Tag: M.W=250-300

Kancharla, Papireddy published the artcileLead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials, Recommanded Product: (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, the publication is Journal of Medicinal Chemistry (2020), 63(11), 6179-6202, database is CAplus and MEDLINE.

The global impact of malaria remains staggering despite extensive efforts to eradicate the disease. With increasing drug resistance and the absence of a clin. available vaccine, there is an urgent need for novel, affordable, and safe drugs for prevention and treatment of malaria. Previously, we described a novel antimalarial acridone chemotype that is potent against both blood-stage and liver-stage malaria parasites. Here, we describe an optimization process that has produced a second-generation acridone series with significant improvements in efficacy, metabolic stability, pharmacokinetics, and safety profiles. These findings highlight the therapeutic potential of dual-stage targeting acridones as novel drug candidates for further preclin. development.

Journal of Medicinal Chemistry published new progress about 21101-63-3. 21101-63-3 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,sulfides,Benzyl bromide,Benzene, name is (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, and the molecular formula is C8H6BrF3S, Recommanded Product: (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane.

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

Yu, Yingjian published the artcileA p-π* conjugated triarylborane as an alcohol-processable n-type semiconductor for organic optoelectronic devices, Recommanded Product: 2-Bromo-3-(2-ethylhexyl)thiophene, the publication is Journal of Materials Chemistry C: Materials for Optical and Electronic Devices (2019), 7(24), 7427-7432, database is CAplus.

A p-π* conjugated organic mol. based on triarylborane is reported as n-type organic semiconductor with unique alc. solubility Its favorable alc. solubility even in the absence of polar side chains is mainly due to the large dipole moment and enhanced flexibility of the conjugated backbone once the boron atom is embedded. The p-π* conjugation directly affects the electronic structure as the LUMO is fully delocalized, including the boron atom, whereas the HOMO has the boron atom residing on a node. As a result, the mol. exhibits low-lying LUMO/HOMO energy levels of -3.61 eV/-5.73 eV paired with a good electron mobility of 1.37 × 10^-5 cm² V^-1 s^-1. Its application as an electron acceptor is demonstrated in alc.-processed organic solar cells (OSCs). This p-π* conjugated mol. is the first alc.-processable non-fullerene electron acceptor, a feature that is in strong demand for environmentally friendly processing of OSCs.

Journal of Materials Chemistry C: Materials for Optical and Electronic Devices published new progress about 303734-52-3. 303734-52-3 belongs to bromides-buliding-blocks, auxiliary class Thiophene,Bromide, name is 2-Bromo-3-(2-ethylhexyl)thiophene, and the molecular formula is C13H16O2, Recommanded Product: 2-Bromo-3-(2-ethylhexyl)thiophene.

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

Zou, Hong Bin published the artcileDesign, synthesis, and SAR analysis of cytotoxic sinapyl alcohol derivatives, Synthetic Route of 76283-09-5, the publication is Bioorganic & Medicinal Chemistry (2006), 14(6), 2060-2071, database is CAplus and MEDLINE.

Five series totalling 51 of sinapyl alc. derivatives were designed and synthesized. Their cytotoxicity analyses were performed on six human tumor cell lines such as PC-3, CNE, KB, A549, BEL-7404, and HeLa. Certain sinapyl alc. derivatives showed significant cytotoxic activities. Compound I exhibited especially potent cytotoxicity against the BEL-7404 cell line with an IC₅₀ value of 0.7 μM, which showed more cytotoxic activity than the pos. control, cisplatin. The structure-cytotoxicity relationships were discussed and the CoMFA anal. was performed using the cytotoxic data against HeLa cells as a template.

Bioorganic & 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 C15H21BO2, Synthetic Route of 76283-09-5.

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

Mederski, WWKR published the artcileNovel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridines. Potent angiotensin II receptor antagonists with high affinity for both the AT₁ and AT₂ subtypes, Product Details of C7H5Br2F, the publication is European Journal of Medicinal Chemistry (1997), 32(6), 479-491, database is CAplus.

The synthesis and pharmacol. activity of balanced high affinity non-peptide angiotensin II antagonists of the AT₁ and AT₂ subtype receptors have been presented. A series of previously prepared AT₁ selective 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]-pyridines were modified at four different positions in order to increase the AT₂ binding affinity by maintaining the nanomolar activity for the AT₁ receptor. The targeted AT₂/AT₁ IC₅₀ binding ratio of ∼ 1 was achieved with a number of compounds possessing a small alkyl chain at C-2, different acetamide groups at N-5 and a 3-fluoro and 2′-carboxamidosulfonyl substituent at the biphenylmethyl moiety. These modifications led to an analog which exhibited an AT₂/AT₁ ratio of 0.74, a subnanomolar AT₁ antagonistic potency (0.18 nM) and a high metabolic stability in rat and monkey liver microsomes in vitro. After oral administration of 3 mg/kg to cynomolgus monkeys, EMD 90423 (potassium salt of the active analog) demonstrated good efficacy and a long duration of action as an antihypertensive agent.

European 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, Product Details of C7H5Br2F.

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

Wang, Jixin published the artcileSalt-Stabilized Silylzinc Pivalates for Nickel-Catalyzed Carbosilylation of Alkenes, Product Details of C7H5Br2F, the publication is Angewandte Chemie, International Edition (2022), 61(17), e202202379, database is CAplus and MEDLINE.

The authors herein report the preparation of solid and salt-stabilized silylzinc pivalates from the corresponding silyllithium reagents via transmetalation with Zn(OPiv)₂. These resulting organosilylzinc pivalates show enhanced air and moisture stability and unique reactivity in the silylative difunctionalization of alkenes. Thus, a practical chelation-assisted Ni-catalyzed regioselective alkyl and benzylsilylation of alkenes was developed, which provides an easy method to access alkyl silanes with broad substrate scope and wide functional group compatibility. Kinetic experiments highlight that the OPiv-coordination is crucial to improve the reactivity of silylzinc pivalates. Also, late-stage functionalizations of druglike mols. and versatile modifications of the products illustrate the synthetical utility of this protocol.

Angewandte Chemie, International Edition 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 C12H16N2O2, Product Details of C7H5Br2F.

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

Bielecki, Mia published the artcileA fluorescent glucose sensor binding covalently to all five hydroxy groups of α-D-glucofuranose. A reinvestigation, Synthetic Route of 166821-88-1, the publication is Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1999), 449-456, database is CAplus.

The structures of the complexes between a fluorescent bisboronic acid 7 and glucose have been determined Shinkai et al.¹ previously studied the complex between 7 and glucose and they deduced a 1,2:4,6-α-D-glucopyranose bisboronate structure. We have shown that this structure is only valid as an initial complex formed under completely nonaqueous conditions. In the presence of water the pyranose complex rearranges rapidly into an α-D-glucofuranose-1,2:3,5,6-bisboronate in which all five free hydroxy groups of glucose are covalently bound by the sensor mol. A favorable B-N interaction around the 1,2-binding site and the effect of an o-ammoniomethyl group on the pK_a value of the second boronic acid group allow for the observed binding at neutral pH. The structure evaluations are based on ¹H and ¹³C NMR data as well as information obtained from ¹J_CC coupling constants The fluorescence spectra of both complexes were measured and discussed. MALDI TOF-MS experiments showed competitive formation of 1:2 (boronic acid:glucose) complexes under conditions of physiol. glucose levels.

Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry published new progress about 166821-88-1. 166821-88-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzyl bromide,Benzene,Boronic Acids,Boronic acid and ester, name is 2-(2-(Bromomethyl)phenyl)-5,5-dimethyl-1,3,2-dioxaborinane, and the molecular formula is C12H16BBrO2, Synthetic Route of 166821-88-1.

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

Donzel, Maxime published the artcileBioinspired Photoredox Benzylation of Quinones, Product Details of C7H5Br2F, the publication is Journal of Organic Chemistry (2021), 86(15), 10055-10066, database is CAplus and MEDLINE.

3-Benzylmenadiones were obtained in good yield by using a blue-light-induced photoredox process in the presence of Fe(III), oxygen, and γ-terpinene acting as a hydrogen-atom transfer agent. This methodol. is compatible with a wide variety of diversely substituted 1,4-naphthoquinones as well as various cheap, readily available benzyl bromides with excellent functional group tolerance. The benzylation mechanism was investigated and supports a three-step radical cascade with the key involvement of the photogenerated superoxide anion radical.

Journal of Organic 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, Product Details of C7H5Br2F.

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

Alexiou, Polyxeni published the artcileA Diverse Series of Substituted Benzenesulfonamides as Aldose Reductase Inhibitors with Antioxidant Activity: Design, Synthesis, and in Vitro Activity, Synthetic Route of 76283-09-5, the publication is Journal of Medicinal Chemistry (2010), 53(21), 7756-7766, database is CAplus and MEDLINE.

Based on bioisosteric principles, 2,6-difluorophenol and tetrazole, methylsulfonylamide, and isoxazolidin-3-one phenylsulfonamide derivatives were synthesized and tested in vitro in protocols primarily related to the long-term diabetic complications. Most of the compounds were found as aldose reductase inhibitors (ARIs) at IC₅₀ < 100 μM, while the introduction of the 4-bromo-2-fluorobenzyl group in a phenylsulfonamidodifluorophenol structure resulted in I, presenting a submicromolar inhibitory profile. However, the derivatives of tetrazole, methylsulfonylamine, and the (R)-enantiomer of isoxazolidin-3-one did not exhibit appreciable aldose reductase inhibitors (ARI) activity. The selectivity of the active ARIs is also discussed. Furthermore, the synthesized compounds exhibit potent antioxidant potential (homogeneous and heterogeneous systems).

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, Synthetic Route of 76283-09-5.

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

Shi, Zhi-Cai published the artcileModulation of Peripheral Serotonin Levels by Novel Tryptophan Hydroxylase Inhibitors for the Potential Treatment of Functional Gastrointestinal Disorders, Category: bromides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2008), 51(13), 3684-3687, database is CAplus and MEDLINE.

The discovery of a novel class of peripheral tryptophan hydroxylase (TPH) inhibitors is described. This class of TPH inhibitors exhibits excellent potency in in vitro biochem. and cell-based assays, and it selectively reduces serotonin levels in the murine intestine after oral administration without affecting levels in the brain. These TPH1 inhibitors may provide novel treatments for gastrointestinal disorders associated with dysregulation of the serotonergic system, such as chemotherapy-induced emesis and irritable bowel syndrome.

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 C15H14Cl2S2, Category: bromides-buliding-blocks.

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

Uddin, Jamal Md. published the artcilePhotoinduced electron transfer quenching and sugar effects on the electrostatic interaction between an anionic Ru(II) complex and cationic bipyridinium derivatives functionalized with boronic acids, SDS of cas: 166821-88-1, the publication is Inorganica Chimica Acta (2012), 104-110, database is CAplus and MEDLINE.

The photoinduced electron transfer quenching of an anionic ruthenium(II) metal-ligand-complex (Ru(dpp(SO₃Na)))₂(mcbpy)Cl₂ by two boronic acid functionalized benzyl viologen (BV²⁺) derivatives has been investigated as well as their response to sugar. The electrostatic interaction between these two charge species lead to the formation of static quenching which is removed in presence of sugar due to the formation of a neutral zwitterionic quencher. Spectral data, quenching parameters and sugar titration curves are presented and discussed in term of future developments of optical sensors for sugar.

Inorganica Chimica Acta published new progress about 166821-88-1. 166821-88-1 belongs to bromides-buliding-blocks, auxiliary class Bromide,Boronic acid and ester,Benzyl bromide,Benzene,Boronic Acids,Boronic acid and ester, name is 2-(2-(Bromomethyl)phenyl)-5,5-dimethyl-1,3,2-dioxaborinane, and the molecular formula is C11H8O3, SDS of cas: 166821-88-1.

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