Tag: M.W=200-250

Roberts, Dean D.; McLaughlin, Mark G. published the artcile< Regioselective Synthesis of Multifunctional Allylic Amines; Access to Ambiphilic Aziridine Scaffolds>, Synthetic Route of 22952-32-5, the main research area is allylic amine ambiphilic aziridine preparation regioselective; propargylic amine dimethylphenylsilane hydrosilylation platinum chloride XantPhos catalyst.

A highly regioselective hydrosilylation of propargylic amines has been described here for the first time. The reaction utilizes a PtCl2/XantPhos catalyst system to deliver hydrosilanes across the alkyne to afford multifunctional allylic amines in high yields. The reaction is tolerant to a wide variety of functional groups and provides high value intermediates with two distinct functional handles. The synthetic applicability of the reaction has been shown through the synthesis of diverse ambiphilic aziridines.

Organic Letters published new progress about Allyl amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Synthetic Route of 22952-32-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Bischof, Joachim; Leban, Johann; Zaja, Mirko; Grothey, Arnhild; Radunsky, Barbara; Othersen, Olaf; Strobl, Stefan; Vitt, Daniel; Knippschild, Uwe published the artcile< 2-Benzamido-N-(1H-benzo[d]imidazol-2-yl)thiazole-4-carboxamide derivatives as potent inhibitors of CK1δ/ε>, Electric Literature of 162046-61-9, the main research area is benzamidobenzoimidazolylthiazolecarboxamide derivative preparation inhibition casein kinase 1 isoenzyme antitumor; crystal structure casein kinase isoenzyme inhibitor complex.

In this study two heterocyclic compounds (5 and 6) were identified as potent and specific inhibitors of CK1δ (IC50 = 0.040 and 0.042 μM, resp.). Whereas compound 5 exhibited 5-fold higher affinity toward CK1δ than to CK1ε (IC50 CK1ε = 0.199 μM), compound 6 also inhibited CK1ε (IC50 = 0.0326 μM) in the same range as CK1δ. Selected compound 5 was screened over 442 kinases identifying 5 as a highly potent and selective inhibitor of CK1δ. X-ray anal. of 5 bound to CK1δ demonstrated its binding mode. In addition, characterization of 5 and 6 in a cell biol. approach revealed the ability of both compounds to inhibit proliferation of tumor cell lines in a dose and cell line specific manner. In summary, these optimizations lead to the development of new highly selective CK1δ and ε specific inhibitors with biol. activity.

Amino Acids published new progress about Antitumor agents. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Electric Literature of 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jatav, Varsha; Kashaw, Sushil; Mishra, Pradeep published the artcile< Synthesis, antibacterial and antifungal activity of some novel 3-[5-(4-substituted phenyl) 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones>, Application of C8H6ClN3S, the main research area is aryl thiadiazolyl styryl quinazolinone preparation antibacterial antifungal activity.

A series of novel 3-[5-substituted phenyl-1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones, e.g., I, were synthesized and evaluated for antibacterial activity against pathogenic strains of Staphylococcus aureus (MTCC number 96), Bacillus subtilis (MTCC number 619), Pseudomonas aeruginosa (MTCC number 424) and Escherichia coli (MTCC number 40) and antifungal activity against Aspergillus niger, Candida albicans and Fusarium oxysporum. The cup-plate method was employed to determine the min. inhibitory concentration (MIC) value of the compounds Some of the compounds exhibited activity comparable to Norfloxacin. The present report reveals that synthesized 2-styryl-quinazoline-4(3H)-one exhibited better antibacterial than antifungal activity.

Medicinal Chemistry Research published new progress about Antibacterial agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Application of C8H6ClN3S.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

McClure, Kelly J.; Maher, Michael; Wu, Nancy; Chaplan, Sandra R.; Eckert, William A. III; Lee, Dong H.; Wickenden, Alan D.; Hermann, Michelle; Allison, Brett; Hawryluk, Natalie; Breitenbucher, J. Guy; Grice, Cheryl A. published the artcile< Discovery of a novel series of selective HCN1 blockers>, COA of Formula: C8H4ClF3O2, the main research area is HCN1 blocker preparation SAR; heterocyclylindanemethyl heterocyclylethyl benzamide preparation; structure heterocyclylindanemethyl heterocyclylethyl benzamide inhibition HCN1 cation channel.

The discovery of a series of novel, potent, and selective blockers of the hyperpolarization-activated cation-nonselective cyclic nucleotide-modulated ion channel HCN1 is disclosed. Here we report an SAR study around a series of selective blockers of the HCN1 channel. Utilization of a high-throughput VIPR assay led to the identification of a novel series of 2,2-disubstituted indane derivatives, which had moderate selectivity and potency at HCN1. Optimization of this hit led to the identification of the potent, 1,1-disubstituted cyclohexane HCN1 blocker, 2-ethoxy-N-((1-(4-isopropylpiperazin-1-yl)cyclohexyl)methyl)benzamide. The work leading to the discovery of this compound is described herein.

Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, COA of Formula: C8H4ClF3O2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Laeckmann, Didier; Rogister, Francoise; Dejardin, Jean-Victor; Prosperi-Meys, Christelle; Geczy, Joseph; Delarge, Jacques; Masereel, Bernard published the artcile< Synthesis and biological evaluation of aroylguanidines related to amiloride as inhibitors of the human platelet Na+/H+ exchanger>, Product Details of C6H2Cl3NO2, the main research area is pyridine benzene isostere amiloride preparation sodium hydrogen exchanger inhibitor; structure amiloride isostere activity inhibitor sodium hydrogen exchanger.

Pyridine and benzene bioisosteres of amiloride such as I and II were synthesized and evaluated for their inhibitory potency against the sodium-hydrogen exchanger involved in intracellular pH regulation. Substituted diaminochloro-2-pyridinecarbonyl and diaminochloro-3-pyridinecarbonyl guanidines are prepared from 2-chloro-6-methyl-3,5-dinitropyridine and 2-methyl-1,5-pentanedinitrile, resp. Dichloro- and trichloropyridine-3-carbonyl guanidines, and simple pyridinecarbonyl and benzoyl guanidines are also prepared Several benzene derivatives and compounds bearing an carbonylguanidine moiety in the meta position of the pyridine nitrogen were much more potent than amiloride, but less so than the pyrazine inhibitor III (R = Et; R1 = Me2CH). II is the most active mol. in assays measuring the reduction in human platelet swelling due to sodium ion uptake and in assays of the inhibition of sodium ion uptake, with IC50 values of 0.8 μM in both assays. Replacement of the pyrazine ring of amiloride III (R = R1 = H) by a pyridine or a Ph ring improved the inhibitory potency for the sodium-hydrogen exchanger involved in intracellular pH regulation in the order Ph > pyridine > pyrazine.

Bioorganic & Medicinal Chemistry published new progress about Homo sapiens. 54718-39-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H2Cl3NO2, Product Details of C6H2Cl3NO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Pandit, Neelanjana; Shah, Kamal; Agrawal, Neetu; Upmanyu, Neeraj; Shrivastava, Sushant K.; Mishra, Pradeep published the artcile< Synthesis, characterization and biological evaluation of some novel fluoroquinolones>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is fluoroquinolone thiadiazole derivative preparation bactericide fungicide.

Different derivatives of fluoroquinolones were synthesized by combining them with different thiadiazoles. The synthesized compounds were characterized by IR spectroscopy, proton NMR and mass spectral data. The compounds were screened for their antibacterial and antifungal activity. Ciprofloxacin thiadiazole 7c (I) showed good antibacterial as well as antifungal activities, whereas 13c and 13e (II; R1 = Cl, R2 = H and R1 = R2 = OMe, resp.) showed antibacterial and antifungal activity resp. Sparfloxacin derivative 8c (III) showed both antibacterial and antifungal activity. Sparfloxacin derivatives 14b and 14e (IV; R1 = H, R2 = Cl and R1 = R2 OMe) showed antibacterial and antifungal activity resp.

Medicinal Chemistry Research published new progress about Antibacterial agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Ferro, Stefania; Buemi, Maria Rosa; De Luca, Laura; Agharbaoui, Fatima E.; Pannecouque, Christophe; Monforte, Anna-Maria published the artcile< Searching for novel N1-substituted benzimidazol-2-ones as non-nucleoside HIV-1 RT inhibitors>, Product Details of C8H8BrCl, the main research area is benzimidazolone synthesis HIV1 reverse transcriptase inhibitor; Benzimidazolones; Design; RTs mutant; Reverse transcriptase inhibitors; Synthesis.

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) represent an integral part of the currently available combination antiretroviral therapy (cART) contributing to reduce the AIDS-mortality and turned the disease from lethal to chronic. In this context we recently reported a series of 6-chloro-1-(3-methylphenylsulfonyl)-1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. In this paper, we describe the design and the synthesis of two novel series of benzimidazolone analogs in which the linker moiety between the Ph ring and the sulfonyl group was modified and new small lipophilic groups on the benzyl sulfonyl pendant were introduced. All the new obtained compounds were evaluated as RT inhibitors and were also tested against RTs containing single amino acid mutations. Finally, mol. docking studies were performed in order to rationalize the observed activity of the most promising compound

Bioorganic & Medicinal Chemistry published new progress about Anti-HIV agents. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Product Details of C8H8BrCl.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zhou, Jie; Zhang, Yi; Cui, Yi-Wen; Li, Zhan-Mei; Song, Hong-Rui; Dong, Jin-Hua; Chen, Xiao-Guang; Xu, Bai-Ling published the artcile< Synthesis and cytotoxic evaluation of N-(4-methoxy-1H-benzimidazol-7-yl)arenesulfonamide and N-aryl-(4-methoxy-1H-benzimidazol)-7-sulfonamide analogs of combretastatin A-4>, Computed Properties of 42413-03-6, the main research area is antitumor anticancer agent combretastatin analog preparation.

Benzimidazole derivatives [Combretastatin A-4 2-methoxy-5-[(1Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol analogs] were designed and the synthesis of the target compounds was achieved using 4-methoxy-1H-benzimidazol-7-amine and 4-Methoxy-1H-benzimidazole-7-sulfonic acid as reactants. The title compounds were evaluated in-vitro against cell line HCT-8 (human epithelial intestinal adenocarcinoma, colon carcinoma), cell line BEL-7402 (hepatocellular carcinoma, human hepatoma, liver cancer cell line), cell line BGC 823 (human gastric cancer cell line, stomach adenocarcinoma), cell line A549 (human lung carcinoma cell line) and cell line A-2780 (human ovarian carcinoma cell line) and it was discovered that several compounds displayed cytotoxic activity against the HCT-8 cell line.

Journal of Asian Natural Products Research published new progress about Adenocarcinoma (epithelial adenocarcinoma, intestine). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Computed Properties of 42413-03-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics