Author: Jessica.F

Hailu, Hillete published the artcileVariable denticity of a multidentate terthiophene derivative towards Ni(II) and Zn(II) – structural studies, Synthetic Route of 52431-30-8, the publication is Bulletin of the Chemical Society of Ethiopia (2011), 25(2), 221-231, database is CAplus.

A multidentate ligand, 3,4-bis(2-iminomethylphenol)-2,2′:5,2″-terthiophene (L), was synthesized by the condensation of 3,4-diamino-2,2′:5,2″-terthiophene and salicylaldehyde. The ligand and Ni(II) and Zn(II) complexes were synthesized and characterized by IR, NMR, UV-visible, AAS, MS, molar conductivity and magnetic susceptibility measurements. The ligand behaves as neutral ONS-ONS bis-chelant towards Ni(II) in [Ni₂LCl₄(H₂O)₂]·4H₂O and as dibasic ONNO donor towards Zn(II) in [ZnL(NH₃)₂]. The dinuclear Ni(II) complex exhibits subnormal magnetic moment at room temperature due to metal-metal interaction through extended conjugation. The participation of the ring sulfur in bonding towards Ni(II) and the non-participation of the same towards Zn(II) are notable features. Octahedral geometries are proposed for both complexes. Cyclic voltammetric studies revealed electrochem. polymerization of the free ligand (L) but not of the Ni(II) and Zn(II) complexes.

Bulletin of the Chemical Society of Ethiopia published new progress about 52431-30-8. 52431-30-8 belongs to bromides-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 2,5-Dibromo-3,4-dinitrothiophene, and the molecular formula is C4Br2N2O4S, Synthetic Route of 52431-30-8.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Zhang, Dapeng published the artcileThe Unexpected Importance of the Primary Structure of the Hydrophobic Part of One-Component Ionizable Amphiphilic Janus Dendrimers in Targeted mRNA Delivery Activity, Safety of 1-Bromododecane, the publication is Journal of the American Chemical Society (2022), 144(11), 4746-4753, database is CAplus and MEDLINE.

Viral and synthetic vectors for delivery of nucleic acids impacted genetic nanomedicine by aiding the rapid development of the extraordinarily efficient Covid-19 vaccines. Access to targeted delivery of nucleic acids is expected to expand the field of nanomedicine beyond most expectations. Both viral and synthetic vectors have advantages and disadvantages. The major advantage of the synthetic vectors is their unlimited synthetic capability. The four-component lipid nanoparticles (LNPs) are the leading nonviral vector for mRNA used by Pfizer and Moderna in Covid-19 vaccines. Their synthetic capacity inspired us to develop a one-component multifunctional sequence-defined ionizable amphiphilic Janus dendrimer (IAJD) delivery system for mRNA. The first experiments on IAJDs provided, through a rational-library design combined with orthogonal-modular accelerated synthesis and sequence control in their hydrophilic part, some of the most active synthetic vectors for the delivery of mRNA to lung. The second experiments employed a similar strategy, generating, by a less complex hydrophilic structure, a library of IAJDs targeting spleen, liver, and lung. Here, we report preliminary studies designing the hydrophobic region of IAJDs by using dissimilar alkyl lengths and demonstrate the unexpectedly important role of the primary structure of the hydrophobic part of IAJDs by increasing up to 90.2-fold the activity of targeted delivery of mRNA to spleen, lymph nodes, liver, and lung. The principles of the design strategy reported here and in previous publications indicate that IAJDs could have a profound impact on the future of genetic nanomedicine.

Journal of the American Chemical Society published new progress about 143-15-7. 143-15-7 belongs to bromides-buliding-blocks, auxiliary class Bromide,Aliphatic hydrocarbon chain, name is 1-Bromododecane, and the molecular formula is C7H7ClN2S, Safety of 1-Bromododecane.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Zhang, Dapeng published the artcileThe Unexpected Importance of the Primary Structure of the Hydrophobic Part of One-Component Ionizable Amphiphilic Janus Dendrimers in Targeted mRNA Delivery Activity, SDS of cas: 111-83-1, the publication is Journal of the American Chemical Society (2022), 144(11), 4746-4753, database is CAplus and MEDLINE.

Viral and synthetic vectors for delivery of nucleic acids impacted genetic nanomedicine by aiding the rapid development of the extraordinarily efficient Covid-19 vaccines. Access to targeted delivery of nucleic acids is expected to expand the field of nanomedicine beyond most expectations. Both viral and synthetic vectors have advantages and disadvantages. The major advantage of the synthetic vectors is their unlimited synthetic capability. The four-component lipid nanoparticles (LNPs) are the leading nonviral vector for mRNA used by Pfizer and Moderna in Covid-19 vaccines. Their synthetic capacity inspired us to develop a one-component multifunctional sequence-defined ionizable amphiphilic Janus dendrimer (IAJD) delivery system for mRNA. The first experiments on IAJDs provided, through a rational-library design combined with orthogonal-modular accelerated synthesis and sequence control in their hydrophilic part, some of the most active synthetic vectors for the delivery of mRNA to lung. The second experiments employed a similar strategy, generating, by a less complex hydrophilic structure, a library of IAJDs targeting spleen, liver, and lung. Here, we report preliminary studies designing the hydrophobic region of IAJDs by using dissimilar alkyl lengths and demonstrate the unexpectedly important role of the primary structure of the hydrophobic part of IAJDs by increasing up to 90.2-fold the activity of targeted delivery of mRNA to spleen, lymph nodes, liver, and lung. The principles of the design strategy reported here and in previous publications indicate that IAJDs could have a profound impact on the future of genetic nanomedicine.

Journal of the American Chemical Society published new progress about 111-83-1. 111-83-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Aliphatic hydrocarbon chain, name is 1-Bromooctane, and the molecular formula is C7H5ClN2S, SDS of cas: 111-83-1.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Chang, Linda L. published the artcilePotent and orally active angiotensin II receptor antagonists with equal affinity for human AT₁ and AT₂ subtypes, Application In Synthesis of 76283-09-5, the publication is Journal of Medicinal Chemistry (1995), 38(19), 3741-58, database is CAplus and MEDLINE.

In order to block the effects induced by the interactions between angiotensin II (AII) and both AT₁ and AT₂ receptors, the authors have pursued the discovery of orally active non-peptide AII antagonists that exhibit potent and equal affinity for human AT₁ and AT₂ receptor subtypes. A series of previously prepared nanomolar (IC₅₀) trisubstituted 1,2,4-triazolinone biphenylsulfonamide dual-acting AII antagonists has been modified at five different positions in order to increase AT₂ binding affinity, maintain AT₁ activity, and reduce the human adrenal AT₂/AT₁ potency ratio (IC₅₀ ratio) from ≥10. The targeted human adrenal potency ratio of ≤1 was achieved with a number of compounds possessing an Et group at C⁵ of the triazolinone and a 3-fluoro substituent at the N⁴-biarylmethyl moiety. The most favored of these was triazolinone I which exhibited subnanomolar potency at both the AT₁ (rabbit aorta) and AT₂ (rat midbrain) receptors, with a slight preference for the latter, and had a human adrenal AT₂/AT₁ IC₅₀ ratio of 1. This tert-Bu sulfonylcarbamate had excellent i.v. activity at 1 mg/kg (100% peak inhibition, ≥4 h duration of action) and is orally active at 3 mg/kg with >6 h duration of action in a conscious rat model. The present study shows that the NH of the amide on the N²-aryl moiety is not required for subnanomolar binding affinity to either receptor subtype, although a keto functionality at this position is essential for acceptable AT₂ binding. Receptor-ligand binding interactions derived from the structure-activity relationships are discussed with respect to both receptor subtypes.

Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Application In Synthesis of 76283-09-5.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Chang, L. L. published the artcilePotent triazolinone-based angiotensin II receptor antagonists with equivalent affinity for both the AT₁ and AT₂ subtypes, Name: 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is Bioorganic & Medicinal Chemistry Letters (1994), 4(23), 2787-92, database is CAplus.

A series of subnanomolar (IC₅₀) triazolinone-based AT₁/AT₂-balanced AII antagonists has been identified. The 70-240-fold gain in AT₂ activity relative to prototype compounds was achieved by the introduction of a 5-acylamino group on the N²-aryl moiety and the addition of (3-F-5′-Pr)biphenyl substituents on 4. These analogs exhibited AT₂/AT₁ IC₅₀ ratios of ≤1 in multiple assay systems including human adrenal gland.

Bioorganic & Medicinal Chemistry Letters published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Name: 4-Bromo-1-(bromomethyl)-2-fluorobenzene.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Sarfraz, Ayesha published the artcileSynthesis, In silico and in vitro studies of Silver(I)-N-heterocyclic carbene complexes, Quality Control of 111-83-1, the publication is Journal of Molecular Structure (2022), 131946, database is CAplus.

In the present study, four silver based NHC (N-heterocyclic carbene) complexes (1c–4c) were designed and synthesized from their precursor salts (1b–4b). The successful synthesis of salts and complexes was assured through spectroscopic techniques (UV-visible, FTIR, ¹H NMR) as well as mass spectrometry. The in silico ADMET study and mol. docking calculations predicted the compounds are good drug candidates having therapeutic potential against multiple cancer targets including COX-1, VEGFA, HIF as well as VGF. Results of in vitro study conducted through MTT assay confirmed that all test compounds have concentration dependent potency but silver complexes (1c–4c) have far superior activity than precursor, salts (1b–4b) and slightly lower than standard drugs (carboplatin and cisplatin) against various cancer cell lines. Among the studied compounds, 3c showed lowest IC₅₀ value of 0.981 ± 0.09, 1.10 ± 0.14 and 0.973 ± 0.12μg/mL against MCF-7, HCT-116 and A549 resp. The test compounds were found good antibacterial agents, when screened against bacterial strains (Staphylococcus aureus, Micrococcus luteus, Escherichia coli and S. typhimurium), as well as antioxidant agents when tested against DPPH free radicals.

Journal of Molecular Structure published new progress about 111-83-1. 111-83-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Aliphatic hydrocarbon chain, name is 1-Bromooctane, and the molecular formula is C8H17Br, Quality Control of 111-83-1.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Kajigaeshi, Shoji published the artcileOxidation using quaternary ammonium polyhalides. I. An efficient method for the Hofmann degradation of amides by use of benzyltrimethylammonium tribromide, COA of Formula: C10H16Br3N, the publication is Chemistry Letters (1989), 463-4, database is CAplus.

The reaction of amides with a calculated amount of benzyltrimethylammonium tribromide (I) in aqueous NaOH under mild conditions gave corresponding amines in fairly good yields. Thus benzmide gave 72% aniline in the presence of I in aqueous NaOH.

Chemistry Letters published new progress about 111865-47-5. 111865-47-5 belongs to bromides-buliding-blocks, auxiliary class Benzenes, name is Mono(N,N,N-trimethyl-1-phenylmethanaminium) tribromide, and the molecular formula is C10H16Br3N, COA of Formula: C10H16Br3N.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Mylari, Banavara L. published the artcileA novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners, Category: bromides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2005), 48(20), 6326-6339, database is CAplus and MEDLINE.

Discovery of a highly selective, potent, and safe non-carboxylic acid, non-hydantoin inhibitor of aldose reductase (AR) capable of potently blocking the excess glucose flux through the polyol pathway that prevails under diabetic conditions has been a long-standing challenge. In response, we did high-throughput screening of our internal libraries of compounds and identified 6-phenylsulfonylpyridazin-2H-3-one, 8, which showed modest inhibition of AR, both in vitro and in vivo. Initial structure-activity relationships concentrated on Ph substituents and led to 6-(2,4-dichlorophenylsulfonyl)-2H-pyridazin-3-one, 8l, which was more potent than 8, both in vitro and in vivo. Incorporation of extant literature findings with other aldose reductase inhibitors, including zopolrestat, resulted in the title inhibitor, 19m, which is one of the most potent and highly selective non-carboxylic acid, non-hydantoin inhibitors of AR yet described (IC₅₀, 1 nM; ED₉₀ vs sciatic nerve sorbitol and fructose, resp., 0.8 and 4.0 mg/kg). In rats, its oral bioavailability is 98% and it has a favorable plasma t_1/2 (26 ± 3 h).

Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Category: bromides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Fujita, Takeshi published the artcileCatalytic defluorinative [3 + 2] cycloaddition of trifluoromethylalkenes with alkynes via reduction of nickel(II) fluoride species, Name: 7-Bromohept-1-yne, the publication is Dalton Transactions (2015), 44(45), 19460-19463, database is CAplus and MEDLINE.

Nickel-catalyzed [3+2] cycloaddition of 2-trifluoromethyl-1-alkenes with alkynes via domino C-F bond activation was achieved by sequential β-fluorine elimination to give corresponding cyclopentadienes I [R¹ = C₆H₅, 3-FC₆H₄, t-BuOC(O), etc.; R² = n-Pr, iPr; R³ = Me, n-Pr] regioselectively. The nickel(II) fluoride species formed in this reaction was reduced by a diboron compound, regenerating the catalytically active nickel(0) species.

Dalton Transactions published new progress about 81216-14-0. 81216-14-0 belongs to bromides-buliding-blocks, auxiliary class Linker,PROTAC Linker, name is 7-Bromohept-1-yne, and the molecular formula is C7H11Br, Name: 7-Bromohept-1-yne.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

O’Brien, Luke published the artcileGold(I)-Catalyzed Nucleophilic Allylation of Azinium Ions with Allylboronates, Category: bromides-buliding-blocks, the publication is Angewandte Chemie, International Edition (2022), 61(22), e202202305, database is CAplus and MEDLINE.

Gold(I)-catalyzed nucleophilic allylations of pyridinium and quinolinium ions with various allyl pinacolboronates was reported. The reactions was completely selective with respect to the site of the azinium ion that was attacked, to give various functionalized 1,4-dihydropyridines and 1,4-dihydroquinolines. Evidence suggested that the reactions proceed through nucleophilic allylgold(I) intermediates formed by transmetalation from allylboronates. D. functional theory (DFT) calculations provided mechanistic insight.

Angewandte Chemie, International Edition published new progress about 111-83-1. 111-83-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Aliphatic hydrocarbon chain, name is 1-Bromooctane, and the molecular formula is C8H17Br, Category: bromides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary