Tag: M.W=150-200

Gallou, Fabrice; Reeves, Jonathan T.; Tan, Zhulin; Song, Jinhua J.; Yee, Nathan K.; Harcken, Christian; Liu, Pingrong; Thomson, David; Senanayake, Chris H. published the artcile< Practical regioselective bromination of azaindoles and diazaindoles>, Reference of 23612-36-4, the main research area is azaindole regioselective bromination copper bromide; diazaindole regioselective bromination; brominated azaindole preparation; pyridine pyrrolo bromo preparation; pyridazine pyrrolo bromo preparation.

A mild and efficient synthesis of various 3-brominated azaindoles and diazaindoles was developed by regioselective halogenation of the parent systems. This practical and high-yielding transformation was achieved with copper(II) bromide in acetonitrile at room temperature

Synlett published new progress about Bromination, regioselective. 23612-36-4 belongs to class pyridine-derivatives, and the molecular formula is C7H5BrN2, Reference of 23612-36-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kanizaj, Lidija; Molcanov, Kresimir; Toric, Filip; Pajic, Damir; Loncaric, Ivor; Santic, Ana; Juric, Marijana published the artcile< Ladder-like [CrCu] coordination polymers containing unique bridging modes of [Cr(C2O4)3]3- and Cr2O72->, Application In Synthesis of 366-18-7, the main research area is crystal structure copper oxalate chromium dichromate diimine coordination polymer; copper oxalate chromium dichromate diimine polymer preparation antiferromagnetic.

Three heterometallic 1-dimensional (1D) coordination polymers {A[CrCu2(bpy)2(C2O4)4]·H2O}n [A = K+ 1 and NH4+ 2; bpy = 2,2′-bipyridine] and [(Cr2O7)Cu2(C2O4)(phen)2]n (3; phen = 1,10-phenanthroline) with uncommon topol. were synthesized using a building block approach and characterized by single-crystal x-ray diffraction, IR and impedance spectroscopies, magnetization measurements, and DFT calculations Due to the partial decomposition of the building block [Cr(C2O4)3]3-, all three compounds contain oxalate-bridged [Cu2(L)2(μ-C2O4)]2+ units [L = bpy 1 and 2 and phen 3]. In compounds 1 and 2, these cations are mutually connected through oxalate groups from [Cr(C2O4)3]3-, thus forming ladder-like topologies. Unusually, three different bridging modes of the oxalate ligand are observed in these chains. In compound 3 Cu(II) ions from cationic units are bridged through the O atoms of Cr2O72- anions in a novel ladder-like mode. Very strong antiferromagnetic coupling observed in all three compounds, determined from the magnetization measurements and confirmed by DFT calculations (J = -343, -371 and -340 cm-1 for 1-3, resp.), appears between two Cu(II) ions interacting through the oxalate bridge.

Dalton Transactions published new progress about Antiferromagnetic exchange. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Application In Synthesis of 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Park, Eunsun; Lee, Sun Joo; Moon, Heegyum; Park, Jongmi; Jeon, Hyeonho; Hwang, Ji Sun; Hwang, Hayoung; Hong, Ki Bum; Han, Seung-Hee; Choi, Sun; Kang, Soosung published the artcile< Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors>, Formula: C8H5ClN2O2, the main research area is methyl pyrrolopyridine carboxamide preparation Janus kinase inhibitor mol docking.

Janus kinase 1 (JAK1) plays a key role in most cytokine-mediated inflammatory and autoimmune responses through JAK/STAT signaling; thus, JAK1 inhibition is a promising therapeutic strategy for several diseases. Anal. of the binding modes of current JAK inhibitors to JAK isoforms allowed the design of N-alkyl-substituted 1-H-pyrrolo[2,3-b] pyridine carboxamides I (R = H, Me, cyclopropyl, cyclopentyl) as a JAK1-selective scaffold, and the synthesis of various Me amide derivatives e.g., II, provided III as a potent JAK1-selective inhibitor. In particular, the (S,S)-enantiomer of III exhibited excellent potency for JAK1 and selectivity over JAK2, JAK3, and TYK2. On investigating the effect of III on hepatic fibrosis, it was found that it reduces the proliferation and fibrogenic gene expression of TGF-β-induced hepatic stellate cells (HSCs). Specifically, III significantly inhibited TGF-β-induced migration of HSCs at 0.25μM in wound-healing assays.

Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 920966-03-6 belongs to class pyridine-derivatives, and the molecular formula is C8H5ClN2O2, Formula: C8H5ClN2O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lv, Tengteng; Song, Tongxiang; Liu, Huijie; Peng, Ruibing; Jiang, Xiamin; Zhang, Weiwei; Han, Qingxi published the artcile< Isolation and characterization of a virulence related Vibrio alginolyticus strain Wz11 pathogenic to cuttlefish, Sepia pharaonis>, HPLC of Formula: 366-18-7, the main research area is Vibrio Sepia virulence hemolysin gene; Bacterial swarming; Haemolysin; Sepia pharaonis; Siderophore production; Vibrio alginolyticus.

Vibrio alginolyticus is a ubiquitous marine opportunistic pathogen that can infect various hosts in marine environment. In the present study, V. alginolyticus strain Wz11 was isolated from diseased cuttlefish, Sepia pharaonis, with 20% of promoted death and high survival capacity in skin mucus and tissue liquid Its growth, siderophore production, and expressions of haemolysin and swarming related genes were characterized under iron limited conditions. The minimal inhibitory concentration (MIC) of 2,2-dipyridyl (DP) to V. alginolyticus strain Wz11 was 640μM. While growth of V. alginolyticus strain Wz11 was inhibited by DP, production of iron-seizing substances, haemolytic activity and swarming motility were increased. Moreover, expressions of haemolysin related genes tlh, tdh and vah and flagellar related genes flgH, fliC, fliD and fliS were also characterized using real-time reverse transcriptase PCR. Expression of tdh was up-regulated to 7.7-fold, while expressions of tlh and vah were down-regulated to 0.016-fold and 0.03-fold, resp. The expression of fliC, flgH, fliD and fliS was up-regulated to 4.9-, 3.8-, 8.6- and 4.5-fold, resp. Concluded from our results suggested that V. alginolyticus strain Wz11 was considered as a potential pathogen of S. pharaonis, and iron level played an important role in the production of iron-seizing substances, and activities of haemolysin and bacterial swarming as well as their related gene expressions.

Microbial Pathogenesis published new progress about Aeromonas hydrophila. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, HPLC of Formula: 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bej, Somnath; Nandi, Mandira; Ghosh, Pradyut published the artcile< Development of fluorophoric [2]pseudorotaxanes and [2]rotaxane: selective sensing of Zn(II)>, Name: 2,2′-Bipyridine, the main research area is .

Fluorophoric [2]pseudorotaxanes {NiPR1(ClO4)2-NiPR3(ClO4)2} are synthesized by utilizing newly designed fluorophoric bidentate ligands (L1-L3) and a heteroditopic naphthalene containing macrocycle (NaphMC) with high yields via Ni(II) templation and π-π stacking interactions. Subsequently, a fluorophoric [2]rotaxane (NAPRTX) is established through a Cu(I) catalyzed click reaction between an azide terminated pseudorotaxane, {NiPR4(ClO4)2}, which contains the newly designed fluorophoric ligand L4, and alkyne terminated bulky stopper units. All these fluorophoric [2]pseudorotaxanes and the [2]rotaxane were characterized using numerous techniques such as mass spectrometry, NMR, UV/Vis, PL, and elemental anal., wherever applicable. Furthermore, to investigate the effect of the fluorophoric moieties, the coordinating ability of chelating units, and size and shape of the three dimensional cavity generated by the mech. bond in the interlocked [2]rotaxane (NAPRTX), we have performed a sensing study of various metal ions. Thus, the interlocked [2]rotaxane is found to have potential as a selective fluorescent sensor for Zn(II) metal ions over other transition, alkali and alk. earth metal ions, where the 2,2′-bipyridyl arylvinylene moiety of the axle acts as a fluorescence signalling unit.

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

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Filla, Sandra A.; Mathes, Brian M.; Johnson, Kirk W.; Phebus, Lee A.; Cohen, Marlene L.; Nelson, David L.; Zgombick, John M.; Erickson, Jon A.; Schenck, Kathryn W.; Wainscott, David B.; Branchek, Theresa A.; Schaus, John M. published the artcile< Novel Potent 5-HT1F Receptor Agonists: Structure-Activity Studies of a Series of Substituted N-[3-(1-Methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides>, Formula: C6H7N3O2, the main research area is pyrrolopyridine amido sulfonamido preparation 5HT receptor agonist migraine; pyrrolopyrimidine amido preparation 5HT receptor agonist migraine.

5-Amidoindole I [X = Y = CH, R = 4-FC6H4; (II)] (LY334370), a selective 5-HT1F receptor agonist (SSOFRA), inhibited dural inflammation in the neurogenic plasma protein extravasation model of migraine and demonstrated clin. efficacy for the acute treatment of migraine. Although II was greater than 100-fold selective over both the 5-HT1B and 5-HT1D receptors, it exhibited appreciable 5-HT1A receptor affinity. Thus, a series of pyrrolo[2,3-c]pyridines I (X = N; Y = CH; R = Me, 4-FC6H4) and pyrrolo[3,2-b]pyridines I (X = CH; Y = N; R = Me, Et, Ph, 3-thienyl, 2-furyl, 2-pyridyl, cyclopropyl, etc.) as well as pyrrolo[3,2-d]pyrimidines I (X = Y = N; R = Me, 4-FC6H4) were synthesized as analogs of II and evaluated in an effort to identify SSOFRAs with improved selectivity over other 5-HT1 receptor subtypes. I (X = CH, Y = N, R = 4-FC6H4) showed high 5-HT1F receptor affinity but offered no improvement in selectivity compared to II; however, I (X = CH, Y = N, R = Me) was greater than 100-fold selective over the 5-HT1A, 5-HT1B, and 5-HT1D receptors. SAR studies of this series determined that alkylamides in particular exhibited high selectivity for the 5-HT1F receptor. These SAR studies identified SSOFRAs that demonstrated oral activity in the neurogenic plasma protein extravasation model, a model indicative of antimigraine activity.

Journal of Medicinal Chemistry published new progress about 5-HT1 agonists. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Formula: C6H7N3O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hu, Ziwei; Banothu, Janardhan; Beesu, Mallesh; Gustafson, Collin J.; Brush, Michael J. H.; Trautman, Kathryn L.; Salyer, Alex C. D.; Pathakumari, Balaji; David, Sunil A. published the artcile< Identification of Human Toll-like Receptor 2-Agonistic Activity in Dihydropyridine-Quinolone Carboxamides>, Formula: C7H7F3N2, the main research area is dihydropyridine quinolone carboxamide synthesis SAR TLR2 vaccine adjuvant.

Using a multiplexed, reporter gene-based, high-throughput screen, we identified 9-fluoro-7-hydroxy-3-methyl-5-oxo-N-(pyridin-3-ylmethyl)-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-6-carboxamide as a TLR2 agonist. Preliminary structure-activity relationship studies on the carboxamide moiety led to the identification of analogs that induce chemokines and cytokines in a TLR2-dependent manner. These results represent new leads for the development of vaccine adjuvants.

ACS Medicinal Chemistry Letters published new progress about Chemokines Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 387350-39-2 belongs to class pyridine-derivatives, and the molecular formula is C7H7F3N2, Formula: C7H7F3N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Romines, Karen R.; Freeman, George A.; Schaller, Lee T.; Cowan, Jill R.; Gonzales, Steve S.; Tidwell, Jeffrey H.; Andrews, Clarence W. III; Stammers, David K.; Hazen, Richard J.; Ferris, Robert G.; Short, Steven A.; Chan, Joseph H.; Boone, Lawrence R. published the artcile< Structure-Activity Relationship Studies of Novel Benzophenones Leading to the Discovery of a Potent, Next Generation HIV Nonnucleoside Reverse Transcriptase Inhibitor>, Synthetic Route of 22280-62-2, the main research area is AntiAIDS reverse transcriptase inhibitor benzophenone preparation structure activity HIV1; AIDS antiviral reverse transcriptase inhibitor benzophenone preparation HIV1.

Despite the progress of the past two decades, there is still considerable need for safe, efficacious drugs that target human immunodeficiency virus (HIV). This is particularly true for the growing number of patients infected with virus resistant to currently approved HIV drugs. Our high throughput screening effort identified a benzophenone template as a potential nonnucleoside reverse transcriptase inhibitor (NNRTI). This manuscript describes our extensive exploration of the benzophenone structure-activity relationships, which culminated in the identification of several compounds with very potent inhibition of both wild type and clin. relevant NNRTI-resistant mutant strains of HIV. These potent inhibitors include 70h (GW678248), which has in vitro antiviral assay IC50 values of 0.5 nM against wild-type HIV, 1 nM against the K103N mutant associated with clin. resistance to efavirenz, and 0.7 nM against the Y181C mutant associated with clin. resistance to nevirapine. Compound 70h has also demonstrated relatively low clearance in i.v. pharmacokinetic studies in three species, and it is the active component of a drug candidate which has progressed to phase 2 clin. studies.

Journal of Medicinal Chemistry published new progress about AIDS (disease). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Synthetic Route of 22280-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hameed P, Shahul; Chinnapattu, Murugan; Shanbag, Gajanan; Manjrekar, Praveena; Koushik, Krishna; Raichurkar, Anandkumar; Patil, Vikas; Jatheendranath, Sandesh; Rudrapatna, Suresh S.; Barde, Shubhada P.; Rautela, Nikhil; Awasthy, Disha; Morayya, Sapna; Narayan, Chandan; Kavanagh, Stefan; Saralaya, Ramanatha; Bharath, Sowmya; Viswanath, Pavithra; Mukherjee, Kakoli; Bandodkar, Balachandra; Srivastava, Abhishek; Panduga, Vijender; Reddy, Jitender; Prabhakar, K. R.; Sinha, Achyut; Jimenez-Diaz, Maria Belen; Martinez, Maria Santos; Angulo-Barturen, Inigo; Ferrer, Santiago; Sanz, Laura Maria; Gamo, Francisco Javier; Duffy, Sandra; Avery, Vicky M.; Magistrado, Pamela A.; Lukens, Amanda K.; Wirth, Dyann F.; Waterson, David; Balasubramanian, V.; Iyer, Pravin S.; Narayanan, Shridhar; Hosagrahara, Vinayak; Sambandamurthy, Vasan K.; Ramachandran, Sreekanth published the artcile< Aminoazabenzimidazoles, a Novel Class of Orally Active Antimalarial Agents>, Category: pyridine-derivatives, the main research area is aminoazabenzimidazole preparation SAR antimalarial Plasmodium.

Whole-cell high-throughput screening of the AstraZeneca compound library against the asexual blood stage of Plasmodium falciparum (Pf) led to the identification of amino imidazoles, a robust starting point for initiating a hit-to-lead medicinal chem. effort. Structure-activity relation studies followed by pharmacokinetics optimization resulted in the identification of (I) as an attractive lead with good oral bioavailability. Compound I was efficacious (ED90 of 28.6 mg·kg-1) in the humanized P. falciparum mouse model of malaria (Pf/SCID model). Representative compounds displayed a moderate to fast killing profile that is comparable to that of chloroquine. This series demonstrates no cross-resistance against a panel of Pf strains with mutations to known antimalarial drugs, thereby suggesting a novel mechanism of action for this chem. class.

Journal of Medicinal Chemistry published new progress about Antimalarials. 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Winter, Andreas; Endres, Patrick; Schroeter, Erik; Jaeger, Michael; Goerls, Helmar; Neumann, Christof; Turchanin, Andrey; Schubert, Ulrich S. published the artcile< Towards covalent photosensitizer-polyoxometalate dyads-bipyridyl-functionalized polyoxometalates and their transition metal complexes>, Computed Properties of 366-18-7, the main research area is hybrid materials; metal complexes; photocatalysis; polyoxometalates.

A triol-functionalized 2,2′-bipyridine (bpy) derivative has been synthesized and used for the tris-alkoxylation of polyoxometalate (POM) precursors. The resultant POM-bpy conjugates of the Wells-Dawson- and Anderson-type feature a C-C bond as a linkage between the POM and bpy fragments. This structural motif is expected to increase the hydrolytic stability of the compounds This is of particular relevance with respect to the application of POM-bpy metal complexes, as photocatalysts, in the hydrogen-evolution reaction (HER) in an aqueous environment. Accordingly, Rh(III) and Ir(III) complexes of the POM-bpy ligands have been prepared and characterized. These catalyst-photosensitizer dyads have been analyzed with respect to their electrochem. and photophys. properties. Cyclic and square-wave voltammetry, as well as UV/vis absorption and emission spectroscopy, indicated a negligible electronic interaction of the POM and metal-complex subunits in the ground state. However, emission-quenching experiments suggested an efficient intramol. electron-transfer process from the photo-excited metal centers to the POM units to account for the non-emissive nature of the dyads (thus, suggesting a strong interaction of the subunits in the excited state). In-depth photophys. investigations, as well as a functional characterization, i.e., the applicability in the HER reaction, are currently ongoing.

Molecules published new progress about 366-18-7. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Computed Properties of 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem