2-amino-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide (1), designed using 2-chloro-6-methylaniline (2) as the start material, was successfully obtained via multiple synthesis route and finally characterized by IR, H-1 NMR, and single-cystal X-ray crystallography. To select the suitable candidates for tissue regeneration, the induction activity of the compound on the dental pulp mesenchymal stem cells (DP-MSCs) was evaluated. Firstly, the DP-MSCs cells were isolated and the cell colon formation ability was measured after compound treatment with cell colony determination. After that, the RT-PCT assay was conducted and the relative expression level of the genes related with cell osteogenesis and proliferation was further detected.

Bye, fridends, I hope you can learn more about C7H8ClN, If you have any questions, you can browse other blog as well. See you lster.. Name: 2-Chloro-6-methylaniline

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

An article Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine WOS:000517673100012 published article about CELL LUNG-CANCER; IRREVERSIBLE INHIBITORS; FAMILY KINASES; DISCOVERY; GROWTH; RESISTANCE; PROTEIN; OPTIMIZATION; ACTIVATION; EXPRESSION in [Gurbani, Deepak; Westover, Kenneth D.; Zhang, Tinghu] Univ Texas Southwestern Med Ctr Dallas, Dept Biochem, Dallas, TX 75390 USA; [Gurbani, Deepak; Westover, Kenneth D.; Zhang, Tinghu] Univ Texas Southwestern Med Ctr Dallas, Dept Radiat Oncol, Dallas, TX 75390 USA; [Du, Guangyan; Rao, Suman; Henning, Nathaniel J.; Jiang, Jie; Che, Jianwei; Ficarro, Scott B.; Marto, Jarrod A.; Westover, Kenneth D.; Zhang, Tinghu; Gray, Nathanael S.] Harvard Med Sch, Dept Biol Chem & Mol Pharmacol, Boston, MA 02115 USA; [Du, Guangyan; Rao, Suman; Henning, Nathaniel J.; Jiang, Jie; Che, Jianwei; Westover, Kenneth D.; Zhang, Tinghu; Gray, Nathanael S.] Dana Farber Canc Inst, Dept Canc Biol, Boston, MA 02215 USA; [Yang, Annan; Aguirre, Andrew J.] Dana Farber Canc Inst, Dept Med Oncol, Boston, MA 02215 USA; [Sorger, Peter K.] Harvard Med Sch, Lab Syst Biol, Boston, MA 02115 USA in 2020, Cited 51. Computed Properties of C7H8ClN. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8

SRC is a major regulator of many signaling pathways and contributes to cancer development. However, development of a selective SRC inhibitor has been challenging, and FDA-approved SRC inhibitors, dasatinib and bosutinib, are multitargeted kinase inhibitors. Here, we describe our efforts to develop a selective SRC covalent inhibitor by targeting cysteine 277 on the P-loop of SRC. Using a promiscuous covalent kinase inhibitor (CKI) SM1-71 as a starting point, we developed covalent inhibitor 15a, which discriminates SRC from other covalent targets of SM1-71 including TAK1 and FGFR1. As an irreversible covalent inhibitor, compound 15a exhibited sustained inhibition of SRC signaling both in vitro and in vivo. Moreover, 15a exhibited potent antiproliferative effects in nonsmall cell lung cancer cell lines harboring SRC activation, thus providing evidence that this approach may be promising for further drug development efforts.

Computed Properties of C7H8ClN. Welcome to talk about 87-63-8, If you have any questions, you can contact Du, GY; Rao, SM; Gurbani, D; Henning, NJ; Jiang, J; Che, JW; Yang, A; Ficarro, SB; Marto, JA; Aguirre, AJ; Sorger, PK; Westover, KD; Zhang, TH; Gray, NS or send Email.

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Safety of 2-Chloro-6-methylaniline. In 2020 J MED CHEM published article about CELL LUNG-CANCER; IRREVERSIBLE INHIBITORS; FAMILY KINASES; DISCOVERY; GROWTH; RESISTANCE; PROTEIN; OPTIMIZATION; ACTIVATION; EXPRESSION in [Gurbani, Deepak; Westover, Kenneth D.; Zhang, Tinghu] Univ Texas Southwestern Med Ctr Dallas, Dept Biochem, Dallas, TX 75390 USA; [Gurbani, Deepak; Westover, Kenneth D.; Zhang, Tinghu] Univ Texas Southwestern Med Ctr Dallas, Dept Radiat Oncol, Dallas, TX 75390 USA; [Du, Guangyan; Rao, Suman; Henning, Nathaniel J.; Jiang, Jie; Che, Jianwei; Ficarro, Scott B.; Marto, Jarrod A.; Westover, Kenneth D.; Zhang, Tinghu; Gray, Nathanael S.] Harvard Med Sch, Dept Biol Chem & Mol Pharmacol, Boston, MA 02115 USA; [Du, Guangyan; Rao, Suman; Henning, Nathaniel J.; Jiang, Jie; Che, Jianwei; Westover, Kenneth D.; Zhang, Tinghu; Gray, Nathanael S.] Dana Farber Canc Inst, Dept Canc Biol, Boston, MA 02215 USA; [Yang, Annan; Aguirre, Andrew J.] Dana Farber Canc Inst, Dept Med Oncol, Boston, MA 02215 USA; [Sorger, Peter K.] Harvard Med Sch, Lab Syst Biol, Boston, MA 02115 USA in 2020, Cited 51. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8.

SRC is a major regulator of many signaling pathways and contributes to cancer development. However, development of a selective SRC inhibitor has been challenging, and FDA-approved SRC inhibitors, dasatinib and bosutinib, are multitargeted kinase inhibitors. Here, we describe our efforts to develop a selective SRC covalent inhibitor by targeting cysteine 277 on the P-loop of SRC. Using a promiscuous covalent kinase inhibitor (CKI) SM1-71 as a starting point, we developed covalent inhibitor 15a, which discriminates SRC from other covalent targets of SM1-71 including TAK1 and FGFR1. As an irreversible covalent inhibitor, compound 15a exhibited sustained inhibition of SRC signaling both in vitro and in vivo. Moreover, 15a exhibited potent antiproliferative effects in nonsmall cell lung cancer cell lines harboring SRC activation, thus providing evidence that this approach may be promising for further drug development efforts.

Safety of 2-Chloro-6-methylaniline. Bye, fridends, I hope you can learn more about C7H8ClN, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

An article Chemical conversion of nicotinamide into type I positive allosteric modulator of alpha 7 nAChRs WOS:000471750200013 published article about ACETYLCHOLINE-RECEPTOR AGONIST; PHARMACOLOGICAL CHARACTERIZATION; IDENTIFICATION; APOPTOSIS; SUBUNIT; RELEASE in [Li, Xin; Xie, Wenjun; Huang, Zongze; Sun, Qi] Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China; [Xie, Wenjun; Wang, Xintong; Bian, Xiling; Wang, KeWei] Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China; [Wang, KeWei] Qingdao Univ, Sch Pharm, Dept Pharmacol, Qingdao 266021, Shandong, Peoples R China in 2019, Cited 38. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8. SDS of cas: 87-63-8

Structural modifications of nicotinamide, a form of vitamin B3, gave rise to a series of compounds (8aa-8ce) that exhibit activities as type I positive allosteric modulators (PAMs) of human alpha 7 nAChR expressed in Xenopus oocytes in two-electrode voltage clamp assay. The compound 8ai was a potent and efficacious PAM with an EC50 = 3.34 +/- 1.13 mu M and the maximum activation effect of alpha 7 current over 1474 +/- 246% in the presence of acetylcholine (100 mu M). It is highly specific to alpha 7 nAChR over other subtypes of nAChR and 5-HT3A receptors. The structure-activity relationship analysis identified a key skeleton of nicotinamide nucleus critical for biological activity. Taken together, the 8ai as a type I PAM of alpha 7 nAChR may be beneficial for improvement of cognitive deficit.

SDS of cas: 87-63-8. Welcome to talk about 87-63-8, If you have any questions, you can contact Li, X; Xie, WJ; Wang, XT; Huang, ZZ; Bian, XL; Wang, KW; Sun, Q or send Email.

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Chen, C; Wang, YB; Shi, XN; Sun, W; Zhao, JH; Zhu, YP; Liu, LY; Zhu, BL in [Chen, Chen; Wang, Yuebo; Shi, Xiaonan; Sun, Wan; Zhao, Jinghui; Liu, Liying; Zhu, Bolin] Tianjin Normal Univ, Coll Chem, Tianjin Key Lab Struct & Peiformance Funct Mol, Tianjin 300387, Peoples R China; [Zhu, Yan-Ping] Collaborat Innovat Ctr Adv Drug Delivery Syst & B, Sch Pharm, Key Lab Mol Pharmacol & Drug Evaluat, Minist Educ, Yantai 264005, Shandong, Peoples R China published Palladium-Catalyzed C-2 and C-3 Dual C-H Functionalization of Indoles: Synthesis of Fluorinated Isocryptolepine Analogues in 2020, Cited 56. Formula: C7H8ClN. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8.

Here we report a protocol to synthesize diversiform fluorinated isocryptolepine analogues with potential biological activities in one step via directed C-2 and C-3 dual C-H functionalization of indoles. We also attempted to take into account fluorinated imidoyl chlorides as a novel kind of synthons in the directed C-H functionalization reactions. As a result, a variety of fluorinated isocryptolepine analogues were obtained in up to 96% yield. Moreover, we conducted control experiments to disclose the reaction mechanism.

Formula: C7H8ClN. Bye, fridends, I hope you can learn more about C7H8ClN, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

An article Design and Synthesis of Novel Positive Allosteric Modulators of alpha 7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice WOS:000455561400010 published article about VITRO PHARMACOLOGICAL CHARACTERIZATION; RELEASE; AGONIST; SCHIZOPHRENIA; DISCOVERY; TARGETS; SERIES; ACID in [Li, Yuanheng; Jiao, Wenxuan; Huang, Zongze; Meng, Ying; Luo, Laichun; Wang, KeWei; Sun, Qi] Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China; [Sun, Lilan; Zhang, Fang; Wang, KeWei] Qingdao Univ, Sch Pharm, Dept Pharmacol, Qingdao 266021, Peoples R China; [Yang, Taoyi; Tang, Jingshu; Huang, Xiaomin; Wang, Xintong; Bian, Xiling; Wang, KeWei] Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China in 2019, Cited 49. Formula: C7H8ClN. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8

A series of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones (3aa-3eq) were designed, synthesized, and evaluated as the type I positive allosteric modulators of human alpha 7 nAChR expressed in Xenopus ooctyes by a two-electrode voltage clamp. The structure-activity relationship analysis identified the compound 3ea as a potent and efficacious PAM with the maximum activation effect of the alpha 7 current of over 1633% in the presence of acetylcholine (100 mu M) and an EC50 = 1.26 mu M. It is highly specific to alpha 7 nAChR over other subtypes of nAChR, 5-HT3A, NMDA, and GABA(A) receptors. Compound 3ea showed an elimination half-life of 10.8 +/- 1.5 h for 3 mg/kg, i.v., and 7.4 +/- 1.1 h for 60 mg/kg, i.g. in rat. It also exhibited sufficient blood-brain barrier penetration with no significant effect on hERG channel. Most importantly, compound 3ea dose-dependently (0.1-1 mg/kg, i.p.) reversed the prepulse inhibition deficit induced by MK-801 in the mouse schizophrenia model. X

Formula: C7H8ClN. Welcome to talk about 87-63-8, If you have any questions, you can contact Li, YH; Sun, LL; Yang, TY; Jiao, WX; Tang, JS; Huang, XM; Huang, ZZ; Meng, Y; Luo, LC; Wang, XT; Bian, XL; Zhang, F; Wang, KW; Sun, Q or send Email.

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

In 2020 SYNTHESIS-STUTTGART published article about ARYLATION; PHOTOSWITCHES; DYNAMICS; DYES in [Jacob, Nicolas; Guillemard, Lucas; Wencel-Delord, Joanna] Univ Haute Alsace, Lab Innovat Mol & Applicat, ECPM, CNRS,UMR 7042,Univ Strasbourg, 25 Rue Becquerel, F-67087 Strasbourg, France in 2020, Cited 45. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8. Category: chlorides-buliding-blocks

Although 3-azoindoles have recently emerged as an appealing family of photoswitch molecules, the synthesis of such compounds has been poorly covered in the literature. Herein a high-yielding and operationally simple protocol is reported allowing the synthesis of 3-azoindoles, featuring important steric hindrance around the azo motif. Remarkably, this C-H coupling is characterized by excellent atom economy and occurs under metal-free conditions, at room temperature, and within few minutes, delivering the expected products in excellent yields (quantitatively in most of the cases). Accordingly, a library of new molecules, with potential applications as photochromic compounds, is prepared.

Category: chlorides-buliding-blocks. Bye, fridends, I hope you can learn more about C7H8ClN, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

HPLC of Formula: C7H8ClN. In 2019 J MED CHEM published article about VITRO PHARMACOLOGICAL CHARACTERIZATION; RELEASE; AGONIST; SCHIZOPHRENIA; DISCOVERY; TARGETS; SERIES; ACID in [Li, Yuanheng; Jiao, Wenxuan; Huang, Zongze; Meng, Ying; Luo, Laichun; Wang, KeWei; Sun, Qi] Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China; [Sun, Lilan; Zhang, Fang; Wang, KeWei] Qingdao Univ, Sch Pharm, Dept Pharmacol, Qingdao 266021, Peoples R China; [Yang, Taoyi; Tang, Jingshu; Huang, Xiaomin; Wang, Xintong; Bian, Xiling; Wang, KeWei] Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China in 2019, Cited 49. The Name is 2-Chloro-6-methylaniline. Through research, I have a further understanding and discovery of 87-63-8.

A series of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones (3aa-3eq) were designed, synthesized, and evaluated as the type I positive allosteric modulators of human alpha 7 nAChR expressed in Xenopus ooctyes by a two-electrode voltage clamp. The structure-activity relationship analysis identified the compound 3ea as a potent and efficacious PAM with the maximum activation effect of the alpha 7 current of over 1633% in the presence of acetylcholine (100 mu M) and an EC50 = 1.26 mu M. It is highly specific to alpha 7 nAChR over other subtypes of nAChR, 5-HT3A, NMDA, and GABA(A) receptors. Compound 3ea showed an elimination half-life of 10.8 +/- 1.5 h for 3 mg/kg, i.v., and 7.4 +/- 1.1 h for 60 mg/kg, i.g. in rat. It also exhibited sufficient blood-brain barrier penetration with no significant effect on hERG channel. Most importantly, compound 3ea dose-dependently (0.1-1 mg/kg, i.p.) reversed the prepulse inhibition deficit induced by MK-801 in the mouse schizophrenia model. X

Bye, fridends, I hope you can learn more about C7H8ClN, If you have any questions, you can browse other blog as well. See you lster.. HPLC of Formula: C7H8ClN

Reference:
Patent; ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.; WO2006/20879; (2006); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics