Category: 76283-09-5

Karlstroem, Sofia published the artcileSubstituted 7-Amino-5-thio-thiazolo[4,5-d]pyrimidines as Potent and Selective Antagonists of the Fractalkine Receptor (CX₃CR1), HPLC of Formula: 76283-09-5, the publication is Journal of Medicinal Chemistry (2013), 56(8), 3177-3190, database is CAplus and MEDLINE.

The authors have developed two parallel series, A and B, of CX₃CR1 antagonists for the treatment of multiple sclerosis. By modifying the substituents on the 7-amino-5-thio-thiazolo[4,5-d]pyrimidine core structure, they were able to achieve compounds with high selectivity for CX₃CR1 over the closely related CXCR2 receptor. The structure-activity relationships showed that a leucinol moiety attached to the core-structure in the 7-position together with α-Me branched benzyl derivatives in the 5-position displayed promising affinity, and selectivity as well as physicochem. properties, as exemplified by compounds I and II. They show the preparation of the first potent and selective orally available CX₃CR1 antagonists.

Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, HPLC of Formula: 76283-09-5.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Rakowitz, Dietmar published the artcileOn the synthesis of bioisosteres of O-benzothiazolyl-oxybenzoic acids and evaluation as aldose reductase inhibitors, Formula: C7H5Br2F, the publication is Archiv der Pharmazie (Weinheim, Germany) (2005), 338(9), 419-426, database is CAplus and MEDLINE.

A series of compounds characterized by bioisosteric replacement of pharmacophores were prepd, e.g., I (R = CH(=NOH) or NO₂) and tested as aldose reductase inhibitors (ARIs). On the one hand, the acidic function was formally replaced by an oxime or a nitro group and on the other hand the lipophilic substituent was modified. The results of the biol. evaluation of these derivatives permitted to gain insight into structural features critical for the aldose reductase inhibition.

Archiv der Pharmazie (Weinheim, Germany) published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Poslusney, Michael S. published the artcileSpirocyclic replacements for the isatin in the highly selective, muscarinic M₁ PAM ML137: The continued optimization of an MLPCN probe molecule, Category: bromides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(6), 1860-1864, database is CAplus and MEDLINE.

This Letter describes the further optimization of an MLPCN probe mol. (ML137) through the introduction of 5- and 6-membered spirocycles in place of the isatin ketone. Interestingly divergent structure-activity relationships, when compared to earlier M₁ PAMs, are presented. These novel spirocycles, e.g. I, possess improved efficacy relative to ML137, while also maintaining high selectivity for the human and rat muscarinic M₁ receptor subtype.

Bioorganic & Medicinal Chemistry Letters published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Category: bromides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Camp, David published the artcileDevelopment of a Synthetic Process towards a Hepatitis C Polymerase Inhibitor, SDS of cas: 76283-09-5, the publication is Organic Process Research & Development (2006), 10(4), 814-821, database is CAplus.

The synthesis of clin. candidate 2-(4-{2-[(2R)-2-Cyclopentyl-5-(5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-ylmethyl)-4-hydroxy-6-oxo-3,6-dihydro-2H-pyran-2-yl]-ethyl}-2-fluoro-phenyl)-2-methyl-propionitrile (I) on multikilogram scale is described. Initial synthesis of I, clin. candidate for inhibition of the hepatitis C viral polymerase (HCVP) protein, was executed via a racemic synthetic route coupled with chiral HPLC separation Due to the achiral route and instability of key intermediates, the initial route was determined to be unsuitable for large-scale manufacture An alternate route was developed utilizing a convergent Heck coupling, resolution of a carboxylic acid via diastereomeric salt formation, and an efficient chem. recycling of the undesired enantiomer.

Organic Process Research & Development published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, SDS of cas: 76283-09-5.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Li, Yuan-Xiang published the artcileDesign and syntheses of novel phthalazin-1(2H)-one derivatives as acetohydroxyacid synthase inhibitors, Formula: C7H5Br2F, the publication is Journal of Agricultural and Food Chemistry (2006), 54(24), 9135-9139, database is CAplus and MEDLINE.

A series of 2-substituted-8-(4,6-dimethoxypyrimidin-2-yloxy)-4-methylphthalazin-1-one derivatives were designed via ortho-substituent cyclization to discover a new herbicidal lead structure. These compounds were synthesized by a seven-step route using 3-hydroxy-acetophenone as a starting material. Determination of the K_i values against wild-type A. thaliana acetohydroxyacid synthase (AHAS) (EC 4.1.3.18) indicated that some of the compounds displayed good enzyme inhibition activity comparable to that of KIH-6127. Bioassay data on weeds showed that the synthesized compounds exhibited the typical injury symptoms of AHAS-inhibiting herbicides, and some of them showed broad-spectrum and high herbicidal activities in postemergence treatments against Echinochloa crusgalli, Digitaria sanguinalis, Setaria viridis, Brassica juncea, Amaranthus retroflexus, and Chenopodium album, at an application rate of 150 g/ha. To our knowledge, this is the first report of methylphthalazin-1-one derivatives as AHAS inhibitors.

Journal of Agricultural and Food Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Li, Yuan-Xiang published the artcileDesign and syntheses of novel phthalazin-1(2H)-one derivatives as acetohydroxyacid synthase inhibitors, Formula: C7H5Br2F, the publication is Journal of Agricultural and Food Chemistry (2006), 54(24), 9135-9139, database is CAplus and MEDLINE.

A series of 2-substituted-8-(4,6-dimethoxypyrimidin-2-yloxy)-4-methylphthalazin-1-one derivatives were designed via ortho-substituent cyclization to discover a new herbicidal lead structure. These compounds were synthesized by a seven-step route using 3-hydroxy-acetophenone as a starting material. Determination of the K_i values against wild-type A. thaliana acetohydroxyacid synthase (AHAS) (EC 4.1.3.18) indicated that some of the compounds displayed good enzyme inhibition activity comparable to that of KIH-6127. Bioassay data on weeds showed that the synthesized compounds exhibited the typical injury symptoms of AHAS-inhibiting herbicides, and some of them showed broad-spectrum and high herbicidal activities in postemergence treatments against Echinochloa crusgalli, Digitaria sanguinalis, Setaria viridis, Brassica juncea, Amaranthus retroflexus, and Chenopodium album, at an application rate of 150 g/ha. To our knowledge, this is the first report of methylphthalazin-1-one derivatives as AHAS inhibitors.

Journal of Agricultural and Food Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Ndikuryayo, Ferdinand published the artcileHydrophobicity-oriented drug design (HODD) of new human 4-hydroxyphenylpyruvate dioxygenase inhibitors, Quality Control of 76283-09-5, the publication is European Journal of Medicinal Chemistry (2019), 22-31, database is CAplus and MEDLINE.

Involved in the tyrosine degradation pathway, 4-hydroxyphenylpyruvate dioxygenase (HPPD) is an important target for treating type I tyrosinemia. To discover novel HPPD inhibitors, we proposed a hydrophobicity-oriented drug design (HODD) strategy based on the interactions between HPPD and the com. drug NTBC. Most of the new compounds showed improved activity, compound d23 being the most active candidate (IC₅₀ = 0.047 μM) with about 2-fold more potent than NTBC (IC₅₀ = 0.085 μM). Therefore, compound d23 is a potential drug candidate to treat type I tyrosinemia.

European Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Quality Control of 76283-09-5.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Seo, Jin-soo published the artcileNovel inhibitors of prolyl 4-hydroxylase; solid-phase synthesis of 2,2-dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyran derivatives, COA of Formula: C7H5Br2F, the publication is Bulletin of the Korean Chemical Society (2006), 27(6), 909-917, database is CAplus.

2,2-Dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyrans were identified as prolyl 4-hydroxylase inhibitors via a screening process using HSC-T6 and LI 90 cells that express an immortalized rat hepatic stellate cell line and as part of a test of the type I collagen contents employing the ELISA method. A subsequent lead optimization effort based on solid-phase parallel synthesis led to the identification of 2,2-dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyrans as potent inhibitors of prolyl 4-hydroxylase.

Bulletin of the Korean Chemical Society published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C9H8BrF3, COA of Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Mistry, Shailesh N. published the artcile4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M₁ Muscarinic Acetylcholine Receptor, Computed Properties of 76283-09-5, the publication is Journal of Medicinal Chemistry (2016), 59(1), 388-409, database is CAplus and MEDLINE.

Pos. allosteric modulators (PAMs) of the M₁ muscarinic acetylcholine receptor (M₁ mAChR) are a promising strategy for the treatment of the cognitive deficits associated with diseases including Alzheimer’s and schizophrenia. Herein, we report the design, synthesis, and characterization of a novel family of M₁ mAChR PAMs. The most active compounds of the 4-phenylpyridin-2-one series exhibited comparable binding affinity to the reference compound, 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (BQCA), but markedly improved pos. cooperativity with acetylcholine, and retained exquisite selectivity for the M₁ mAChR. Furthermore, the pharmacol. characterization revealed ligands with a diverse range of activities, including modulators that displayed both high intrinsic efficacy and PAM activity, those that showed no detectable agonism but robust PAM activity and ligands that displayed robust allosteric agonism but little modulatory activity. Compound I was found to have the best pharmacol. profile. Thus, the 4-phenylpyridin-2-one scaffold offers an attractive starting point for further lead optimization.

Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Computed Properties of 76283-09-5.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Seo, Jin-soo published the artcileNovel inhibitors of prolyl 4-hydroxylase; solid-phase synthesis of 2,2-dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyran derivatives, COA of Formula: C7H5Br2F, the publication is Bulletin of the Korean Chemical Society (2006), 27(6), 909-917, database is CAplus.

2,2-Dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyrans were identified as prolyl 4-hydroxylase inhibitors via a screening process using HSC-T6 and LI 90 cells that express an immortalized rat hepatic stellate cell line and as part of a test of the type I collagen contents employing the ELISA method. A subsequent lead optimization effort based on solid-phase parallel synthesis led to the identification of 2,2-dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyrans as potent inhibitors of prolyl 4-hydroxylase.

Bulletin of the Korean Chemical Society published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C9H8BrF3, COA of Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary