Tag: 200-300

On November 19, 1998, Liu, Shenquan; Tang, Cheng; Ho, Bin; Ankersen, Michael; Stidsen, Carsten E.; Crider, A. Michael published an article.Synthetic Route of 199522-66-2 The title of the article was Nonpeptide Somatostatin Agonists with sst4 Selectivity: Synthesis and Structure-Activity Relationships of Thioureas. And the article contained the following:

Utilizing NNC 26-9100 as a structural lead, a variety of nonpeptide derivatives of somatostatin were synthesized and evaluated for sst2 and sst4 receptor binding affinity. A novel thiourea scaffold was utilized to attach (1) a heteroaromatic nucleus to mimic the Trp8 residue, (2) a nonheteroarom. nucleus to mimic Phe7, and (3) a primary amine or other basic group to mimic the Lys9 residue of somatostatin. Displacement studies were carried out using membranes from cell lines expressing ssts [BHK cells (sst4) and HEK 293 cells (sst2)] utilizing [125I]Tyr11-SRIF as the radioligand. Several thioureas and an urea derivative exhibited Ki values of less than 100 nM. Two thioureas and the urea derivative are believed to be the most potent nonpeptide sst4 agonists known with Ki of 6, 16, and 14 nM, resp. Since the thiourea and the urea derivatives exhibit high sst4 selectivity, these novel nonpeptide derivatives may be useful tools for studying the sst4 receptor. Studies are currently in progress to evaluate the therapeutic potential of NNC 26-9100 in the treatment of glaucoma. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Synthetic Route of 199522-66-2

The Article related to thiourea preparation structure somatostatin agonist, nnc26910 derivative somatostatin sst4 receptor agonist, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Marugan, Juan Jose; Huang, Wenwei; Motabar, Omid; Zheng, Wei; Xiao, Jingbo; Patnaik, Samarjit; Southall, Noel; Westbroek, Wendy; Lea, Wendy A.; Simeonov, Anton; Goldin, Ehud; DeBernardi, Maria A.; Sidransky, Ellen published an article in 2012, the title of the article was Non-iminosugar glucocerebrosidase small molecule chaperones.Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine And the article contains the following content:

Small mol. chaperones are a promising therapeutic approach for the Lysosomal Storage Disorders (LSDs). Here, we report the discovery of a new series of non-iminosugar glucocerebrosidase inhibitors with chaperone capacity, and describe their structure-activity relationship (SAR), selectivity, cell activity and pharmacokinetics. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to glucocerebrosidase inhibitor chaperone pharmacokinetics brain ml156 msbar, Pharmacology: Structure-Activity and other aspects.Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 30, 2018, Robke, Lucas; Rodrigues, Tiago; Schroeder, Peter; Foley, Daniel J.; Bernardes, Goncalo J. L.; Laraia, Luca; Waldmann, Herbert published an article.Name: 3,5-Dibromo-4-methoxypyridine The title of the article was Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors. And the article contained the following:

Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small mol. modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to the discovery of a dimethoxypyridine-based class of autophagy inhibitors, which derive from previously reported, natural product-inspired MAP4K4 inhibitors. Comprehensive structure-activity relationship studies led to a potent compound, and biol. validation experiments indicated that the mode of action was upstream or independent of mTOR. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Name: 3,5-Dibromo-4-methoxypyridine

The Article related to dimethoxy pyridine derivative preparation autophagy inhibitor structure, Pharmacology: Structure-Activity and other aspects.Name: 3,5-Dibromo-4-methoxypyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 10, 2020, Smil, David; Wong, Jong Fu; Williams, Eleanor P.; Adamson, Roslin J.; Howarth, Alison; McLeod, David A.; Mamai, Ahmed; Kim, Soyoung; Wilson, Brian J.; Kiyota, Taira; Aman, Ahmed; Owen, Julie; Poda, Gennady; Horiuchi, Kurumi Y.; Kuznetsova, Ekaterina; Ma, Haiching; Hamblin, J. Nicole; Cramp, Sue; Roberts, Owen G.; Edwards, Aled M.; Uehling, David; Al-awar, Rima; Bullock, Alex N.; O’Meara, Jeff A.; Isaac, Methvin B. published an article.Recommanded Product: 3,5-Dibromo-4-methoxypyridine The title of the article was Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma. And the article contained the following:

There are currently no effective chemotherapeutic drugs approved for the treatment of diffuse intrinsic pontine glioma (DIPG), an aggressive pediatric cancer resident in the pons region of the brainstem. Radiation therapy is beneficial but not curative, with the condition being uniformly fatal. Anal. of the genomic landscape surrounding DIPG has revealed that activin receptor-like kinase-2 (ALK2) constitutes a potential target for therapeutic intervention given its dysregulation in the disease. An open science approach has been adopted to develop a series of potent, selective, orally bioavailable, and brain-penetrant ALK2 inhibitors based on the lead compound LDN-214117. Modest structural changes to the C-3, C-4, and C-5 position substituents of the core pyridine ring afforded compounds M4K2009, M4K2117, and M4K2163, each with a superior potency, selectivity, and/or blood-brain barrier (BBB) penetration profile. Robust in vivo pharmacokinetic (PK) properties and tolerability mark these inhibitors as advanced preclin. compounds suitable for further development and evaluation in orthotopic models of DIPG. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Recommanded Product: 3,5-Dibromo-4-methoxypyridine

The Article related to preparation alk2 inhibitor diffuse intrinsic pontine glioma, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 3,5-Dibromo-4-methoxypyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 31, 2004, Crider, A. M.; Liu, S.; Li, T.; Mahajan, S.; Ankersen, M.; Stidsen, C. E. published an article.Category: pyridine-derivatives The title of the article was Somatostatin receptor subtype 4 (sst4) ligands: Synthesis and evaluation of indol-3-yl- and 2-pyridyl-thioureas. And the article contained the following:

Thiourea analogs of NNC 26-9100 (2) were prepared as somatostatin receptor subtype 4 (sst4) ligands. The indole 9 exhibited high affinity (Ki = 23 nM) and about a 100-fold selectivity at sst4 compared to sst2 receptors. The (imidazol-4-yl) Pr group appears to play a major role in the affinity and selectivity of these thioureas at sst4. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Category: pyridine-derivatives

The Article related to somatostatin receptor sst4 thiourea ligand, Pharmacology: Structure-Activity and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 7, 1999, Kanno, Hisashi; Yoshida, Kazuo; Sato, Tsutomu; Sato, Kobi; Kanda, Yoichi published a patent.Category: pyridine-derivatives The title of the patent was Preparation of 6-phenoxypicolinic acid alkylidenehydrazide derivatives as herbicides. And the patent contained the following:

Claimed are 6-Phenoxypicolinic acid alkylidenehydrazide derivatives [I; R1 = halo, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C1-4 alkylthio, C1-4 alkylamino, C1-4 dialkylamino, (C1-4 alkyl)(C7-8aralkyl)amino; m = 0-3; R2, R3 = H, C1-10 C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, Ph, or aryl-C1-3 alkyl each optionally substituted with Xa or Xb; ; X1, Xb = halo, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkyl, C3-6 cycloalkyl, or cyano; na = nb = 0 or integer selected from number of H atoms substitutable with Xa and Xb in R2 and R3; or when R2 and R3 are an alkyl chain, R2 and R3 are directly linked together to form a ring optionally interposed with O, S, or optionally C1-4 alkyl-substituted NH; Y = C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C1-4 alkylthio, or halo; p = 0-5; when m, n, na, nb, and p are ≥2, R1, R2, Xa, Xb, and Y are same or different groups], a process for producing these, and a herbicide containing any of the derivatives as the active ingredient. These compounds exhibit excellent herbicidal activity with high selectivity at low dosage and does not inflict damage to the subsequent crops in double-cropping. Thus, 6-methoxy-6-[3-(trifluoromethyl)phenoxy]picolinic acid was stirred with chloroacetaldehyde in a mixture of 40% aqueous NaOH and EtOH at room temperature for ∼4 h to give 88% 6-methoxy-6-[3-(trifluoromethyl)phenoxy]picolinic acid (2-chloroethylidene)hydrazide (II). II 100 g/10 post emergence are controlled ≥50% Amaranthus retroflexus, Brassica kaber, Solanum nigrum, and Galium spurium. The experimental process involved the reaction of Methyl 6-bromo-5-methoxypicolinate(cas: 170235-18-4).Category: pyridine-derivatives

The Article related to phenoxypicolinic acid alkylidenehydrazide preparation herbicide, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 9, 1998, Kanno, Hisashi; Kanda, Yoichi; Sunagawa, Kazuhiko; Eizuka, Takayoshi published a patent.SDS of cas: 170235-18-4 The title of the patent was Preparation of phenoxypicolinic acid derivatives as agrochemical fungicides. And the patent contained the following:

The title compounds [I; R = halo, C1-4 alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, or alkylamino, etc.; n1 = 1-3; Y = C1-4 alkyl, haloalkyl, alkoxy, or haloalkoxy, etc.; m = 0-5] are prepared I are useful as active ingredients contained in agricultural or horticultural fungicides. Thus, 2-bromo-4-methoxy-6-[3-(trifluoromethyl)phenoxy]pyridine (preparation given) was treated with n-BuLi, reacted with CO2, and treated with 1N HCl to give 30% I (Rn1 = 4-OMe, Ym = 3-CF3), which at 1 kg/ha showed > 70% fungicidal effect for Botrytis cinerea. The experimental process involved the reaction of Methyl 6-bromo-5-methoxypicolinate(cas: 170235-18-4).SDS of cas: 170235-18-4

The Article related to phenoxypicolinic acid preparation agrochem fungicide, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.SDS of cas: 170235-18-4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 23, 2017, Watanabe, Atsushi; Sato, Yuuki; Ogura, Keiji; Tatsumi, Yoshiyuki published a patent.Synthetic Route of 25813-24-5 The title of the patent was Preparation of biaryl derivatives as antifungal agents and medicine containing them. And the patent contained the following:

Biaryl derivatives represented by general formula I (ring A, X1, X2, X3, Y, Z, R2a, R3, and Q are defined below) or salts thereof having excellent antifungal activity against Trichophyton, which is a major causative organism of superficial mycoses. Ring A, X1, X2, X3, Y, Z, Q, and R3 are defined as [ring A = each (un)substituted Ph or 5- or 6-membered heteroaryl each optionally fused to form (un)substituted condensed ring; Q = CH2, CF2, S(O), SO2, C(O), NH, or S; X1, X2, X3 = CR1 or N; Y = CH or N; Z = CR2b or N; R1 = H, halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, or C1-6 haloalkoxy; R3 = H, halo, or each (un)substituted C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, or aralkyl]. R2a and R2b are defined as [R2a, R2b = H, halo, HO, cyano, formyl, pentafluorosulfanyl, Q1, or each (un)substituted C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-4 alkoxy-C1-4 alkyl, C1-4 alkoxy-C1-4 haloalkyl, C1-6 alkyl carbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C3-7 cycloalkyl, heterocycloalkyl, heterocycloalkyloxy, C2-6 alkenyl, C2-6 alkenyloxy, C2-6 alkenyl-C1-6 alkyl, C2-6 alkenyl-C1-6 alkoxy, C2-6 alkenyloxy-C1-4 alkoxy, C2-6 alkenyloxy-C1-4 haloalkyl, C2-6 alkenyloxy-C1-4 haloalkoxy, C2-6 alkynyl, C2-6 alkynyloxy, C2-6 alkynyl-C1-6 alkyl, C2-6 alkynyl-C1-6 alkoxy, C2-6 alkynyloxy-C1-4 alkyl, C2-6 alkynyloxy-C1-4 alkoxy, C2-6 alkynyloxy-C1-4 haloalkyl, C2-6 alkynyloxy-C1-4 haloalkoxy, NH2, C1-6 alkylthio, C1-6 haloalkylthio; ring B = each (un)substituted carbocyclic or heterocyclic ring; L = a single bond, (CH2)p, O(CH2)p, (CH2)pO, (CH2)pO(CH2)q, NRc(CH2)p , (CH2)pNRc, or (CH2)pNRc(CH2)q; p, q = 1, 2, or 3; one or a plural number of H atoms of each (CH2)p or (CH2)q is optionally substituted with halo, C1-4 alkyl, or C3-7 cycloalkyl; Rc = H or C1-6 alkyl; when Z = CR2b, R2a and R2b together with the carbon atoms to which they are bonded form each (un)substituted carbocyclic or heterocyclic ring]. The biaryl derivatives I include arylpyridine or heterocyclylpyridine derivatives, e.g. 3-phenyl-2-[(pyridin-3-yl)oxy]pyridine, 2-[(pyridin-3-yl)oxy]-3,3′-bipyridine, 5-[2-[(pyridin-3-yl)oxy]pyridin-3-yl]isoquinoline, 8-[2-[(pyridin-3-yl)oxy]pyridin-3-yl]quinoline, 3-(2,3-dihydrobenzofuran-7-yl)-2-[(pyridin-3-yl)oxy]pyridine, 5-[2-[(pyridin-3-yl)oxy]pyridin-3-yl]quinoxaline, and 3-(chroman-8-yl)-2-[(pyridin-3-yl)oxy]pyridine derivatives Thus, etherification of 3-bromo-2-chloropyridine with 6-(trifluoromethyl)pyridin-3-ol in the presence of Cs2CO3 in DMSO with stirring at 120° for 18 h gave 76% 3-[(3-bromopyridin-2-yl)oxy]-6-(trifluoromethyl)pyridine (II). Coupling of II with 2-methoxyphenylboronic acid in the presence of bis[di-tert-butyl(4-dimethylaminophenyl)phosphine]palladium(II) and Cs2CO3 in aqueous dioxane solution with stirring at 120° for 30 min under microwave irradiation gave 76% 3-(2-methoxyphenyl)-2-[[6-(trifluoromethyl)pyridin-3-yl]oxy]pyridine (III). III showed min. inhibitory concentration of ≤0.1 μg/mL against Trichophyton mentagrophytes and T. rubrum. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Synthetic Route of 25813-24-5

The Article related to bipyridine phenylpyridine pyridylquinoline pyrimidinylpyridine heterocyclylpyridine preparation antifungal, biaryl preparation antifungal agent, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Synthetic Route of 25813-24-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 20, 2018, Watanabe, Atsushi; Sato, Yuki; Ogura, Keiji; Tatsumi, Yoshiyuki published a patent.Recommanded Product: 3,5-Dibromo-4-methoxypyridine The title of the patent was Preparation of biaryl derivatives as antifungal agents and medicine containing them. And the patent contained the following:

Biaryl derivatives represented by general formula I (ring A, X1, X2, X3, Y, Z, R2a, R3, and Q are defined below) or salts thereof having excellent antifungal activity against Trichophyton which is a major causative organism of superficial mycoses are prepared Ring A, X1, X2, X3, Y, Z, Q, and R3 are defined as [ring A = each (un)substituted Ph or 5- or 6-membered heteroaryl each optionally fused to form (un)substituted condensed ring; Q = CH2, CF2, S(O), SO2, C(O), NH, or S; X1, X2, X3 = CR1 or N; Y = CH or N; Z = CR2b or N; R1 = H, halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, or C1-6 haloalkoxy; R3 = H, halo, or each (un)substituted C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, or aralkyl]. R2a and R2b are defined as [R2a, R2b = H, halo, HO, cyano, formyl, pentafluorosulfanyl, Q1, or each (un)substituted C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-4 alkoxy-C1-4 alkyl, C1-4 alkoxy-C1-4 haloalkyl, C1-6 alkyl carbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C3-7 cycloalkyl, heterocycloalkyl, heterocycloalkyloxy, C2-6 alkenyl, C2-6 alkenyloxy, C2-6 alkenyl-C1-6 alkyl, C2-6 alkenyl-C1-6 alkoxy, C2-6 alkenyloxy-C1-4 alkoxy, C2-6 alkenyloxy-C1-4 haloalkyl, C2-6 alkenyloxy-C1-4 haloalkoxy, C2-6 alkynyl, C2-6 alkynyloxy, C2-6 alkynyl-C1-6 alkyl, C2-6 alkynyl-C1-6 alkoxy, C2-6 alkynyloxy-C1-4 alkyl, C2-6 alkynyloxy-C1-4 alkoxy, C2-6 alkynyloxy-C1-4 haloalkyl, C2-6 alkynyloxy-C1-4 haloalkoxy, NH2, C1-6 alkylthio, C1-6 haloalkylthio; ring B = each (un)substituted carbocyclic or heterocyclic ring; L = a single bond, (CH2)p, O(CH2)p, (CH2)pO, (CH2)pO(CH2)q, NRc(CH2)p , (CH2)pNRc, or (CH2)pNRc(CH2)q; p, q = 1, 2, or 3; one or a plural number of H atoms of each (CH2)p or (CH2)q is optionally substituted with halo, C1-4 alkyl, or C3-7 cycloalkyl; Rc = H or C1-6 alkyl; when Z = CR2b, R2a and R2b together with the carbon atoms to which they are bonded form each (un)substituted carbocyclic or heterocyclic ring]. The biaryl derivatives I include arylpyridine or heterocyclylpyridine derivatives, e.g. 3-phenyl-2-[(pyridin-3-yl)oxy]pyridine, 2-[(pyridin-3-yl)oxy]-3,3′-bipyridine, 5-[2-[(pyridin-3-yl)oxy]pyridin-3-yl]isoquinoline, 8-[2-[(pyridin-3-yl)oxy]pyridin-3-yl]quinoline, 3-(2,3-dihydrobenzofuran-7-yl)-2-[(pyridin-3-yl)oxy]pyridine, 5-[2-[(pyridin-3-yl)oxy]pyridin-3-yl]quinoxaline, and 3-(chroman-8-yl)-2-[(pyridin-3-yl)oxy]pyridine derivatives Thus, etherification of 3-bromo-2-chloropyridine with 6-(trifluoromethyl)pyridin-3-ol in the presence of Cs2CO3 in DMSO with stirring at 120° for 18 h gave 76% 3-[(3-bromopyridin-2-yl)oxy]-6-(trifluoromethyl)pyridine (II). Coupling of II with 2-methoxyphenylboronic acid in the presence of bis[di-tert-butyl(4-dimethylaminophenyl)phosphine]palladium(II) and Cs2CO3 in aqueous dioxane solution with stirring at 120° for 30 min under microwave irradiation gave 76% 3-(2-methoxyphenyl)-2-[[6-(trifluoromethyl)pyridin-3-yl]oxy]pyridine (III). III showed min. inhibitory concentration of ≤0.1 μg/mL against Trichophyton mentagrophytes and T. rubrum. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Recommanded Product: 3,5-Dibromo-4-methoxypyridine

The Article related to bipyridine phenylpyridine pyridylquinoline pyrimidinylpyridine heterocyclylpyridine preparation antifungal, biaryl preparation antifungal agent, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 3,5-Dibromo-4-methoxypyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yi, Xiao; Chen, Jing; Xu, Xiuling; Ma, Yongmin published an article in 2017, the title of the article was Solvent and substituent effects on the conversion of 4-methoxypyridines to N-methyl-4-pyridones.Formula: C6H5Br2NO And the article contains the following content:

In the reaction of 4-methoxypyridine derivatives with alkyl iodides in the presence or absence of solvent, not only the pyridinium ions but also the related 1-methylpyridones are produced. The presence of solvent favors the formation of the 1-methylpyridone. Electron withdrawing groups on the pyridine ring also favor this conversion. A possible mechanism is presented. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Formula: C6H5Br2NO

The Article related to solvent substituent effect methoxypyridine derivative alkyl iodide pyridone, Physical Organic Chemistry: Addition, Elimination, and Substitution Reactions and other aspects.Formula: C6H5Br2NO

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem