Tag: M.W=150-200

Kedari, Chaitanya Kumar published the artcileBiarylmethoxy Nicotinamides As Novel and Specific Inhibitors of Mycobacterium tuberculosis, Computed Properties of 766549-26-2, the publication is ACS Medicinal Chemistry Letters (2014), 5(5), 491-495, database is CAplus and MEDLINE.

A whole cell based screening effort on a focused library from corporate collection resulted in the identification of biarylmethoxy nicotinamides as novel inhibitors of M. tuberculosis (Mtu) H37Rv. The series exhibited tangible structure-activity relationships, and during hit to lead exploration, a cellular potency of 100 nM was achieved, which is an improvement of >200-fold from the starting point. The series is very specific to Mtu and noncytotoxic up to 250 μM as measured in the mammalian cell line THP-1 based cytotoxicity assay. This compound class retains its potency on several drug sensitive and single drug resistant clin. isolates, which indicate that the compounds could be acting through a novel mode of action.

ACS Medicinal Chemistry Letters published new progress about 766549-26-2. 766549-26-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Phenol,Boronic Acids,Boronic acid and ester, name is 2-Chloro-4-hydroxyphenylboronic acid, and the molecular formula is C6H6BClO3, Computed Properties of 766549-26-2.

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

Charier, Sandrine published the artcilePhotophysics of a series of efficient fluorescent pH probes for dual-emission-wavelength measurements in aqueous solutions, Related Products of chlorides-buliding-blocks, the publication is Chemistry – A European Journal (2006), 12(4), 1097-1113, database is CAplus and MEDLINE.

This paper evaluates the 5-aryl-2-pyridyloxazole backbone to engineer donor-acceptor fluorescent pH probes after one- or two-photon absorption. Parent fluorophores, as well as derivatives that can be used to label biomols., can be easily obtained in good yields. These mols. exhibit a large one-photon absorption in the near-UV range, and a strong fluorescence emission that covers the whole visible domain. The 5-aryl-2-pyridyloxazole derivatives also possess significant cross sections for two-photon absorption. Upon pyridine protonation, large shifts were observed in the absorption spectra after one- and two-photon excitation, as well as in the emission spectra. This feature was used to measure the pK_a of the investigated compounds that range between 2 and 8. In most of the investigated derivatives, the pK_a increased upon light excitation and protonation exchanges took place during the lifetime of the excited state, as shown by phase-modulation fluorometry anal. Several 5-aryl-2-pyridyloxazole derivatives are suggested as efficient probes to reliably measure the pH of aqueous solutions by means of ratiometric methods that are dependent on fluorescence emission.

Chemistry – A European Journal published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Related Products of chlorides-buliding-blocks.

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

Charier, Sandrine published the artcilepH sensors: An efficient fluorescent probe for ratiometric pH measurements in aqueous solutions, Safety of 2-Chloroisonicotinic acid, the publication is Angewandte Chemie, International Edition (2004), 43(36), 4785-4788, database is CAplus and MEDLINE.

Just a litmus paper changes from red to blue with an increase in pH, so the fluorescence emission of the oxazole derivative 1 shifts from green to blue. Ratiometric measurements of the fluorescence emissions of the two species, after one- or two-photon excitation, allow 1 to be employed as a pH sensor over the mid-pH range.

Angewandte Chemie, International Edition published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Safety of 2-Chloroisonicotinic acid.

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

Daengrot, Charuwan published the artcileEremophilane sesquiterpenes and diphenyl thioethers from the soil fungus Penicillium copticola PSU-RSPG138, Application of 3-Chloro-4-hydroxyphenylacetic acid, the publication is Journal of Natural Products (2015), 78(4), 615-622, database is CAplus and MEDLINE.

Four new compounds including two eremophilane sesquiterpenes, penicilleremophilanes A (1) and B (2), as well as two sulfur-containing biphenols, penicillithiophenols A (3) and B (4), were isolated from the soil fungus Penicillium copticola PSU-RSPG138 together with 16 known compounds Their structures were elucidated by spectroscopic methods. Known sporogen AO-1 exhibited significant antimalarial activity against Plasmodium falciparum with an IC₅₀ value of 1.53 μM and cytotoxic activity to noncancerous (Vero) cell lines with an IC₅₀ value of 4.23 μM. Although compound 1 was approx. half as active against P. falciparum with the IC₅₀ value of 3.45 μM, it showed much weaker cytotoxic activity.

Journal of Natural Products published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Application of 3-Chloro-4-hydroxyphenylacetic acid.

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

Epple, Robert published the artcile3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists, Category: chlorides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2006), 16(16), 4376-4380, database is CAplus and MEDLINE.

The authors report the identification of a novel series of trisubstituted isoxazoles as PPAR activators from a high-throughput screen. A series of structural optimizations led to improved efficacy and excellent functional receptor selectivity for PPARδ. The isoxazoles represent a series of agonists which display a scaffold that lies outside the typical PPAR agonist motif.

Bioorganic & Medicinal Chemistry Letters published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Category: chlorides-buliding-blocks.

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

Yuan, Tengrui published the artcileStereoselective gold(I)-catalyzed vinylcyclopropanation via generation of sulfur-substituted vinyl carbene equivalent, HPLC of Formula: 1263414-46-5, the publication is Angewandte Chemie, International Edition (2021), 60(8), 4070-4074, database is CAplus and MEDLINE.

A stereoselective gold(I)-catalyzed vinylcyclopropanation of alkenes has been developed. A gold-coordinated cationic vinyl carbene species, readily generated via a rearrangement of the ethylenedithioacetal of propargyl aldehyde, reacts with a wide range of alkenes to afford thio-substituted vinylcyclopropanes. The gold-catalyzed vinyl cyclopropanation proceeds under mild conditions at room temperature and is generally selective for the formation of cis-substituted cyclopropanes. The reaction allows the formal introduction of a “naked” vinyl carbene, by subsequent chemoselective hydrodesulfuration of the ethylenedithio-bridge. The synthetic utility of the new method is demonstrated by a short, racemic formal synthesis of the alkaloid cephalotaxin, hinging on a key vinyl cyclopropane-cyclopentene rearrangement.

Angewandte Chemie, International Edition published new progress about 1263414-46-5. 1263414-46-5 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Alkenyl,Benzene, name is 4-Chloro-3-fluorostyrene, and the molecular formula is C19H34ClN, HPLC of Formula: 1263414-46-5.

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

Jellen, Emily E. published the artcileProbing the stability and structure of metalloporphyrin complexes with basic peptides by mass spectrometry, Quality Control of 6249-56-5, the publication is European Journal of Mass Spectrometry (2005), 11(1), 65-72, database is CAplus and MEDLINE.

The stability and structure of noncovalent complexes of various peptides containing basic amino acid residues (Arg, Lys) with metalloporphyrins were studied in a quadrupole ion trap mass spectrometer. The complexes of heme and three other metalloporphyrins with a variety of basic peptides and model systems were formed via electrospray ionization (ESI) and their stability was probed by energy-variable collision-induced dissociation (CID). A linear dependence for basic peptides and model compounds/metalloporphyrin complexes was observed in the plots of stability vs. degrees of freedom and was used to evaluate relative bond strength. These results were then compared with previous data obtained for complexes of metalloporphyrins with His-containing peptides and peptides containing no basic amino acids. The binding strengths of Lys-containing peptide complexes in the gas phase is almost as strong as that of Arg-containing complexes. Both systems showed stronger binding than His-containing peptides studied previously. To probe the structure of Arg and Lys noncovalent complexes (charge solvation vs. salt bridges), two techniques, CID and ion-mol. reactions, were used. CID experiments indicate that the gas-phase complexes are most likely formed by charge solvation of the central metal ion in the metalloporphyrin by basic side chains of Arg or Lys. Results from the ion-mol. reaction studies are consistent with the charge solvation structure as well.

European Journal of Mass Spectrometry published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C7H16ClNO2, Quality Control of 6249-56-5.

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

Kumar, Rohitesh published the artcileDesign and Synthesis of a Screening Library Using the Natural Product Scaffold 3-Chloro-4-hydroxyphenylacetic Acid, Recommanded Product: 3-Chloro-4-hydroxyphenylacetic acid, the publication is Journal of Natural Products (2015), 78(4), 914-918, database is CAplus and MEDLINE.

The fungal metabolite 3-chloro-4-hydroxyphenylacetic acid (I) was utilized in the generation of a unique drug-like screening library using parallel solution-phase synthesis. A 20-membered amide library, II (R = CH₂CH₂CHMe₂, morpholinoethyl, CH₂CH₂NMe₂, etc.), III (R¹, R² = H, F, R³ = H, Br, Cl, F), and IV, was generated by first converting I to Me (3-chloro-4-hydroxyphenyl)acetate, then reacting this scaffold with a diverse series of primary amines via a solvent-free aminolysis procedure. The structures of the synthetic analogs II, III, and IV were elucidated by spectroscopic data anal. The structures of compounds III (R¹ = F, R² = R³ = H), IV (R¹ = R² = H, R³ = F), and the hydrate of II (R = CH₂CH₂NMe₂) were confirmed by single X-ray crystallog. anal. All compounds were evaluated for cytotoxicity against a human prostate cancer cell line (LNCaP) and for antiparasitic activity toward Trypanosoma brucei brucei and Plasmodium falciparum and showed no significant activity at 10 μM. The library was also tested for effects on the lipid content of LNCaP and PC-3 prostate cancer cells, and it was demonstrated that the fluorobenzyl analogs IV (R¹ = R² = H, R³ = F; R¹ = R³ = H, R² = F; R¹ = F, R² = R³ = H) significantly reduced cellular phospholipid and neutral lipid levels.

Journal of Natural Products published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Recommanded Product: 3-Chloro-4-hydroxyphenylacetic acid.

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

Sharma, Prabodh Chander published the artcileDesign, Synthesis and Molecular Docking Studies of Some Thiazole Clubbed Heterocyclic Compounds as Possible Anti-infective Agents, HPLC of Formula: 3696-23-9, the publication is Letters in Organic Chemistry (2018), 15(8), 716-726, database is CAplus.

{[(Chlorophenyl)thiazolyl]arylpyrazolylmethylene}(arylimino)thiazolidinones I (R = 4-ClC₆H₄, 2-ClC₆H₄, Ph, 3-Cl-2-FC₆H₃, 4-FC₆H₄, 2,4-Cl₂C₆H₃, 2-ClC₆H₄, 4-MeOC₆H₄, 4-O₂NC₆H₄; R¹ = H, F, Cl, Br) were prepared and tested as antibacterial, antifungal, antimalarial, and antihelminthic agents. Potential binding modes of selected compounds with 14α-sterol demethylase and DNA gyrase subunit A were determined using mol. docking calculations The tested compounds exhibited moderate to significant antimicrobial activities. I (R = 4-O₂NC₆H₄; R¹ = Br) showed significant antimalarial activity with an IC₅₀ value of 0.59 μg/mL [as compared to chloroquine (IC₅₀ = 0.020 μg/mL) and quinine (IC₅₀ = 0.268 μg/mL)]. I (R = 2,4-Cl₂C₆H₃; R¹ = Cl) showed antihelminthic activity in earthworms with a mean time to paralysis of 19.2 ± 0.9 min and mean time to death of 31.7 ± 2.5 min.

Letters in Organic Chemistry published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C15H14O3, HPLC of Formula: 3696-23-9.

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

Somawardhana, C. W. published the artcileSynthesis of 2-[¹²³I and ¹²⁴I]-iodoisonicotinic acid hydrazide-potential radiotracers for tuberculosis, SDS of cas: 6313-54-8, the publication is Applied Radiation and Isotopes (1991), 42(3), 215-20, database is CAplus and MEDLINE.

The radiochem. syntheses of Me 2-[¹²³I]-iodoisonicotinate, 2-[¹²³I]-iodoisonicotinic acid hydrazide (I) and 2-[¹²⁴I]-iodoisonicotinic acid hydrazide was accomplished. Iodine-123 was incorporated in the Me ester mol. by an exchange reaction in glacial acetic acid. The average efficiency of iodine exchange reaction was (92.6%). This radiotracer was extracted with ether and the solvent was evaporated The residue was re-dissolved in anhydrous ethanol and treated with hydrazine under anhydrous conditions to obtain I. The overall radiochem. yield was 69%. Biodistribution data of both radio-tracers in male Sprague-Dawley rats were collected. This is the first report of SPECT radiopharmaceuticals which may be useful for differential diagnosis of intracranial masses (tuberculoma vs. glioma), and CNS tuberculosis in immunosuppressed subjects.

Applied Radiation and Isotopes published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C9H10O4, SDS of cas: 6313-54-8.

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