Month: October 2022

Nimje, Roshan Y.; Vytla, Devaiah; Kuppusamy, Prakasam; Velayuthaperumal, Rajeswari; Jarugu, Lokesh Babu; Reddy, China Anki; Chikkananjaiah, Nanjundaswamy Kanikahalli; Rampulla, Richard A.; Cavallaro, Cullen L.; Li, Jianqing; Mathur, Arvind; Gupta, Anuradha; Roy, Amrita published the artcile< Synthesis of differentially protected azatryptophan analogs via Pd2(dba)3/XPhos catalyzed Negishi coupling of N-Ts azaindole halides with zinc derivative from Fmoc-protected tert-butyl (R)-2-amino-3-iodopropanoate>, Category: pyridine-derivatives, the main research area is azatryptophan protected synthesis; azaindole tosyl halide Negishi coupling aminoiodopropanoate zinc.

Unnatural amino acids play an important role in peptide based drug discovery. Herein, we report a class of differentially protected azatryptophan derivatives synthesized from N-tosyl-3-haloazaindoles (I) (Pg = protective groups: Ts (tosyl), Fmoc (9-fluorenylmethoxycarbonyl), and tert-Bu) and Fmoc-protected tert-Bu iodoalanine (II) (Fmoc = 9-fluorenylmethoxycarbonyl) via a Negishi coupling. Through ligand screening, Pd2(dba)3/XPhos was found to be a superior catalyst for the coupling of 1 with the zinc derivative of 2 to give tert-Bu (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-3-(1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)propanoate derivatives (III) (Pg = protective groups: Ts, Fmoc, and tert-Bu; Fmoc = 9-fluorenylmethoxycarbonyl) in 69-91% isolated yields. In addition, we have demonstrated that the protecting groups, namely, Ts, Fmoc, and tert-Bu, can be easily removed selectively.

Journal of Organic Chemistry published new progress about (Fluorenylmethoxy)carbonyl group. 23612-36-4 belongs to class pyridine-derivatives, and the molecular formula is C7H5BrN2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Koovits, Paul J.; Dessoy, Marco A.; Matheeussen, An; Maes, Louis; Caljon, Guy; Mowbray, Charles E.; Kratz, Jadel M.; Dias, Luiz C. published the artcile< Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi>, COA of Formula: C12H14N2O2, the main research area is azaindole piperidine structure activity relationship trypanosoma cruzi chagas disease; Azaindole; Chagas disease; Drug discovery; Neglected diseases.

The structure-activity relationship of a 4-Azaindole-2-piperidine compound selected from GlaxoSmithKline’s recently disclosed open-resource “”Chagas box”” and possessing moderate activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, is presented. Despite considerable medicinal chem. efforts, a suitably potent and metabolically stable compound could not be identified to advance the series into in vivo studies. This research should be of interest to those in the area of neglected diseases and in particular anti-kinetoplastid drug discovery.

Bioorganic & Medicinal Chemistry Letters published new progress about Chagas disease. 1018950-15-6 belongs to class pyridine-derivatives, and the molecular formula is C12H14N2O2, COA of Formula: C12H14N2O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xu, Jingcong; Abetz, Volker published the artcile< Double thermoresponsive graft copolymers with different chain ends: feasible precursors for covalently crosslinked hydrogels>, SDS of cas: 2127-03-9, the main research area is graft copolymer covalently crosslinked hydrogel RAFT polymerization thermoresponsive property.

The tailored synthesis of graft copolymers from acrylic and methacrylic monomers can be accomplished solely through photoiniferter reversible addition-fragmentation chain transfer (RAFT) polymerization Samples with poly[oligo(ethylene glycol) methacrylate] (POEGMA) backbones synthesized under green light irradiation and poly(N-isopropylacrylamide) (PNIPAM) side chains growing under blue light irradiation are presented. As monitored by temperature-dependent dynamic light scattering (DLS) measurements and temperature-variable NMR spectroscopy, the architecture of the graft copolymers allows unique two-step lower critical solution temperature (LCST) transitions in aqueous solutions Meanwhile, different end-groups introduced by the corresponding RAFT agents affect the detailed thermoresponsive behavior remarkably. This RAFT strategy shows more advantages when the multiple trithiocarbonate groups are converted into thiol reactive pyridyl disulfide (PDS) groups via a facile post-polymerization modification. The PDS-terminated graft copolymer can then be regarded as a usable precursor for various applications, such as thermoresponsive hydrogels.

Soft Matter published new progress about Hydrodynamic radius. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, SDS of cas: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wisniewski, Jacek R. published the artcile< Filter Aided Sample Preparation - A tutorial>, Electric Literature of 2127-03-9, the main research area is filter aided sample preparation proteomic ultrafiltration; Detergent removal; Filter Aided Sample Preparation; Lysate preparation; Multi enzyme digestion filter aided sample preparation; Protein digestion conditions; Proteomic sample preparation.

Filter Aided Sample Preparation (FASP) is a widely used protein processing technique in “”bottom-up”” proteomics. Its popularity reflects the key features of the method: its applicability to a variety of sample types and the high quality of the released peptides. Successful application of FASP requires optimized properties of sample lysate and its amount, use of ultrafiltration units with membranes having large mol. mass cut-offs and well selected conditions for protein digestion. In contrast to the majority of sample preparation methods, FASP allows digestion of proteins with a variety of enzymes and a straightforward monitoring of protein-to-peptide conversion. A unique feature of FASP is the possibility to cleave proteins in a consecutive way using several proteases and to sep. peptide fractions. Understanding principles of the method gives guidance in applying FASP to different types of samples in optimization of conditions of the FASP-workflow.

Analytica Chimica Acta published new progress about Critical micelle concentration. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Electric Literature of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fu, Bo; Wang, Xiaobei; Chen, Zhengda; Jiang, Nan; Guo, Zhigang; Zhang, Yuhui; Zhang, Shaopeng; Liu, Xiankun; Liu, Li published the artcile< Improved myocardial performance in infarcted rat heart by injection of disulfide-cross-linked chitosan hydrogels loaded with basic fibroblast growth factor>, Reference of 2127-03-9, the main research area is bFGF cardioprotective disulfide crosslinked chitosan hydrogel myocardial infarction.

Myocardial infarction (MI) has been considered as the leading cause of cardiovascular-related deaths worldwide. Basic fibroblast growth factor (bFGF) is a member of the fibroblast growth factor family that promotes angiogenesis after MI; however, it has poor clin. efficacy due to proteolytic degradation, low drug accumulation, and severe drug-induced side effects. In this study, an injectable disulfide-cross-linked chitosan hydrogel loaded with bFGF was prepared via a thiol-disulfide exchange reaction for MI treatment. The thiol-disulfide exchange reaction between pyridyl disulfide-modified carboxymethyl chitosan (CMCS-S-S-Py) and reduced BSA (rBSA) was carried out under physiol. conditions (37 °C and pH 7.4). The mech. properties of the disulfide-cross-linked chitosan hydrogel were evaluated based on the molar ratio of the pyridyl disulfide groups of CMCS-S-S-Py and the thiol groups of rBSA. The disulfide-cross-linked chitosan hydrogel showed good swelling performance, rapid glutathione-triggered degradation behavior and well-defined cell proliferation towards NIH 3T3 fibroblast cells. In the process of establishing a rat MI model, the squeezing heart method was used to make the operation more accurate and the mortality of rats was decreased by using a ventilator. The disulfide-cross-linked chitosan hydrogel loaded with bFGF (bFGF-hydrogel) was injected into a peri-infarcted area of cardiac tissue immediately following MI. Echocardiog. demonstrated that the left ventricular functions were improved by the bFGF-hydrogel after 28 days of treatment. Histol. results revealed that the hydrogel significantly reduced the fibrotic area of MI, and this was further improved by the bFGF-hydrogel treatment. TUNEL and immunohistochem. staining results showed that the bFGF-hydrogel had a more synergistic effect on antiapoptosis and proangiogenesis than using either bFGF or the hydrogel alone.

Journal of Materials Chemistry B: Materials for Biology and Medicine published new progress about Angiogenesis. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Reference of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xie, Dongsheng; Lu, Jun; Xie, Jin; Cui, Junjun; Li, Teng-Fei; Wang, Yan-Chao; Chen, Yuan; Gong, Nian; Li, Xin-Yan; Fu, Lei; Wang, Yong-Xiang published the artcile< Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent D-amino acid oxidase inhibitor>, Formula: C5H4Cl2N2, the main research area is chlorodihydro pyridopyrazine dione preparation amino acid oxidase inhibitor; 5-Azaquinoxaline-2,3-diones; 8-Chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione; Analgesic effects; D-amino acid oxidase; DAAO inhibitors.

A series of 5-azaquinoxaline-2,3-dione derivatives were synthesized and evaluated on D-amino acid oxidase (DAAO) inhibition as potential α-hydroxylactam-based inhibitors. The potent inhibitory activities in vitro suggested that 5-nitrogen could significantly enhance the binding affinity by strengthening relevant hydrogen bond interactions. The analgesic effects of intrathecal and systemic injection of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione, a representative mol. of 5-azaquinoxaline-2,3-dione, were investigated in rodents. This research not only confirmed the analgesic effect of the DAAO inhibitors but provided a new class of chem. entities with oral application potential for the treatment of chronic pain and morphine analgesic tolerance.

European Journal of Medicinal Chemistry published new progress about Analgesics. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Formula: C5H4Cl2N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Prakash, Muthuraj; Itoh, Yukihiro; Fujiwara, Yoshie; Takahashi, Yukari; Takada, Yuri; Mellini, Paolo; Elboray, Elghareeb E.; Terao, Mitsuhiro; Yamashita, Yasunobu; Yamamoto, Chika; Yamaguchi, Takao; Kotoku, Masayuki; Kitao, Yuki; Singh, Ritesh; Roy, Rohini; Obika, Satoshi; Oba, Makoto; Wang, Dan Ohtan; Suzuki, Takayoshi published the artcile< Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach>, Reference of 329214-79-1, the main research area is fat mass obesity associated protein inhibitor preparation cancer.

Fat mass obesity-associated protein (FTO) is a DNA/RNA demethylase involved in the epigenetic regulation of various genes and is considered a therapeutic target for obesity, cancer, and neurol. disorders. Here, we aimed to design novel FTO-selective inhibitors by merging fragments of previously reported FTO inhibitors. Among the synthesized analogs, compound 11b, which merges key fragments of Hz (3) and MA (4), inhibited FTO selectively over alkylation repair homolog 5 (ALKBH5), another DNA/RNA demethylase. Treatment of acute monocytic leukemia NOMO-1 cells with a prodrug of 11b decreased the viability of acute monocytic leukemia cells, increased the level of the FTO substrate N6-methyladenosine in mRNA, and induced upregulation of MYC and downregulation of RARA, which are FTO target genes. Thus, Hz (3)/MA (4) hybrid analogs represent an entry into a new class of FTO-selective inhibitors.

Journal of Medicinal Chemistry published new progress about Acute monocytic leukemia. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Reference of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Impert, Olga; Kozakiewicz, Anna; Wrzeszcz, Grzegorz; Katafias, Anna; Bienko, Alina; van Eldik, Rudi; Ozarowski, Andrew published the artcile< Characterization of a Mixed-Valence Ru(II)/Ru(III) Ion-Pair Complex. Unexpected High-Frequency Electron Paramagnetic Resonance Evidence for Ru(III)-Ru(III) Dimer Coupling>, Name: 2,2′-Bipyridine, the main research area is ruthenium picolinate bipyridine complex preparation EPR DFT magnetic property; crystal structure ruthenium picolinate bipyridine.

In this contribution, we report the synthesis and full characterization of the first mixed-valence Ru(II)/Ru(III) ion-pair complex, [RuII(bipy)2(pic)]+[cis-RuIIICl2(pic)2]-, in the solid state and in aqueous solution, where bipy = 2,2′-bipyridine and pic- = picolinate. In addition, unexpected high-frequency ESR evidence for interactions between two neighboring Ru(III) ions, resulting in a triplet state, S = 1, was found.

Inorganic Chemistry published new progress about Crystal structure. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Name: 2,2′-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Aretz, Christopher D.; Morwitzer, M. Jane; Sanford, Austin G.; Hogan, Alicia M.; Portillo, Madelene V.; Kharade, Sujay V.; Kramer, Meghan; McCarthey, James B.; Trigueros, Renata Rusconi; Piermarini, Peter M.; Denton, Jerod S.; Hopkins, Corey R. published the artcile< Discovery and Characterization of 2-Nitro-5-(4-(phenylsulfonyl)piperazin-1-yl)-N-(pyridin-4-ylmethyl)anilines as Novel Inhibitors of the Aedes aegypti Kir1 (AeKir1) Channel>, Safety of Pyridin-4-ylmethanamine, the main research area is nitrophenylsulfonylpiperazinylpyridinylmethylaniline preparation Kir1 potassium channel inhibitor Aedes; Kir channels; Zika; larvae; vector-borne diseases.

Mosquito-borne arboviral diseases such as Zika, dengue fever, and chikungunya are transmitted to humans by infected adult female Aedes aegypti mosquitoes and affect a large portion of the world’s population. The Kir1 channel in Ae. aegypti (AeKir1) is an important ion channel in the functioning of mosquito Malpighian (renal) tubules and one that can be manipulated in order to disrupt excretory functions in mosquitoes. We have previously reported the discovery of various scaffolds that are active against the AeKir1 channel. Herein we report the synthesis and biol. characterization of a new 2-nitro-5-(4-(phenylsulfonyl) piperazin-1-yl)-N-(pyridin-4-ylmethyl)anilines scaffold as inhibitors of AeKir1. This new scaffold is more potent in vitro compared to the previously reported scaffolds, and the mols. kill mosquito larvae.

ACS Infectious Diseases published new progress about Aedes aegypti. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Safety of Pyridin-4-ylmethanamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem