Author: tianli

Priebbenow, Daniel L. published the artcileDiscovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines, Safety of 3,3,3-Trifluoropropan-1-ol, the publication is Journal of Medicinal Chemistry (2021), 64(7), 4150-4162, database is CAplus and MEDLINE.

Novel 3,3′-disubstituted-5,5′-bi(1,2,4-triazine) compounds with potent in vitro activity against Plasmodium falciparum parasites were recently discovered. To improve the pharmacokinetic properties of the triazine derivatives, a new structure-activity relationship (SAR) investigation was initiated with a focus on enhancing the metabolic stability of lead compounds These efforts led to the identification of second-generation highly potent antimalarial bis-triazines, exemplified by triazine 23(I), which exhibited significantly improved in vitro metabolic stability (8 and 42μL/min/mg protein in human and mouse liver microsomes). The disubstituted triazine dimer 23 was also observed to suppress parasitemia in the Peters 4-day test with a mean ED₅₀ value of 1.85 mg/kg/day and exhibited a fast-killing profile, revealing a new class of orally available antimalarial compounds of considerable interest.

Journal of Medicinal Chemistry 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, Safety of 3,3,3-Trifluoropropan-1-ol.

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

Reddy, Kumbam Lingeshwar published the artcileMandelic acid appended chiral gels as efficient templates for multicolour circularly polarized luminescence, Application of 2-Hydroxy-2-phenylacetic acid, the publication is Nanoscale (2022), 14(13), 4946-4956, database is CAplus and MEDLINE.

Mandelic acid is a medicinally important chiral mol. that is widely used as a vital component in antibiotics, antiseptics and cosmetics. While the medicinal properties of mandelic acid are well known, its aggregation and gelation characteristics, which are crucial to finding applications as cosmetics and ointments, are least explored. We have designed and synthesized a pair of mandelic acid derivatives and investigated their aggregation properties in binary solvent mixtures The compounds undergo self-assembly through various noncovalent interactions, leading to the formation of robust chiral gels. Strong birefringence could be visualised from the individual structures constituting the gel. The large rod-like chiral structures are utilized as efficient templates for the assembly of ultra-small luminescent achiral carbon nanodots. The transfer of optical activity from the chiral host matrix to the fluorescent guest nanoparticles resulted in the generation of circularly polarized luminescence signals from the hybrid nanocomposites. The use of blue, green and red-emitting nanodots led to the fabrication of multicolor chiral light-emitting materials capable of covering the entire visible range. Considering the numerous medicinal benefits offered by mandelic acid and carbon nanodots, the materials constituting the nanocomposites, the distinct dimensions presented in the current work open new avenues for chiral light emitting materials to be used in biomedical research.

Nanoscale published new progress about 90-64-2. 90-64-2 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Alcohol,Natural product, name is 2-Hydroxy-2-phenylacetic acid, and the molecular formula is C8H8O3, Application of 2-Hydroxy-2-phenylacetic acid.

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

Hamaguchi, Wataru published the artcileDesign and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition, Category: alcohols-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry (2013), 21(24), 7612-7623, database is CAplus and MEDLINE.

A novel class of phosphodiesterase 10A (PDE10A) inhibitors with reduced CYP1A2 inhibition were designed and synthesized starting from 2-{[(1-phenyl-1H-benzimidazol-6-yl)oxy]methyl}quinoline I. Introduction of an iso-Pr group at the 2-position and a methoxy group at the 5-position of the benzimidazole ring of lead compound 1 resulted in the identification of 2-{[(2-isopropyl-5-methoxy-1-phenyl-1H-benzimidazol-6-yl)oxy]methyl}quinoline II, which exhibited potent PDE10A inhibitory activity with reduced CYP1A2 inhibitory activity compared to compound 1.

Bioorganic & Medicinal Chemistry published new progress about 120103-18-6. 120103-18-6 belongs to alcohols-buliding-blocks, auxiliary class Fluoride,Nitro Compound,Benzene,Phenol, name is 2,5-Difluoro-4-nitrophenol, and the molecular formula is C6H3F2NO3, Category: alcohols-buliding-blocks.

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

Serusi, Lorenzo published the artcileThe First Highly Enantioselective Synthesis of 3-Sulfinyl-Substituted Isoindolinones Having Adjacent Carbon and Sulfur Stereocenters, Application In Synthesis of 4410-99-5, the publication is Journal of Organic Chemistry (2021), 86(15), 10630-10639, database is CAplus and MEDLINE.

A highly stereoselective access to 3-sulfinyl-substituted isoindolinones was achieved by a tandem organocatalytic addition/cyclization reaction of 2-carbobenzyloxy-N-tosylbenzylidenimine with thiols and succeeding diastereoselective oxidation with MCPBA. First, enantioenriched isoindolinone N,S-acetals was obtained through a dynamic kinetic asym. transformation induced by a bifunctional chiral thiourea organocatalyst. In turn, the newly created carbon stereocenter enabled a high diastereocontrol in the subsequent sulfoxidation Based on DFT calculations, a theor. rationale for the stereoselectivity of the oxidation reaction was also provided.

Journal of Organic Chemistry published new progress about 4410-99-5. 4410-99-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Benzene, name is 2-Phenylethanethiol, and the molecular formula is C13H13N, Application In Synthesis of 4410-99-5.

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

Kanafusa, Sumiyo published the artcileInfluence of pulsed electric field-assisted dehydration on the volatile compounds of basil leaves, HPLC of Formula: 106-25-2, the publication is Innovative Food Science & Emerging Technologies (2022), 102979, database is CAplus.

Pulsed elec. field (PEF) was applied to basil leaves prior air drying at 40°C. The parameters of the elec. treatment were designed in such a way that (i) electroporated the tissue reversibly, provoking a permanent opening of the stomatal guard cells and (ii) electroporated the tissue irreversibly, damaging the cells. Treated leaves lost some volatile compounds due to both PEF treatments, probably related with the direct effect of permeabilization on the secretory cells of glandular trichomes. Upon drying, the irreversible permeabilization treatment showed the highest influence on the profile of volatiles in the dried leaves showing better retention of some terpenoids than the control. The performed statistical anal. allowed to select six compounds that can be used as markers both for the effect of pre-treatments prior dehydration and for the effects of dehydration itself on the volatile compounds of basil leaves.

Innovative Food Science & Emerging Technologies published new progress about 106-25-2. 106-25-2 belongs to alcohols-buliding-blocks, auxiliary class Natural product, name is cis-3,7-Dimethyl-2,6-Octadien-1-Ol, and the molecular formula is C10H18O, HPLC of Formula: 106-25-2.

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

Dave, H. N. published the artcileApplication of two advanced derivative spectrophotometric methods for simultaneous estimation of salbutamol sulphate, ambroxol hydrochloride and theophylline in pure and commercial formulations, Recommanded Product: trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, the publication is International Journal of Current Pharmaceutical Research (2022), 14(3), 33-38, database is CAplus.

Two advanced spectrophotometric methods have been proposed for the simultaneous determination of Salbutamol sulfate, Ambroxol hydrochloride and Theophylline in pure and pharmaceutical formulations. The proposed methods exclude the hectic steps of time-consuming sample preparations or purification or separation steps. There is no any spectrophotometric method has been avail for simultaneous estimation of the ternary mixture containing Salbutamol sulfate, Ambroxol hydrochloride and Theophylline. The methods are derivative ratio spectra zero-crossing method and double divisor ratio spectra derivative method resp. Both the methods are found to be rapid, accurate, precise, reliable and economical as well. The developed methods show best results in terms of linearity, accuracy, precision, limit of detection and limit of quantification for standard laboratory mixtures of pure drugs and marketed formulations. The range for Salbutamol sulfate, Ambroxol hydrochloride and Theophyllineare found to be 1-35μg ml^-1, 5-35μg ml^-1 and 6-60μg ml^-1 resp. For the derivative ratio spectra zero-crossing method, the values of the limit of detection are found to be 0.3161μg ml-1, 0.2212μg ml^-1 and 0.2910μg ml^-1 and the values limit of quantification are found to be 0.9571μg ml^-1, 0.7412μg ml^-1 and 0.9671μg ml^-1 for Salbutamol sulfate, Ambroxol hydrochloride and Theophylline resp. For double divisor ratio spectra derivative method, limit of detection values is found to be 0.3251μg ml^-1, 0.2591μg ml^-1 and 0.2640μg ml^-1 and the limit of quantification values are found to be 0.9870μg ml^-1, 0.8650μg ml^-1 and 0.8812μg ml^-1 for Salbutamol sulfate, Ambroxol hydrochloride and Theophylline resp. The common excipients and additives did not interfere in the determinations of any of the drugs while being analyzed for com. formulations. These two spectrophotometric methods, which determine SS, AH, and THE simultaneously, are simple, specific, accurate, precise, rapidly, and economically, indicating that they can be used routinely in pharmaceutical anal. As a result, derivative spectrophotometry may be used effectively for the simultaneous determination of SS, AH and THE in the combined dosage forms without any prior separation of individual drugs.

International Journal of Current Pharmaceutical Research published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Recommanded Product: trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride.

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

Hagen, Helen published the artcileAminoferrocene-Based Prodrugs Activated by Reactive Oxygen Species, COA of Formula: C14H21BO3, the publication is Journal of Medicinal Chemistry (2012), 55(2), 924-934, database is CAplus and MEDLINE.

Cancer cells generally generate higher amounts of reactive oxygen species than normal cells. On the basis of this difference, prodrugs have been developed (e.g., hydroxyferrocifen), which remain inactive in normal cells, but become activated in cancer cells. In this work we describe novel aminoferrocene-based prodrugs, which, in contrast to hydroxyferrocifen, after activation form not only quinone methides (QMs), but also catalysts (iron or ferrocenium ions). The released products act in a concerted fashion. In particular, QMs alkylate glutathione, thereby inhibiting the antioxidative system of the cell, whereas the iron species induce catalytic generation of hydroxyl radicals. Since the catalysts are formed as products of the activation reaction, it proceeds autocatalytically. The most potent prodrug described here is toxic toward cancer cells (human promyelocytic leukemia (HL-60), IC₅₀ = 9 μM, and human glioblastoma-astrocytoma (U373), IC₅₀ = 25 μM), but not toxic (up to 100 μM) toward representative nonmalignant cells (fibroblasts).

Journal of Medicinal Chemistry published new progress about 1370732-71-0. 1370732-71-0 belongs to alcohols-buliding-blocks, auxiliary class Boronic acid and ester, name is (3-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanol, and the molecular formula is C14H21BO3, COA of Formula: C14H21BO3.

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

Symmons, M F published the artcileDynamic properties of nucleated microtubules: GTP utilisation in the subcritical concentration regime., Application of Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is Journal of cell science (1996), 2755-66, database is MEDLINE.

Microtubule assembly kinetics have been studied quantitatively under solution conditions supporting microtubule dynamic instability. Purified GTP-tubulin (Tu-GTP) and covalently cross-linked short microtubule seeds (EGS-seeds; Koshland et al. (1988) Nature 331, 499) were used with and without biotinylation. Under sub-critical concentration conditions ([Tu-GTP] < 5.3 microM), significant microtubule growth of limited length was observed on a proportion of the EGS-seeds by immuno-electron microscopy. A sensitive fluorescence assay for microtubule GDP production was developed for parallel assessment of GTP utilisation. This revealed a correlation between the detected microtubule growth and the production of tubulin-GDP, deriving from the shortening phase of the dynamic microtubules. This correlation was confirmed by the action of nocodazole, a specific inhibitor of microtubule assembly, that was found to abolish the GDP release. The variation of the GDP release with tubulin concentration (Jh(c) plot) was determined below the critical concentration (Cc). The GDP production observed was consistent with the elongation of the observed seeded microtubules with an apparent rate constant of 1.5 x 10(6) M-1 second-1 above a threshold of approximately 1 microM tubulin. The form of this Jh(c) plot for elongation below Cc is reproduced by the Lateral Cap model for microtubule dynamic instability adapted for seeded assembly. The behaviour of the system is contrasted with that previously studied in the absence of detectable microtubule elongation (Caplow and Shanks (1990) J. Biol. Chem. 265, 8935-8941). The approach provides a means of monitoring microtubule dynamics at concentrations inaccessible to optical microscopy, and shows that essentially the same dynamic mechanisms apply at all concentrations. Numerical simulation of the subcritical concentration regime shows dynamic growth features applicable to the initiation of microtubule growth in vivo.

Journal of cell science 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 0, Application of Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.

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

Foister, Shane published the artcileShape selective recognition of T·A base pairs by hairpin polyamides containing N-terminal 3-methoxy (and 3-chloro) thiophene residues, COA of Formula: C4H4OS, the publication is Bioorganic & Medicinal Chemistry (2003), 11(20), 4333-4340, database is CAplus and MEDLINE.

Hairpin polyamides selectively recognize predetermined DNA sequences with affinities comparable to naturally occurring proteins. Internal side-by-side pairs of unsym. aromatic rings within the minor groove of DNA distinguish each of the four Watson-Crick base pairs. In contrast, N-terminal ring pairs exhibit less specificity, with the exception of Im/Py targeting G·C base pairs. In an effort to explore the sequence specificity of new ring pairs, a series of hairpin polyamides containing 3-substituted-thiophene-2-carboxamide residues at the N-terminus was synthesized. An N-terminal 3-methoxy (or 3-chloro) thiophene residue paired opposite Py displayed 6- (and 3-) fold selectivity for T·A relative to A·T base pair, while disfavoring G·C base pairs by >200-fold. Our data suggests shape selective recognition with projection of the 3-thiophene substituent (methoxy or chloro) to the floor of the minor groove.

Bioorganic & Medicinal Chemistry published new progress about 17236-59-8. 17236-59-8 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Alcohol, name is Thiophen-3-ol, and the molecular formula is C4H4OS, COA of Formula: C4H4OS.

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

Swierczewski, Michal published the artcileDeposition of Extended Ordered Ultrathin Films of Au₃₈(SC₂H₄Ph)₂₄ Nanocluster using Langmuir-Blodgett Technique, Recommanded Product: 2-Phenylethanethiol, the publication is Small (2021), 17(27), 2005954, database is CAplus and MEDLINE.

Langmuir-Blodgett technique is utilized to deposit ultrathin films of Au₃₈(SC₂H₄Ph)₂₄ nanocluster onto solid surfaces such as mica and silicon. The morphologies of the films transferred at various surface pressures within the mono/bi/trilayer regime are studied by at. force microscopy (AFM). The time spent on the water surface before the deposition has a decisive effect on the final ordering of nanoclusters within the network and is studied by fast AFM, X-ray reflectivity, and grazing-incidence wide-angle X-ray scattering.

Small published new progress about 4410-99-5. 4410-99-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Benzene, name is 2-Phenylethanethiol, and the molecular formula is C11H8O3, Recommanded Product: 2-Phenylethanethiol.

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