Alcohols-buliding-blocks

Pardeshi, Chandrakantsing V. published the artcileMannose-anchored N,N,N-trimethyl chitosan nanoparticles for pulmonary administration of etofylline, Synthetic Route of 96345-79-8, the publication is International Journal of Biological Macromolecules (2020), 165(Part_A), 445-459, database is CAplus and MEDLINE.

Drug delivery to lungs via pulmonary administration offers potential for the development of new drug delivery systems. Here we fabricated the etofylline (ETO) encapsulated mannose-anchored N,N,N-tri-Me chitosan nanoparticles (Mn-TMC NPs). The prominent characteristics like biocompatibility, controlled release, targeted delivery, high penetrability, enhanced phys. stability, and scalability mark Mn-TMC NPs as a viable alternative to various nanoplatform technologies for effective drug delivery. Mannosylation of TMC NPs leads to the evolution of new drug delivery vehicle with gratifying characteristics, and potential benefits in efficient drug therapy. It is widely accepted that following pulmonary administration, the introduction of mannose to the surface of drug nanocarriers provide selective macrophage targeting via receptor-mediated endocytosis. The fabricated Mn-TMC NPs exhibited particle size of 223.3 nm, PDI 0.490, and ζ-potential -19.1 mV, drug-loading capacity 76.26 ± 1.2%, and encapsulation efficiency of 91.75 ± 0.88%. Sustained drug release, biodegradation studies, stability, safety, and aerodynamic behavior revealed the effectiveness of prepared nanoformulation for pulmonary administration. In addition, the in vivo pharmacokinetic studies in Wistar rat model revealed a significant improvement in therapeutic efficacy of ETO, illustrating mannosylation a promising approach for efficient therapy of airway diseases following pulmonary administration.

International Journal of Biological Macromolecules published new progress about 96345-79-8. 96345-79-8 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Gal and Man, name is (2R,3S,4S,5S,6R)-2-(Hydroxymethyl)-6-(4-isothiocyanatophenoxy)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C13H15NO6S, Synthetic Route of 96345-79-8.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Stauber, Gregory B. published the artcileCharacterization and affinity cross-linking of receptors for human recombinant lymphotoxin (tumor necrosis factor-β) on a human histiocytic lymphoma cell line, U-937, COA of Formula: C18H20N2O12, the publication is Journal of Biological Chemistry (1989), 264(6), 3573-6, database is CAplus and MEDLINE.

Recombinant human lymphotoxin (rhLT) was purified and used to examine its receptors on the human histiocytic lymphoma cell line U-937. The rhLT was radioiodinated by the IODO GEN method to a specific activity of 60 μCi/μg. The specific binding reached a plateau within 10, 60, and 180 min at 37, 23, and 4°, resp. Scatchard anal. revealed the presence of a single class of high affinity receptors with an apparent K_d of 0.6 nm and a capacity of 33,000 binding sites/cell. The binding of ¹²⁵I-labeled rhLT to U-937 cells was inhibited by excess unlabeled rhLT or recombinant human tumor necrosis factor-α(rhTNF), suggesting a common receptor for both mols. The crosslinking of the receptor to rhLT revealed 2 distinct bands at approx. mol. masses of 100,000 and 120,000 daltons. Affinity crosslinking of U-937 cells with ¹²⁵I-labeled rhTNF, however, provided only a single band with a mol. mass of about 100,000 daltons. Thus, the manner in which rhLT interacts with its receptor is perhaps somewhat different from that of rhTNF.

Journal of Biological Chemistry published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C16H25BO2, COA of Formula: C18H20N2O12.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Higuchi, Masahiro published the artcileModulation of two forms of tumor necrosis factor receptors and their cellular response by soluble receptors and their monoclonal antibodies, Formula: C18H20N2O12, the publication is Journal of Biological Chemistry (1992), 267(29), 20892-9, database is CAplus and MEDLINE.

Recently, two different receptors for human tumor necrosis factor (TNF) with mol. masses of 60 kDa (p60) and 80 kDa (p80) have been identified. This report investigated the effect of the soluble forms of these receptors and monoclonal antibodies against them on ligand interaction, receptor down-regulation, and mediation of cellular response in U-937 cells. The results indicate that p60 and p80 constitute 20-30 and 60-80% of the total TNF-binding sites on U-937 cells, resp. However, by crosslinking, only the p80 form of the receptor could be detected. In contrast to unlabeled TNF, the anti-p60 and anti-p80 antibodies together only partially inhibited ligand binding, and this inhibition was not additive. Lack of additive inhibition of binding was not due to stereochem. hindrance. TNF binding to cells can be completely displaced by soluble forms of either the p60 or p80 receptor. However, 100-fold more of the p80 than the p60 form of the soluble receptor is needed for equivalent displacement. Under optimum conditions, TNF and the anti-p80 and anti-p60 antibodies down-regulated 30, 80, and 20% of the TNF receptors, resp. The anti-p60 and anti-p80 antibodies down-regulated not only their own receptors, but also reciprocal receptors, suggesting a cross-communication between the p60 and p80 forms of the TNF receptor. In spite of inhibiting as much as 80% of TNF binding, none of the receptor antibodies significantly inhibited the cytotoxic response to TNF in U-937 cells. Soluble forms of both receptors, however, completely abrogated the cellular response to TNF. Thus, these results indicate that the antibodies against both receptors together inhibit the majority of the receptor-ligand interaction without any significant effect on the biol. response to TNF.

Journal of Biological Chemistry published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Formula: C18H20N2O12.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Pawle, Robert H. published the artcileBandgap Engineering of Conjugated Materials with Nonconjugated Side Chains, Related Products of alcohols-buliding-blocks, the publication is Macromolecules (Washington, DC, United States) (2014), 47(7), 2250-2256, database is CAplus.

Controlling the optical properties of conjugated materials, especially their bandgaps, is critical to nearly all of applications of these materials. The most prevalent strategy involves changes to the structures of conjugated backbones, while side chains are generally reserved for imparting solubility This paper, using a series of donor-acceptor conjugated oligo- and poly(arylene-ethynylene)s that have terephthalate units as the electron-deficient unit, demonstrates examples of how the structures of side chains that are not formally part of the conjugated backbone can have significant effects on bandgaps of these materials. In organic solution, changing alkoxy substituents on the terephthalate unit yields changes in absorbance onsets of, in some cases, greater than 20 nm; the position of absorbance spectra of these materials correlates with the Taft σ* values of the ester alkoxy groups, consistent with the side chains inductively altering the electron-accepting nature of the terephthalate ring. This structure-property relationship persists in the solid state. These results indicate that synthetically simple side-chain substitutions of formally nonconjugated groups may be useful in rational design of the optoelectronic properties of conjugated materials in both solution and the solid state.

Macromolecules (Washington, DC, United States) published new progress about 2240-88-2. 2240-88-2 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Aliphatic hydrocarbon chain,Alcohol, name is 3,3,3-Trifluoropropan-1-ol, and the molecular formula is C3H5F3O, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Bottari, Giovanni published the artcileSynthesis of Enantioenriched Amines by Iron-Catalysed Amination of Alcohols Employing at Least One Achiral Substrate, Application In Synthesis of 111-29-5, the publication is Advanced Synthesis & Catalysis (2021), 363(24), 5436-5442, database is CAplus.

The synthesis of a broad range of enantioenriched amines by the direct Fe-catalyzed coupling of amines with alcs. through the borrowing hydrogen strategy, while at least one of these substrates was achiral is reported. When starting from α-chiral amines and achiral alcs., a wide range of enantioenriched amine products, including N-heterocyclic moieties was obtained with complete retention of stereochem.. The power of this method was demonstrated in the one-step synthesis of known pharmaceuticals from com. available, simple enantiopure primary amines and achiral alcs. It was also found that the use of β-branched enantioenriched primary alcs. and achiral amines as reaction partners leads to a partial loss of stereochem. integrity in the final product, however, a systematic optimization enabled partial retention of enantiopurity and possible parameters effecting for racemization were identified.

Advanced Synthesis & Catalysis published new progress about 111-29-5. 111-29-5 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Alcohol,Ploymers, name is Pentane-1,5-diol, and the molecular formula is C5H12O2, Application In Synthesis of 111-29-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Leal, Emilse S. published the artcileDe novo design approaches targeting an envelope protein pocket to identify small molecules against dengue virus, Related Products of alcohols-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2019), 111628, database is CAplus and MEDLINE.

Dengue fever is a mosquito-borne viral disease that has become a major public health concern worldwide. This disease presents with a wide range of clin. manifestations, from a mild cold-like illness to the more serious hemorrhagic dengue fever and dengue shock syndrome. Currently, neither an approved drug nor an effective vaccine for the treatment are available to fight the disease. The envelope protein (E) is a major component of the virion surface. This protein plays a key role during the viral entry process, constituting an attractive target for the development of antiviral drugs. The crystal structure of the E protein reveals the existence of a hydrophobic pocket occupied by the detergent n-octyl-β-d-glucoside (β-OG). This pocket lies at the hinge region between domains I and II and is important for the low pH-triggered conformational rearrangement required for the fusion of the virion with the host’s cell. Aiming at the design of novel mols. which bind to E and act as virus entry inhibitors, we undertook a de novo design approach by “growing” mols. inside the hydrophobic site (β-OG). From more than 240000 small-mols. generated, the 2,4 pyrimidine scaffold was selected as the best candidate, from which one synthesized compound displayed micromolar activity. Mol. dynamics-based optimization was performed on this hit, and thirty derivatives were designed in silico, synthesized and evaluated on their capacity to inhibit dengue virus entry into the host cell. Four compounds were found to be potent antiviral compounds in the low-micromolar range. The assessment of drug-like physicochem. and in vitro pharmacokinetic properties revealed that compounds 3e and 3h presented acceptable solubility values and were stable in mouse plasma, simulated gastric fluid, simulated intestinal fluid, and phosphate buffered saline solution pyrimidine.

European Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Kirkland, Thomas A. published the artcileSynthesis of glutamic acid analogs as potent inhibitors of leukotriene A₄ hydrolase, Application of 4-(1H-Pyrrol-1-yl)phenol, the publication is Bioorganic & Medicinal Chemistry (2008), 16(9), 4963-4983, database is CAplus and MEDLINE.

Leukotriene B₄ (LTB₄) is a potent pro-inflammatory mediator that has been implicated in the pathogenesis of multiple diseases, including psoriasis, inflammatory bowel disease, multiple sclerosis and asthma. As a method to decrease the level of LTB₄ and possibly identify novel treatments, inhibitors of the LTB₄ biosynthetic enzyme, leukotriene A₄ hydrolase (LTA₄-h), have been explored. Here, the authors describe the discovery of a potent inhibitor of LTA₄-h, arylamide of glutamic acid derivative I, starting from Boc-Glu[NHC₆H₄(OCH₂Ph)-4]-OH. Analogs of I are then described, focusing on compounds that are both active and stable in whole blood. This effort culminated in the identification of amino alc. II and amino ester III which meet these criteria.

Bioorganic & Medicinal Chemistry published new progress about 23351-09-9. 23351-09-9 belongs to alcohols-buliding-blocks, auxiliary class Pyrrole,Benzene,Alcohol, name is 4-(1H-Pyrrol-1-yl)phenol, and the molecular formula is C10H9NO, Application of 4-(1H-Pyrrol-1-yl)phenol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Pillow, Thomas H. published the artcileAntibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity, Application of 2-Methyl-2-sulfanylpropan-1-ol, the publication is ChemMedChem (2020), 15(1), 17-25, database is CAplus and MEDLINE.

The ability to selectively degrade proteins with bifunctional small mols. has the potential to fundamentally alter therapy in a variety of diseases. However, the relatively large size of these chimeric mols. often results in challenging physico-chem. properties (e. g., low aqueous solubility) and poor pharmacokinetics which may complicate their in vivo applications. We recently discovered an exquisitely potent chimeric BET degrader (GNE-987) which exhibited picomolar cell potencies but also demonstrated low in vivo exposures. In an effort to improve the pharmacokinetic properties of this mol., we discovered the first degrader-antibody conjugate by attaching GNE-987 to an anti-CLL1 antibody via a novel linker. A single IV dose of the conjugate afforded sustained in vivo exposures that resulted in antigen-specific tumor regressions. Enhancement of a chimeric protein degrader with poor in vivo properties through antibody conjugation thereby expands the utility of directed protein degradation as both a biol. tool and a therapeutic possibility.

ChemMedChem published new progress about 73303-88-5. 73303-88-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Alcohol, name is 2-Methyl-2-sulfanylpropan-1-ol, and the molecular formula is C4H10OS, Application of 2-Methyl-2-sulfanylpropan-1-ol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Patel, Grishma H. published the artcileRp-hplc method development and validation for simultaneous estimation of efonidipine hydrochloride ethanolate and telmisartan in their synthetic mixture, Recommanded Product: 2-(Benzyl(phenyl)amino)ethyl 5-(5,5-dimethyl-2-oxido-1,3,2-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate ethanol hydrochloride, the publication is International Journal of Pharmaceutics and Drug Analysis (2021), 9(3), 190-195, database is CAplus.

A Novel, selective, accurate and rapid Reversed Phase High Performance Liquid Chromatog. (RPHPLC) method for the anal. of Efonidipine Hydrochloride Ethanolate and Telmisartan in binary mixture has been developed and validated. The chromatog. system consisted of a Phenomenex Kinetex 5μ C18 Size: 150 * 4.6mm column and the separation was achieved by using ambient temperature with a mobile phase containing mobile Phase Acetonitrile:25mM Phosphate Buffer pH 4.9 (45:55). The samples were monitored at 253 nm for detection at a flow rate of 1.0 mL/min and the retention time was about 7.77 and 4.10 mins for Efonidipine Hydrochloride Ehanolate and Telmisartan resp. The calibration curve was linear over the concentration range 5-30 and 10-60μg/mL for Efonidipine Hydrochloride Ehanolate and Telmisartan resp. The proposed method is accurate in the range of 99.75% – 100.10% recovery and precise (%RSD of intraday variation and % RSD of inter day variation were found to be within the acceptance criteria). Therefore, this method can be used as a more convenient and efficient option for the anal. of Efonidipine Hydrochloride Ehanolate and Telmisartan in Quality control laboratory

International Journal of Pharmaceutics and Drug Analysis published new progress about 111011-76-8. 111011-76-8 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is 2-(Benzyl(phenyl)amino)ethyl 5-(5,5-dimethyl-2-oxido-1,3,2-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate ethanol hydrochloride, and the molecular formula is C36H45ClN3O8P, Recommanded Product: 2-(Benzyl(phenyl)amino)ethyl 5-(5,5-dimethyl-2-oxido-1,3,2-dioxaphosphinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate ethanol hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Basu Baul, Tushar S. published the artcileSynthesis and structural characterization of diorganotin(IV) complexes with heteroditopic pyridyl-ONO’-ligands, Application In Synthesis of 96-20-8, the publication is Inorganica Chimica Acta (2020), 119892, database is CAplus.

A series of eight novel diorganotin(IV) complexes with heteroditopic pyridyl-ONO’-ligands were prepared viz., [Me₂Sn(L¹)]₂·2(H₂O) (1), [n-Bu₂Sn(L¹)]₂ (2), [Ph₂Sn(L¹)] (3), [Me₂Sn(L²)]₂·2(H₂L²) (4), [n-Bu₂Sn(L²)]₂ (5), [Ph₂Sn(L²)]·0.5(C₆H₆) (6), [Me₂Sn(L³)]₂ (7) and [n-Bu₂Sn(L³)]₂ (8) and structurally characterized. Irresp. of the type of diazo L ligand, the dimethyl- and di-n-butyltin(IV) compounds are dinuclear species with an inversion center in the middle of the {Sn₂O₂} cores affording metals with coordination number six. The mononuclear compounds 3 and 6, with the bulky Ph ligands, present the tin cations with highly distorted square pyramid geometries. The detection of a conformation in the (Lⁿ)^2- ligand in the solid state structures of 3, 4 and 8 which is different from the one in the remaining compounds suggests that the packing of the mols. conceivably have a greater influence than the imine substituents or the metal co-ligands. The solution ¹H and ¹³C NMR of compounds 4–6 displayed an anisochronous behavior of dimethyl-, di-n-butyl- and diphenyltin parts while those of compounds 1–3 are isochronous. The ¹¹⁹Sn NMR chem. shift displacements of all the compounds are indicative of five-coordinate tin atoms, thus revealing dissociation in solution of the dinuclear 1, 2, 4, 5, 7 and 8 complexes.

Inorganica Chimica Acta published new progress about 96-20-8. 96-20-8 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Alcohol, name is 2-Aminobutan-1-ol, and the molecular formula is C4H11NO, Application In Synthesis of 96-20-8.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts