Tag: M.W=200-250

Saheb Sharif-Askari, Narjes published the artcileEffect of common medications on the expression of SARS-CoV-2 entry receptors in kidney tissue, Formula: C12H15ClO3, the publication is Clinical and Translational Science (2020), 13(6), 1048-1054, database is CAplus and MEDLINE.

Besides the respiratory system, severe acute respiratory syndrome-coronavirus 2 (SARS-CoV-2) infection was shown to affect other essential organs such as the kidneys. Early kidney involvement during the course of infection was associated with worse outcomes, which could be attributed to the direct SARS-CoV-2 infection of kidney cells. In this study, the effect of commonly used medications on the expression of SARS-CoV-2 receptor, angiotensin-converting enzyme (ACE)2, and TMPRSS2 protein in kidney tissues was evaluated. This was done by in silico analyses of publicly available transcriptomic databases of kidney tissues of rats treated with multiple doses of commonly used medications. Of 59 tested medications, 56% modified ACE2 expression, whereas 24% modified TMPRSS2 expression. ACE2 was increased with only a few of the tested medication groups, namely the renin-angiotensin inhibitors, such as enalapril, antibacterial agents, such as nitrofurantoin, and the proton pump inhibitor, omeprazole. The majority of the other medications decreased ACE2 expression to variable degrees with allopurinol and cisplatin causing the most noticeable downregulation. The expression level of TMPRSS2 was increased with a number of medications, such as diclofenac, furosemide, and dexamethasone, whereas other medications, such as allopurinol, suppressed the expression of this gene. The prolonged exposure to combinations of these medications could regulate the expression of ACE2 and TMPRSS2 in a way that may affect kidney susceptibility to SARS-CoV-2 infection. Data presented here suggest that the authors should be vigilant about the potential effects of commonly used medications on kidney tissue expression of ACE2 and TMPRSS2.

Clinical and Translational Science published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, Formula: C12H15ClO3.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Yoshida, Masahito published the artcileStructure-activity relationship study on Col-003, a protein-protein interaction inhibitor between collagen and Hsp47, Recommanded Product: 5-Bromo-3-chloro-2-hydroxybenzaldehyde, the publication is Chemical & Pharmaceutical Bulletin (2020), 68(3), 220-226, database is CAplus and MEDLINE.

This study demonstrates the structure-activity relationship of Col-003, a potent collagen-heat-shock protein 47 (Hsp47) interaction inhibitor. Col-003 analogs were successfully synthesized by Pd(0)-catalyzed cross-coupling reactions of 5-bromosalicylaldehyde derivatives with alkyl-metal species, and the inhibitory activities of the synthetic analogs were evaluated using surface plasmon resonance anal. (BIAcore). We succeeded in discovering two potent inhibitors that showed 85 and 81% inhibition at a concentration of 1.9μM against the collagen-Hsp47 interaction. This indicates that elongation of an alkyl linker between two aromatic rings could considerably improve inhibitory activity due to the adjustment of a pendant Ph moiety to an appropriate position, in addition to the hydrophobic interaction with an alkyl linker moiety.

Chemical & Pharmaceutical Bulletin published new progress about 19652-33-6. 19652-33-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Phenol,Aldehyde, name is 5-Bromo-3-chloro-2-hydroxybenzaldehyde, and the molecular formula is C4H10O2, Recommanded Product: 5-Bromo-3-chloro-2-hydroxybenzaldehyde.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Rode, Milind A. published the artcileSynthesis and biological activities of some indoline derivatives, Category: chlorides-buliding-blocks, the publication is Journal of the Serbian Chemical Society (2009), 74(12), 1377-1387, database is CAplus.

The reaction of indoline with a substituted benzoyl chloride in the presence of K₂CO₃ in THF gave 1-aroyl-2,3-dihydro-1H-indole I. The latter was subjected to chlorosulfonation in position 5. Condensation of the latter with aromatic amines led 1-aroyl-2,3-dihydro-1H-indole-5-sulfonamides. Similarly, 5-nitroindoline was treated with a substituted benzoyl chloride to obtain the nitro compound II, which was reduced using stannous chloride and reacted further with aromatic sulfonyl chloride to obtain the N-[1-aroyl-2,3-dihydro-1H-indol-5-yl]sulfonamides. These compounds were tested for antibacterial, tuberculostatic, and antifungal activity. Some of them showed very good activity against some gram-pos. and gram neg. bacteria, fungal strains, and also Mycobacterium tuberculosis. All of the synthesized compounds were subjected to antioxidant activity testing using the in vitro DPPH assay, and most of them showed very good activity.

Journal of the Serbian Chemical Society published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, Category: chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Vicentini, Chiara Beatrice published the artcilePyrazolo[3,4-c]isothiazole and isothiazolo[4,3-d]isoxazole derivatives as antifungal agents, Application In Synthesis of 1869-22-3, the publication is Pharmaceutical Biology (London, United Kingdom) (2011), 49(5), 545-552, database is CAplus and MEDLINE.

Fungal diseases due to zoopathogenic fungi and phytopathogenic fungi are increasing and among the substances used to combat fungi, azoles are of primary interest, both in agricultural fields and health and to void fungal resistance phenomena, the synthesis and tests of new derivatives are necessary. This article discusses the preparation and antifungal activity of pyrazolo[3,4-c]isothiazole and isothiazolo[4,3-d]isoxazole derivatives against three pathogenic fungi for plants and two opportunistic fungi in humans and plants. The synthesis of the target compounds [i.e., 6-[2-chloro-5-(trifluoromethyl)phenyl]-4-methyl-6H-pyrazolo[3,4-c]isothiazol-3-amine, 6-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]-4-methyl-6H-pyrazolo[3,4-c]isothiazol-3-amine] was achieved using 2-cyano-3-ethoxy-2-butenethioamide as a starting material. The title compounds were evaluated against Magnaporthe grisea (phytopathogenic fungi), Pythium ultimum, Sclerotinia minor, Fusarium moniliforme (opportunistic strain ATCC 36541) and Trichoderma viride (opportunistic strain) and it was discovered that the fungi were sensitive toward the different azole-derivatives In general Magnaporthe grisea (T.T. Hebert Yaegashi & Udagawa) was the most sensitive fungus, being blocked almost entirely by a 4-chlorophenyl derivative [6-(4-chlorophenyl)-4-methyl-6H-pyrazolo[3,4-c]isothiazol-3-amine] even at 20 μμg/mL, a concentration at which the reference com. compound Tricyclazole was nearly ineffective. These findings demonstrate that the pyrazolo[3,4-c]isothiazole derivatives have a wide spectrum of activity on phytopathogenic and opportunistic fungi. In particular the 4-chloro derivative seems to have a great potential as new product to combat M. grisea in the agricultural field.

Pharmaceutical Biology (London, United Kingdom) published new progress about 1869-22-3. 1869-22-3 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Hydrazine,Amine,Benzene, name is 1-(2-Chloro-5-(trifluoromethyl)phenyl)hydrazine, and the molecular formula is C10H11NO4, Application In Synthesis of 1869-22-3.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Eidam, Oliv published the artcileFragment-guided design of subnanomolar β-lactamase inhibitors active in vivo, Application of 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, the publication is Proceedings of the National Academy of Sciences of the United States of America (2012), 109(43), 17448-17453, S17448/1-S17448/39, database is CAplus and MEDLINE.

Fragment-based design was used to guide derivatization of a lead series of β-lactamase inhibitors that had heretofore resisted optimization for in vivo activity. X-ray structures of fragments overlaid with the lead suggested new, unanticipated functionality and points of attachment. Synthesis of three derivatives improved affinity over 20-fold and improved efficacy in cell culture. Crystal structures were consistent with the fragment-based design, enabling further optimization to a K_i of 50 pM, a 500-fold improvement that required the synthesis of only six derivatives One of these, compound 5, was tested in mice. Whereas cefotaxime alone failed to cure mice infected with β-lactamase-expressing Escherichia coli, 65% were cleared of infection when treated with a cefotaxime:5 combination. Fragment complexes offer a path around design hurdles, even for advanced mols.; the series described here may provide leads to overcome β-lactamase-based resistance, a key clin. challenge.

Proceedings of the National Academy of Sciences of the United States of America published new progress about 254749-11-6. 254749-11-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Benzene, name is 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, and the molecular formula is C7H3Cl2NO2S, Application of 2-Chloro-4-cyanobenzene-1-sulfonyl chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kamdem, Nestor published the artcileSmall-molecule inhibitors of the PDZ domain of Dishevelled proteins interrupt Wnt signalling, Computed Properties of 61551-49-3, the publication is Magnetic Resonance (2021), 2(1), 355-374, database is CAplus.

Dishevelled (Dvl) proteins are important regulators of the Wnt signalling pathway, interacting through their PDZ domains with the Wnt receptor Frizzled. Blocking the Dvl PDZ-Frizzled interaction represents a potential approach for cancer treatment, which stimulated the identification of small-mol. inhibitors, among them the anti-inflammatory drug Sulindac and Ky-02327. Aiming to develop tighter binding compounds without side effects, we investigated structure-activity relationships of sulfonamides. X-ray crystallog. showed high complementarity of anthranilic acid derivatives in the GLGF loop cavity and space for ligand growth toward the PDZ surface. Our best binding compound inhibits Wnt signalling in a dose-dependent manner as demonstrated by TOP-GFP assays (IC50 ∼ 50 μM) and Western blotting of β-catenin levels. Realtime PCR showed reduction in the expression of Wnt-specific genes. Our compound interacted with Dvl-1 PDZ (KD = 2.4 μM) stronger than Ky-02327 and may be developed into a lead compound interfering with the Wnt pathway.

Magnetic Resonance published new progress about 61551-49-3. 61551-49-3 belongs to chlorides-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 5,6,7,8-Tetrahydronaphthalene-2-sulfonyl chloride, and the molecular formula is C10H11ClO2S, Computed Properties of 61551-49-3.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Los, Johannes published the artcileHydrolytic dissociation constants of substituted 4-aminobenzoic acids, SDS of cas: 5204-46-6, the publication is Recueil des Travaux Chimiques des Pays-Bas (1967), 86(6), 609-21, database is CAplus.

The 4 individual pK values for 4-aminobenzoic acid, the following acids of the general formula 2,6,4-X(Y)(H2N)C6H2CO2H (X and Y given): H, Me; H, Cl; H, Br; H, NO2; H, OH; H, MeO; Me, Me; Et, Et; Cl, Cl; Br, Br; and 3,4-Br(H2N)C6H3CO2H are calculated from the pKI and pKII values. The hydrolytic dissociation constants, KI and KII, are determined in aqueous solutions at 50°. The effect of the CO2H group on the NH3+ → NH2 dissociation is discussed; large ΔpK1′ values are obtained for most of the acids. The effect of the CO2- group on the NH3+ → NH2 dissociation and mesomeric stabilization by CO2H and CO2- are also discussed.

Recueil des Travaux Chimiques des Pays-Bas published new progress about 5204-46-6. 5204-46-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Amine,Benzene, name is 4-Amino-2,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, SDS of cas: 5204-46-6.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Ghosh, Soumen published the artcileHFIP-Assisted Single C-F Bond Activation of Trifluoromethyl Ketones using Visible-Light Photoredox Catalysis, HPLC of Formula: 5860-95-7, the publication is Angewandte Chemie, International Edition (2022), 61(9), e202115272, database is CAplus and MEDLINE.

A visible light photoredox catalytic method for the selective cleavage of single strong C-F bond in trifluoromethyl ketones was reported. Single electron reduction of trifluoromethyl ketones generates difluoromethyl radicals which was engaged in intermol. C-C bond formation with N-methyl-N-arylmethacrylamides to furnish fluorine-containing oxindole derivatives in good yields. The reaction shows excellent chemoselectivity with good functional group tolerance under mild conditions. 1,1,1,3,3,3-Hexafluoroisopropanol (HFIP) as a solvent plays a critical role for the selective single C-F bond cleavage. High-level DFT calculations are depicted to shed light on the mechanism.

Angewandte Chemie, International Edition published new progress about 5860-95-7. 5860-95-7 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Benzene,Ketone, name is 1-(2-Chlorophenyl)-2,2,2-trifluoroethanone, and the molecular formula is C8H4ClF3O, HPLC of Formula: 5860-95-7.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Toledo-Sherman, Leticia M. published the artcileDevelopment of a Series of Aryl Pyrimidine Kynurenine Monooxygenase Inhibitors as Potential Therapeutic Agents for the Treatment of Huntington’s Disease, Name: 3-Chloro-4-isopropoxyphenylboronic acid, the publication is Journal of Medicinal Chemistry (2015), 58(3), 1159-1183, database is CAplus and MEDLINE.

We report on the development of a series of pyrimidine carboxylic acids that are potent and selective inhibitors of kynurenine monooxygenase and competitive for kynurenine. We describe the SAR for this novel series and report on their inhibition of KMO activity in biochem. and cellular assays and their selectivity against other kynurenine pathway enzymes. We describe the optimization process that led to the identification of a program lead compound with a suitable ADME/PK profile for therapeutic development. We demonstrate that systemic inhibition of KMO in vivo with this lead compound provides pharmacodynamic evidence for modulation of kynurenine pathway metabolites both in the periphery and in the central nervous system.

Journal of Medicinal Chemistry published new progress about 480438-56-0. 480438-56-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C8H19NO, Name: 3-Chloro-4-isopropoxyphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Seth, Kapileswar published the artcileCooperative Catalysis by Palladium-Nickel Binary Nanocluster for Suzuki-Miyaura Reaction of Ortho-Heterocycle-Tethered Sterically Hindered Aryl Bromides, SDS of cas: 480438-56-0, the publication is Organic Letters (2014), 16(9), 2334-2337, database is CAplus and MEDLINE.

The palladium-nickel binary nanocluster is reported as a new catalyst system for Suzuki-Miyaura cross-coupling of ortho-heterocycle-tethered sterically hindered aryl bromides. The inferior results obtained with the reported Pd/Ni salts/complexes or individual Pd/Ni nanoparticles as catalyst reveal the cooperative catalytic effect of the Pd and Ni nanoparticles in the Pd-Ni nanocluster. The broad substrate scope with respect to variation of the 2-arylbenzoxazole moiety and boronic acids, which offers a means for diversity generation and catalyst recyclability, marks a distinct advantage. E.g., in presence of palladium-nickel binary nanoclusters in DMF, Suzuki-Miyaura cross-coupling of PhB(OH)₂ with sterically hindered aryl bromide (I) gave 80% II.

Organic Letters published new progress about 480438-56-0. 480438-56-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C4H3Cl2N3, SDS of cas: 480438-56-0.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics