Tag: M.W=150-200

Ding, Huaiwei published the artcileSynthesis and cytotoxic activity of some novel N-pyridinyl-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide derivatives, HPLC of Formula: 55403-35-5, the publication is Molecules (2012), 4703-4716, database is CAplus and MEDLINE.

Novel compounds bearing imidazo[2,1-b]thiazole scaffolds were designed and synthesized based on the optimization of the virtual screening hit compound N-(6-morpholinopyridin-3-yl)-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide (I) and were tested for their cytotoxicity against human cancer cell lines, including HepG2 and MDA-MB-231. 2-{6-(4-Chlorophenyl)imidazo[2,1-b]thiazol-3-yl}-N-{6-[4-(4-methoxybenzyl)piperazin-1-yl]pyridin-3-yl}acetamide, with slightly higher inhibition on VEGFR2 than I (5.72 and 3.76% inhibitory rate at 20 μM, resp.), was a potential inhibitor against MDA-MB-231 (IC₅₀ = 1.4 μM) compared with sorafenib (IC₅₀ = 5.2 μM), and showed more selectivity against MDA-MB-231 than HepG2 cell line (IC₅₀ = 22.6 μM).

Molecules published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C10H16N4, HPLC of Formula: 55403-35-5.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Blass, Benjamin E. published the artcileDesign, synthesis, and evaluation of functionalized 5-(4-arylpiperazin-1-yl)-N-arylpentanamides as selective dopamine D₃ receptor ligands, Quality Control of 178928-58-0, the publication is Medicinal Chemistry Research (2022), 31(1), 132-145, database is CAplus.

Substance use disorder remains a major, unmet medical need. Cocaine is one of the most commonly abused recreational drugs and in 2018, there were over 5.5 million cocaine users. There are no approved therapies for the treatment of cocaine use disorder, but the D₃ dopamine receptor has been identified as a potential therapeutic target. Our initial lead compound (6) is a potent D₃ ligand with a high level of selectivity for D₃ over D2, but its solubility is low. We have identified a new series of functionalized 5-(4-arylpiperazin-1-yl)-N-arylpentanamides (7) that are potent D₃ binders that have moderate to high selectivity for D₃ over D₂. Exemplary members of this series were also significantly more soluble than our initial lead compound (6).

Medicinal Chemistry Research published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Quality Control of 178928-58-0.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Bryan, Marian C. published the artcilePyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR, Application of 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, the publication is ACS Medicinal Chemistry Letters (2016), 7(1), 100-104, database is CAplus and MEDLINE.

The rapid advancement of a series of noncovalent inhibitors of T790M mutants of EGFR is discussed. The optimization of a nonselective high-throughput screening pyridone hit to potent mols. with high levels of selectivity over wtEGFR and the broader kinome is described herein.

ACS Medicinal Chemistry Letters published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C10H16N4, Application of 6-(4-Methylpiperazin-1-yl)pyridin-3-amine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Belfield, Andrew J. published the artcileSynthesis of Meta-substituted aniline derivatives by nucleophilic substitution, Synthetic Route of 178928-58-0, the publication is Tetrahedron (1999), 55(46), 13285-13300, database is CAplus.

Substitution by amines of fluorobenzenes containing a meta-substituted electron withdrawing group (EWG), in DMSO at 100°C over 60 h gave meta-substituted aniline derivatives in isolated yields of up to 98%. The scope of the reaction is explored in terms of reaction conditions and substrates. It is postulated that facile meta-substitutions are facilitated through field stabilization of the intermediate anion by EWG substituents.

Tetrahedron published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Synthetic Route of 178928-58-0.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Leopoldo, Marcello published the artcileStructure-Affinity Relationship Study on N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-Aryl-1-Piperazinealkylamides, a New Class of 5-Hydroxytryptamine₇ Receptor Agents, Application of 1-(3-Cyanophenyl)piperazine, the publication is Journal of Medicinal Chemistry (2004), 47(26), 6616-6624, database is CAplus and MEDLINE.

A series of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides I (n = 3-5, R¹ = OMe, H, R² = OMe, CN, Ac, SMe, OH, etc.) was prepared and their affinity for serotonin (5-hydroxytryptamine, 5-HT) 5-HT₇, 5-HT_1A, and 5-HT_2A receptors was measured by in vitro binding assays. In relation to 5-HT₇ receptor affinity, receptor binding studies indicated that (i) the optimal alkyl chain length was five methylenes, (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus was preferred, and (iii) the substitution pattern of the aryl ring linked to the piperazine ring played a crucial role. Several compound with high affinity for 5-HT₇ receptors were identified. Among them, piperazinehexanamides I [n = 5, R¹ = H, R² = 2-OMe (II), 2-Ac (III), 2-SMe (IV), 2-OH (V), and 2-Me (VI)] were assayed for the 5-HT₇ receptor-mediated relaxation of substance P-induced guinea pig ileum contraction. Compounds II, IV, and VI behaved as full agonists and compound III as a partial agonist, whereas derivative V acted as an antagonist. Among the compounds presented here, it emerged that IV was identified as a potent 5-HT₇ receptor agonist (K_i = 0.22 nM, EC₅₀ = 2.56 μM), endowed with selectivity over 5-HT_1A and 5-HT_2A receptors (200-fold and >1000-fold, resp.).

Journal of Medicinal Chemistry published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C11H13N3, Application of 1-(3-Cyanophenyl)piperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Sasmal, Sanjita published the artcileDesign and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists, SDS of cas: 71260-16-7, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(9), 3157-3162, database is CAplus and MEDLINE.

Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays a role in metabolic and CNS disorders. The modeling-supported design, synthesis and multi-parameter optimization (biol. activity, solubility, metabolic stability, hERG) of novel quinazoline derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified. Clusters of refined hMCHR1 homol. models derived from the X-ray structure of the β2-adrenergic receptor, including extracellular loops, were developed and used to guide the design.

Bioorganic & Medicinal Chemistry Letters published new progress about 71260-16-7. 71260-16-7 belongs to piperazines, auxiliary class Piperazine, name is 2-Methyl-1-(piperazin-1-yl)propan-1-one, and the molecular formula is C8H16N2O, SDS of cas: 71260-16-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Zhang, Dengyou published the artcileNovel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors, Safety of 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(8), 2408-2413, database is CAplus and MEDLINE.

A series of novel 5-(benzyloxy)pyridin-2(1H)-ones were designed, synthesized and biol. evaluated for c-Met inhibition. Various amides and benzimidazoles at the C-3 position were investigated. A potent compound I with a c-Met IC₅₀ of 12 nM was identified. This compound exhibited potent inhibition of EBC-1 cell associated with c-Met constitutive activation and showed high selectivity for c-Met than other tested 11 kinases. The binding model I with c-Met was disclosed by docking anal.

Bioorganic & Medicinal Chemistry Letters published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C13H19Br2ClN2O, Safety of 6-(4-Methylpiperazin-1-yl)pyridin-3-amine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

McCoull, William published the artcileIdentification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes, Product Details of C10H16N4, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(12), 3873-3878, database is CAplus and MEDLINE.

A novel series of DGAT-1 inhibitors was discovered from an oxadiazole amide high throughput screening (HTS) hit. Optimization of potency and ligand lipophilicity efficiency (LLE) resulted in a carboxylic acid containing clin. candidate 53 (AZD3988, I), which demonstrated excellent DGAT-1 potency (0.6 nM), good pharmacokinetics and pre-clin. in vivo efficacy that could be rationalised through a PK/PD relationship.

Bioorganic & Medicinal Chemistry Letters published new progress about 55403-35-5. 55403-35-5 belongs to piperazines, auxiliary class Pyridine,Piperazine,Amine, name is 6-(4-Methylpiperazin-1-yl)pyridin-3-amine, and the molecular formula is C10H16N4, Product Details of C10H16N4.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics