Tag: M.W:200-300

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Synthesis and antiviral activity of a series of novel quinoline derivatives as anti-RSV or anti-IAV agents, published in 2021-03-15, which mentions a compound: 111-24-0, mainly applied to quinoline preparation antiviral activity antiRSV antiIAV agent; Anti-IAV; Anti-RSV; Quinoline derivatives; Structure-activity relationships; Synthesis, Application of 111-24-0.

The synthesis of a series of novel quinoline derivatives, I [R = pyrrolidin-1-yl, methylamino, morpholin-4-yl, etc; R1 = benzyl, adamantan-1-yl, furan-2-ylmethyl, etc; R2 = H; R1R2 = -(CH2)2O(CH2)2-], II (n = 3, 4, 5) based on the lead compound I (R = pyrrolidin-1-yl; R1 = benzyl; R2 = H) (III), identified from a rRSV-mGFP high-throughput screening assay was reported. The results revealed that target compounds I (R = pyrrolidin-1-yl, R1 = 4-fluorobenzyl, R2 = H; R = pyrrolidin-1-yl, R1 = 4-methoxybenzyl, R2 = H; R = pyrrolidin-1-yl, R1 = 3-methoxybenzyl, R2 = H; R = dimethylamino, R1 = benzyl, R2 = H; R = (S)-3-tert-butoxycarbonylaminopyrrolidin-1-yl, R1 = benzyl, R2 = H) (IC50 = 3.10-6.93μM) had good in vitro activity against RSV, which were better than I (R = pyrrolidin-1-yl, R1 = benzyl, R2 = H) and ribavirin. In addition, it is found that compound I (R = 1-tert-butoxycarbonylpiperazin-4-yl, R1 = benzyl, R2 = H) displayed the lower cytotoxicity (CC50: 2490.33μM) and the highest selective index (SI = 673.06), suggest its promising potential as a candidate for further development. On the other hand, some compounds (IC50: 1.87-14.28μM) were more active against IAV than or comparable to ribavirin (IC50: 15.36 ± 0.93μM). Particularly, the most active compound I (R = (S)-3-tert-butoxycarbonylaminopyrrolidin-1-yl, R1 = benzyl, R2 = H) (IC50: 1.87 ± 0.58μM) was found to be 8.2-fold more potent than the reference drug, which could inhibit the virus transcription and replication cycle at an early stage.

In some applications, this compound(111-24-0)Application of 111-24-0 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Arakawa, Yuki; Komatsu, Kenta; Inui, Satoyoshi; Tsuji, Hideto researched the compound: 1,5-Dibromopentane( cas:111-24-0 ).Computed Properties of C5H10Br2.They published the article 《Thioether-linked liquid crystal dimers and trimers: The twist-bend nematic phase》 about this compound( cas:111-24-0 ) in Journal of Molecular Structure. Keywords: thioether linked biphenylcyanide dimer trimer liquid crystal preparation. We’ll tell you more about this compound (cas:111-24-0).

Systematic synthesis of thioether-linked dimers and trimers was carried out to reveal mol. designs for inducing mesophases and twist-bend nematic (NTB) phases. A five-fold approach based on mol. structural parameters including the terminal substituent, the position of the thioether bond, the nature of the bridge bond linking benzene rings in the mesogenic fragments, the nature of bonds at the linkage on the side oppose to the thioether linkage, and oligomeric effect was evaluated. Dimers with cyano groups at the 4,4′-positions in each mesogenic fragment of the thioether-based dimeric system were found to afford a large long-axis directional dipole moment in the fragments and exhibited potential for application as mesogens, with some mols. indicating the ability to form NTB phase. The dimers containing the thioether bond as a part of the spacer and not at the linkage position to the mesogenic fragments deteriorate as twist-bend nematogens but behave as traditional nematogens. Also, imine-, azo- and triple-bond bridged mesogenic fragments lead the dimers to be twist-bend nematogenic. Notably, all asym. thioether-linked cyanobiphenyl dimers with different functional bonds at the linkage on the side oppose to the thioether linkage, such as methylene, ketone, and two-typed esters (C=OO and OC=O) can form NTB phases, with some of them retaining the phase upon cooling to room temperature, which highlights the utility of thioether linkage in the mol. design of twist-bend nematogens. In the trimer system (or oligomeric effect), a cyanobiphenyl-based trimer composed of interior ether and exterior thioether linkers formed an NTB phase. This paper, for the first time, not only reveals the systematic mol. design of thioether-linked dimers but also offers the prospect of the thioether-linked oligomers, for twist-bend nematic liquid crystals.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 1,5-Dibromopentane, is researched, Molecular C5H10Br2, CAS is 111-24-0, about Effect of linker length on photo-cross-linking position mediated by click chemistry via [2 + 2]photocycloaddition, the main research direction is cyanovinylcarbazole photocross linker photocycloaddition.COA of Formula: C5H10Br2.

Ultrafast reversible DNA/RNA photo-crosslinking is a powerful tool for regulating the target strand in living cells. In particular, 3-cyanovinylcarbazole (CNVK) and 3-cyanovinylcarbazole modified by D-threoninol (CNVD) can photo-cross-link to pyrimidine bases within a few seconds of photoirradiation However, these photo-cross-linkers can only cross-link to the counter base if it is adjacent to the 5′-side (-1 position). In this study, we synthesized novel photo-cross-linkers with varying linker lengths capable of photo-crosslinking with pyrimidine bases at locations other than the -1 position via click chem. The photo-crosslinking site was dependent on linker length.

This literature about this compound(111-24-0)COA of Formula: C5H10Br2has given us a lot of inspiration, and I hope that the research on this compound(1,5-Dibromopentane) can be further advanced. Maybe we can get more compounds in a similar way.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Quality Control of 1,5-Dibromopentane. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 1,5-Dibromopentane, is researched, Molecular C5H10Br2, CAS is 111-24-0, about Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression. Author is Zhang, Meng; Aguilar, Angelo; Xu, Shilin; Huang, Liyue; Chinnaswamy, Krishnapriya; Sleger, Taryn; Wang, Bo; Gross, Stefan; Nicolay, Brandon N.; Ronseaux, Sebastien; Harvey, Kaitlin; Wang, Yu; McEachern, Donna; Kirchhoff, Paul D.; Liu, Zhaomin; Stuckey, Jeanne; Tron, Adriana E.; Liu, Tao; Wang, Shaomeng.

Targeting the menin-MLL protein-protein interaction is being pursued as a new therapeutic strategy for the treatment of acute leukemia carrying MLL-rearrangements (MLLr leukemia). Herein, we report M-1121(I), a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression. M-1121 (I) establishes covalent interactions with Cysteine 329 located in the MLL binding pocket of menin and potently inhibits growth of acute leukemia cell lines carrying MLL translocations with no activity in cell lines with wild-type MLL. Consistent with the mechanism of action, M-1121 (I) drives dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line. M-1121 (I) is orally bioavailable and shows potent antitumor activity in vivo with tumor regressions observed at tolerated doses in the MV4;11 s.c. and disseminated models of MLL-rearranged leukemia. Together, our findings support development of an orally active covalent menin inhibitor as a new therapy for MLLr leukemia.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Synthetic Route of C5H3Cl2NO2S. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2-Chloro-5-pyridinesulfonyl chloride, is researched, Molecular C5H3Cl2NO2S, CAS is 6684-39-5, about Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity. Author is Gong, Hua; Weinstein, David S.; Lu, Zhonghui; Duan, James J.-W.; Stachura, Sylwia; Haque, Lauren; Karmakar, Ananta; Hemagiri, Hemalatha; Raut, Dhanya Kumar; Gupta, Arun Kumar; Khan, Javed; Camac, Dan; Sack, John S.; Pudzianowski, Andrew; Wu, Dauh-Rurng; Yarde, Melissa; Shen, Ding-Ren; Borowski, Virna; Xie, Jenny H.; Sun, Huadong; D’Arienzo, Celia; Dabros, Marta; Galella, Michael A.; Wang, Faye; Weigelt, Carolyn A.; Zhao, Qihong; Foster, William; Somerville, John E.; Salter-Cid, Luisa M.; Barrish, Joel C.; Carter, Percy H.; Dhar, T. G. Murali.

We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists. However, a majority of these compounds showed potent activity against pregnane X receptor (PXR) and modest activity against liver X receptor α (LXRα). Structure-based drug design (SBDD) led to the identification of benzothiazine and tetrahydroquinoline sulfonamide analogs which completely dialed out LXRα activity and were less potent at PXR. Pharmacodynamic (PD) data for compound 35 in an IL-23 induced IL-17 mouse model is discussed along with the implications of a high Ymax in the PXR assay for long term preclin. pharmacokinetic (PK) studies.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Safety of 1,5-Dibromopentane. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1,5-Dibromopentane, is researched, Molecular C5H10Br2, CAS is 111-24-0, about Crystal structure and halogen-hydrogen bonding of a Delepine reaction intermediate. Author is Mulrooney, David Z. T.; Muller-Bunz, Helge; Keene, Tony D..

The reaction of 1,5-dibromopentane with urotropine results in crystals of the title mol. salt, 5-bromourotropinium bromide [systematic name: 1-(5-bromopentyl)-3,5,7-triaza-1-azoniatricyclo[3.3.1.13,7]decane bromide], C11H22BrN4+·Br- (1), crystallizing in space group P21/n. The packing in compound 1 is directed mainly by H···H van der Waals interactions and C-H···Br hydrogen bonds, as revealed by Hirshfeld surface anal. Comparison with literature examples of alkylurotropinium halides shows that the interactions in 1 are consistent with those in other bromides and simple chloride and iodide species.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Annulation of Indoles with 1,n-Dibromoalkanes by a Pd(II)-Catalyzed and Norbornene-Mediated Reaction Cascade, published in 2020-04-30, which mentions a compound: 111-24-0, mainly applied to carbazole tetrahydro preparation regioselective; dibromoalkane indole tandem cyclization palladium catalyst, Recommanded Product: 111-24-0.

By employing 1,3-dibromopropane, 1,4-dibromobutane, and 1,5-dibromopentane as biselectrophiles, the annulation of indoles I (R = H, 5-Br, 4-CN, 5-t-BuO2C, etc.) was probed in the presence of PdCl2(CH3CN)2 as a catalyst and norbornene as a transpositional ligand. Ring formation to a five-membered ring was observed at positions C2 and N, while annulation of a six-membered ring occurred at positions C2 and C3. The latter cascade process was successfully applied to the direct synthesis of 1,2,3,4-tetrahydrocarbazoles II from indoles I (11 examples, 31-68% yields). Seven-membered-ring annulation was feasible by an initial coupling at position C2 followed by alkylation at C3.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Ether spaced N-spirocyclic quaternary ammonium functionalized crosslinked polysulfone for high alkaline stable anion exchange membranes, published in 2020-03-15, which mentions a compound: 111-24-0, mainly applied to ether spirocyclic quaternary ammonium crosslinked polysulfone anion exchange membrane, Category: chiral-nitrogen-ligands.

N-spirocyclic cations containing anion exchange membranes (AEMs) possess excellent alk. stability, but poor mech. and conductive properties due to the rigid N-spirocyclic structure and lack of flexible side chain structural design. In this work, a flexible ether spaced N-spirocyclic quaternary ammonium functionalized side chain is proposed, in which hydroxyl substituted N-spirocyclic cation provides active grafting site with chloromethylated polysulfone through Williamson etherification. The flexible ether-oxygen spacer promotes aggregation of the rigid spirocyclic cations and thus significantly improves conductivity The uniformly in-situ thermal crosslinking between benzene rings and the residue chloromethyl groups in polysulfone greatly enhances mech. properties of the membranes. Constrained ring conformation of N-spirocyclic cation, ether spaced benzyl-free side chain, as well as the OH- blocking crosslinked networks endow an excellent alk. stability to the membranes. The ether spaced N-spirocyclic containing membranes exhibit well micro-phase separation structure, up to around 85.7 mS cm-1 of hydroxide conductivity at 80°C, around 10.5 MPa of tensile strength in hydrated state and around 95.6% conductivity retention after immersion in 1 M KOH at 80°C for 720 h. The performance is among the best N-spirocyclic functionalized AEMs reported in the literature.

There are many compounds similar to this compound(111-24-0)Category: chiral-nitrogen-ligands. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis, published in 2019-08-08, which mentions a compound: 6684-39-5, Name is 2-Chloro-5-pyridinesulfonyl chloride, Molecular C5H3Cl2NO2S, Electric Literature of C5H3Cl2NO2S.

Osteoporosis is predominantly treated with drugs that inhibit further bone resorption due to estrogen deficiency. Yet, osteoporosis drugs that not only inhibit bone resorption but also stimulate bone formation, such as potentially inhibitors of 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2), may be more efficacious in the treatment of osteoporosis. Blockade of 17β-HSD2 is thought to increase intracellular estradiol and testosterone in bone, thereby inhibiting bone resorption by osteoclasts and stimulating bone formation by osteoblasts, resp. We here describe the design, synthesis, and biol. characterization of a novel bicyclic-substituted hydroxyphenylmethanone 17β-HSD2 inhibitor (I). Compound I is a nanomolar potent inhibitor of human 17β-HSD2 (IC50 of 6.1 nM) and rodent 17β-HSD2 with low in vitro cellular toxicity, devoid of detectable estrogen receptor α affinity, displays high aqueous solubility and in vitro metabolic stability, and has an excellent oral pharmacokinetic profile for testing in a rat osteoporosis model. Administration of I in a rat osteoporosis model demonstrates its bone-sparing efficacy.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Abdpour, Shahin; Jalili-Baleh, Leili; Nadri, Hamid; Forootanfar, Hamid; Bukhari, Syed Nasir Abbas; Ramazani, Ali; Ebrahimi, Seyed Esmaeil Sadat; Foroumadi, Alireza; Khoobi, Mehdi researched the compound: 1,5-Dibromopentane( cas:111-24-0 ).Related Products of 111-24-0.They published the article 《Chromone derivatives bearing pyridinium moiety as multi-target-directed ligands against Alzheimer’s disease》 about this compound( cas:111-24-0 ) in Bioorganic Chemistry. Keywords: pyridiniumyl alkoxy phenyl chromenone preparation cytotoxicity ADMET docking neuroprotective; chromenone pyridiniumyl alkoxy preparation human AChE BuChE inhibition antitumor; Alzheimer’s disease; Anti-amyloid aggregation; Cholinesterase inhibitors; Chromone; Neuroprotective activity; Pyridinium salts. We’ll tell you more about this compound (cas:111-24-0).

A new serise of 7-hydroxy-chromone derivatives bearing pyridine moiety I [R = H, Ph, 4-ClC6H4, etc.; R1 = H, Et; n= 3, 4, 5] were synthesized and evaluated as multifunctional agents against Alzheimer’s disease (AD). Most of the compounds I were good AChE inhibitors (IC50 = 9.8-0.71μM) and showed remarkable BuChE inhibition activity (IC50 = 1.9-0.006μM) compared with donepezil as the standard drug (IC50 = 0.023 and 3.4μM). Compounds I [R = 4-ClC6H4, R1 = H, n = 4] and I [R = 4-MeOC6H4, R1 = Et, n = 3] showed the best inhibitory activity toward AChE (IC50 = 0.71μM) and BuChE (IC50 = 0.006μM), resp. The ligand-protein docking simulations and kinetic studies revealed that compound I [R = 4-ClC6H4, R1 = H, n = 4] and I [R = 4-MeOC6H4, R1 = Et, n = 3] could bind effectively to the peripheral anionic binding site (PAS) of the AChE and BuChE through mixed-type inhibition. In addition, the most potent compounds I [R = 4-ClC6H4, 4-MeC6H4, R1 = H, Et, n = 4, 3] showed acceptable neuroprotective activity on H2O2- and Aβ-induced .neurotoxicity in PC12 cells, more than standard drugs. The compounds I could block effectively self- and AChE-induced Aβ aggregation. All the results suggest that compounds I [R = 4-ClC6H4, 4-MeC6H4, R1 = H, Et, n = 4, 3] could be considered as promising multi-target-directed ligands against AD.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis