Tag: M.W=250-300

Khwaja, Sadiya; Fatima, Kaneez; Mishra, Divya; Babu, Vineet; Kumar, Yogesh; Malik, Sumera Banu; Tabassum, Misbah; Luqman, Suaib; Bawankule, Dnyaneshwar U.; Chanda, Debabrata; Khan, Feroz; Mondhe, Dilip M.; Negi, Arvind S. published the artcile< An improved synthesis of indanocine and antiproliferative activity of 2-benzylindanocine via microtubule destabilization>, Quality Control of 197638-83-8, the main research area is colon lung pancreatic cancer indanocine antiproliferative 2benzylindanocine microtubule destabilization; Ehrlich ascites carcinoma; acute oral toxicity; anticancer; antitubulin; indanocine.

Indanocine, a potent anticancer investigational drug of National Cancer Institute-USA, has been much discussed in recent years. Present communication aimed at total synthesis of indanocine and its close analogs. Total synthesis was improved by double yields than previously reported yields. Some of the benzylidene and 2-benzyl derivatives with free rotation at C2 position exhibited potential cytotoxicities against various human cancer cell lines. Five such analogs exhibited potential antiproliferative effect against HCT-116 and MIA PACA-2 cell lines. Benzylindanocine 12i induced microtubule destabilization by occupying colchicine binding pocket of β-tubulin. It also exhibited anti-inflammatory activity by down-regulating IL-6 and TNF-α. In Ehrlich ascites carcinoma model, 12i reduced 78.4% of EAC tumor in Swiss albino mice at 90 mg/kg (i.p.) dose. Further, in in vivo safety studies, 12i was found to be safe to rodents up to 1,000 mg/kg dose. Concomitant anticancer and anti-inflammatory activity of benzylindanocine is distinctive, which suggests its further optimization for better efficacy and druggability.

Chemical Biology & Drug Design published new progress about Antiproliferative agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Quality Control of 197638-83-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Rindhe, S. S.; Karale, B. K.; Gupta, R. C.; Rode, M. A. published the artcile< Synthesis, antimicrobial and antioxidant activity of some oxindoles>, Name: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is oxindole preparation antibacterial antifungal antioxidant agent; Antibacterial; antifungal and antioxidant activity; oxindole.

The present work describes the synthesis and spectral anal. of several (3Z)-[4-[4-(arylsulfonyl)-1-piperazinyl]benzylidene]-1,3-dihydro-2H-indol-2-one derivatives The title compounds were screened in-vitro against six species of microorganisms, Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger and Aspergillus clavatus. Most of the compounds exhibited significant antimicrobial activity. All compounds were also screened in-vitro for the antioxidant activity using DPPH assay. Most of them have shown very significant antioxidant activity. The synthesis of the target compounds was achieved by an amidation (sulfonamidation) of 4-[4-[(2-oxo-3-indolylidene)methylene]phenyl]-1-piperazinecarboxylic acid 1,1-dimethylethyl ester with sulfonyl halides. The title compounds thus formed included 1,3-dihydro-3-[(3Z)-[4-[4-[[4-(1-methylethyl)phenyl]sulfonyl]-1-piperazinyl]phenyl]methylene]-2H-indol-2-one (I).

Indian Journal of Pharmaceutical Sciences published new progress about Antibacterial agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Name: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Robke, Lucas; Rodrigues, Tiago; Schroeder, Peter; Foley, Daniel J.; Bernardes, Goncalo J. L.; Laraia, Luca; Waldmann, Herbert published the artcile< Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors>, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is dimethoxy pyridine derivative preparation autophagy inhibitor structure.

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.

Tetrahedron published new progress about Apoptosis. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Knippel, James Levi; Ye, Yuxuan; Buchwald, Stephen L. published the artcile< Enantioselective C2-Allylation of Benzimidazoles Using 1,3-Diene Pronucleophiles>, Product Details of C16H22N2O3, the main research area is benzimidazole aryl alkadiene copper catalyst enantioselective regioselective allylation; aryl alkenylbenzimidazole preparation.

Previously, several enantioselective allylation reactions of benzimidazoles were reported that functionalize the nucleophilic nitrogen atom. To the reversal of this inherent selectivity, N-allylation by using electrophilic N-OPiv benzimidazoles with readily available 1,3-dienes as nucleophile precursors were described. CuH-catalyzed approach utilized mild reaction conditions, exhibited broad functional-group compatibility and exclusively formed the C2-allylated product with excellent stereoselectivity.

Organic Letters published new progress about 1,3-Alkadienes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Product Details of C16H22N2O3.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Nishiguchi, Gisele A.; Atallah, Gordana; Bellamacina, Cornelia; Burger, Matthew T.; Ding, Yu; Feucht, Paul H.; Garcia, Pablo D.; Han, Woo-Seok; Klivansky, Liana; Lindvall, Mika published the artcile< Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases>, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is indole pyrazolopyridine derivative preparation SAR Pim kinase inhibitory.

A series of novel 3,5-disubstituted indole e. g., I and pyrazolopyridine e. g., II derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High throughput screen identified a pan-Pim kinase inhibitor with a promiscuous scaffold. Guided by structure-based drug design, SAR of the series afforded a highly selective indole chemotype that was further developed into a potent set of compounds against Pim-1, 2, and 3 (Pim-1 and Pim-3: IC50 ≤ 2 nM and Pim-2: IC50 ≤ 100 nM).

Bioorganic & Medicinal Chemistry Letters published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Treuer, Adriana V.; De-La-Torre, Pedro; Gutierrez, Margarita I. published the artcile< Synthesis of new (E)-2-(1H-indole-3-ylcarbonyl)-3-heteroaryl-acrylonitriles via microwave-assisted Knoevenagel condensation>, Electric Literature of 197638-83-8, the main research area is indolylcarbonyl heteroaryl acrylonitrile preparation stereoselective green chem; heteroaryl aldehyde stereoselective Knoevenagel condensation cyanoacetyl indole microwave irradiation.

A series of new (E)-2-(1H-indole-3-ylcarbonyl)-3-heteroaryl-acrylonitriles I [R = 2-imidazolyl, 5-phenyl-3-isoxazolyl, 5-(4-chlorophenyl)-2-furyl, etc.] was obtained in 30-94% yields from 3-(cyanoacetyl)indole and the corresponding heteroaryl aldehydes RCHO by microwave-assisted (300 W) Knoevenagel reaction at 100 °C.

Journal of Chemistry published new progress about Aryl aldehydes, heteroaryl Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Electric Literature of 197638-83-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Watanabe, Toshihiro; Kakefuda, Akio; Kinoyama, Isao; Takizawa, Kenji; Hirano, Seiko; Shibata, Hiroshi; Yanagisawa, Isao published the artcile< Synthesis of novel succinamide derivatives having a 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton as potent and selective M2 muscarinic receptor antagonists. II>, Computed Properties of 197638-83-8, the main research area is pyridobenzodiazepinone preparation muscarinic receptor antagonist; succinamide pyridobenzodiazepinone preparation muscarinic receptor antagonist; structure activity pyridobenzodiazepinone muscarinic receptor antagonist; antibradycardiac pyridobenzodiazepinone piperazinylbenzylmethylamino preparation; cardiotonic pyridobenzodiazepinone piperazinylbenzylmethylamino preparation.

Title compounds I (R = H, OMe, Cl, Me, Et, i-Pr, MeS, HO, n-PrO, Me2N, pyrrolidino, morpholino, 4-alkyl-1-piperazinyl; R1 = Me, Et)(26 compounds) were prepared and evaluated for binding affinity to muscarinic receptors in vitro and for antagonism of bradycardia and salivation in vivo in comparison with AF-DX 116 (II). Structure-activity relationships studies in vitro indicated that the 4-(4-alkyl-1-piperazinyl)benzylamino moiety plays a crucial role in enhancing the affinity for M2 muscarinic receptors. I containing a 4-(4-isopropyl-1-piperazinyl)benzylmethylamino moiety, exhibited the highest affinity for M2 muscarinic receptors, being 200 times as potent as II, and I (R = C-4 4-ethyl-1-piperazinyl, R1 = Et)(III) containing a 4-(4-ethyl-1-piperazinyl)benzylethylamino moiety, showed the highest selectivity for M2 over M3 muscarinic receptors. III and I (R = C-4 4-isopropyl-1-piperazinyl, R1 = Me) also antagonized the oxotremorine-induced bradycardia in rats after i.v. or oral administration. Oral evaluation in conscious dogs showed that the efficacy for increasing the heart rate was at least 3-fold greater than that of II.

Chemical & Pharmaceutical Bulletin published new progress about Cardiotonics. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Computed Properties of 197638-83-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Polo, Efrain; Ferrer-Pertuz, Karoll; Trilleras, Jorge; Quiroga, Jairo; Gutierrez, Margarita published the artcile< Microwave-assisted one-pot synthesis in water of carbonylpyrazolo[3,4-b]pyridine derivatives catalyzed by InCl3 and sonochemical assisted condensation with aldehydes to obtain new chalcone derivatives containing the pyrazolopyridinic moiety>, Name: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is arylidene pyrazoloquinolinone preparation diastereoselective; pyrazolopyridinyl chalcone preparation diastereoselective; pyrazolopyridine green preparation aldehyde Claisen Schmidt base catalyst ultrasound; aminopyrazole formaldehyde beta diketone domino condensation indium catalyst microwave.

An efficient method was developed for the synthesis of pyrazolo[3,4-b]pyridine derivatives, e.g., I, via In-catalyzed one-pot three-component condensation of 3-methyl-1-phenyl-1H-pyrazolo-5-amine, formaldehyde (as paraformaldehyde) and β-diketones under microwave irradiation in aqueous media. This process had advantages of simple operation, higher yields, low cost and environmentally benign procedure. Further sonochem.-assisted Claisen-Schmidt condensation of pyrazolopyridines I with aryl aldehydes under basic catalysis afforded arylidene-pyrazolo[3,4-b]quinolinones II [RR1 = (CH2)2; Ar = Ph, 4-MeOC6H4, 1-methylimidazol-2-yl, etc.] and pyrazolo[3,4-b]pyridinyl chalcones II [R = H, R1 = Me].

RSC Advances published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Name: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Tryniszewski, Michal; Basiak, Dariusz; Barbasiewicz, Michal published the artcile< Olefination with Sulfonyl Halides and Esters: Synthesis of Unsaturated Sulfonyl Fluorides>, Name: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is unsaturated sulfonyl fluoride preparation; sulfonyl halide ester arylaldehyde olefination.

Methanedisulfonyl fluoride, CH2(SO2F)2, transforms aromatic aldehydes into β-arylethenesulfonyl fluorides, useful substrates for the SuFEx “”click””-type transformations. The reaction mimics mechanism of the Horner-Wadsworth-Emmons olefination, which runs via addition of the carbanion, followed by cyclization-fragmentation of the four-membered ring intermediate. In the absence of base, electron-rich aldehydes follow an alternative pathway of the Knoevenagel condensation to provide unsaturated 1,1-disulfonyl fluorides. Authors demonstrate also trapping of elusive ethene-1,1-disulfonyl fluoride, CH2=C(SO2F)2, with 4-(dimethylamino)pyridine (DMAP) that forms zwitterionic adduct, characterized with X-ray studies.

Organic Letters published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Name: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Zhang, Wei; Benmohamed, Radhia; Arvanites, Anthony C.; Morimoto, Richard I.; Ferrante, Robert J.; Kirsch, Donald R.; Silverman, Richard B. published the artcile< Cyclohexane 1,3-diones and their inhibition of mutant SOD1-dependent protein aggregation and toxicity in PC12 cells>, Reference of 197638-83-8, the main research area is cyclohexanedione preparation inhibition mutant SOD1 dependent protein aggregation.

Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease characterized by the progressive loss of motor neurons. Currently, there is only one FDA-approved treatment for ALS (riluzole), and that drug only extends life, on average, by 2-3 mo. Mutations in Cu/Zn superoxide dismutase (SOD1) are found in familial forms of the disease and have played an important role in the study of ALS pathophysiol. On the basis of their activity in a PC12-G93A-YFP high-throughput screening assay, several bioactive compounds have been identified and classified as cyclohexane-1,3-dione (CHD) derivatives A concise and efficient synthetic route has been developed to provide diverse CHD analogs. The structural modification of the CHD scaffold led to the discovery of a more potent analog (I) with an EC50 of 700 nM having good pharmacokinetic properties, such as high solubility, low human and mouse metabolic potential, and relatively good plasma stability. It was also found to efficiently penetrate the blood-brain barrier. However, compound I did not exhibit any significant life span extension in the ALS mouse model. It was found that, although I was active in PC12 cells, it had poor activity in other cell types, including primary cortical neurons, indicating that it can penetrate into the brain, but is not active in neuronal cells, potentially due to poor selective cell penetration. Further structural modification of the CHD scaffold was aimed at improving global cell activity as well as maintaining potency. Two new analogs (II and III) were synthesized, which had significantly enhanced cortical neuronal cell permeability, as well as similar potency to that of I in the PC12-G93A assay. These CHD analogs are being investigated further as novel therapeutic candidates for ALS.

Bioorganic & Medicinal Chemistry published new progress about Aggregation (protein). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Reference of 197638-83-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics