Tag: M.W=150-200

Kathade, Prasad P. published the artcileSynthesis of new thiazole derivatives and evaluation of their antimicrobial potential, Safety of 1-(4-Chlorophenyl)thiourea, the publication is World Journal of Pharmacy and Pharmaceutical Sciences (2018), 7(6), 1362-1379, database is CAplus.

The new thiazole derivatives I [R = H, Me, Cl; R¹ = H, Cl, Br] was synthesized by reaction of phenacyl bromides and N-Ph thioureas. In first step substituted acetophenone was allowed to react with bromine in the presence of AlCl₃ gave phenacyl bromide derivatives In second step substituted anilines were reacted with ammonium thiocyanate in the presence of HCl and water which refluxed for about 3-4 h gave various derivatives of N-Ph thiourea. Antibacterial screening of newly synthesized compounds I was carried out against E. coli, S. aureus and antifungal activity against A. niger according to cup-plate method. The synthesized compounds I were more effective against S. aureus and E. coli. and Compound I [R = Me; R¹ = Cl] is effective against A. niger.

World Journal of Pharmacy and Pharmaceutical Sciences 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 C7H7ClN2S, Safety of 1-(4-Chlorophenyl)thiourea.

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

Degorce, Sebastien L. published the artcileInvestigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators, HPLC of Formula: 209919-30-2, the publication is Journal of Medicinal Chemistry (2015), 58(8), 3522-3533, database is CAplus and MEDLINE.

A novel estrogen receptor down-regulator, 7-hydroxycoumarin (5, SS5020), has been reported with antitumor effects against chem. induced mammary tumors. Here, we report on our own investigation of 7-hydroxycoumarins as potential selective estrogen receptor down-regulators, which led us to the discovery of potent down-regulating antagonists, such as 33. Subsequent optimization and removal of the 7-hydroxy group led to coumarin 59, which had increased potency and improved rat bioavailability relative to SS5020.

Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, HPLC of Formula: 209919-30-2.

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

Reichelt, Andreas published the artcileSynthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors, Formula: C7H8BClO2, the publication is European Journal of Medicinal Chemistry (2014), 364-382, database is CAplus and MEDLINE.

The Cell division cycle 7 (Cdc7) protein kinase is essential for DNA replication and maintenance of genome stability. We systematically explored thiazole-based compounds as inhibitors of Cdc7 kinase activity in cancer cells. Our studies resulted in the identification of a potent, selective Cdc7 inhibitor (I) that decreased phosphorylation of the direct substrate MCM2 in vitro and in vivo, and inhibited DNA synthesis and cell viability in vitro.

European Journal of Medicinal Chemistry published new progress about 145349-62-8. 145349-62-8 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids, name is 2-Chloro-4-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Formula: C7H8BClO2.

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

Causey, Patrick W. published the artcileSynthesis, Characterization, and Assessment of Cytotoxic Properties of a Series of Titanocene Dichloride Derivatives, Recommanded Product: 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, the publication is Organometallics (2004), 23(19), 4486-4494, database is CAplus.

A series of 15 water-soluble titanocene dichloride derivatives containing alkylammonium groups pendant to one (monocationic complexes) or both (dicationic complexes) cyclopentadienyl rings has been synthesized and characterized. The in vitro cytotoxicities of this small library of potential anticancer drugs have been assessed against human lung cancer (H209, A549, H209/CP) and ovarian cancer (A2780, A2780/CP) cell lines, and the results are compared with the cytotoxicities of both cisplatin (cis-PtCl₂(NH₃)₂) and a clin. formulation of titanocene dichloride that is commonly used against cisplatin-resistant tumors. While none of the compounds exhibit potency greater than that of cisplatin, several are clearly superior to the clin. formulation. In particular dicationic complexes generally exhibit greater potency than do the corresponding monocationic analogs, and derivatives containing protonated piperidinyl rings exhibit greater potency than do compounds containing protonated 2-aminoethyl or 3-aminopropyl groups. Eight of the compounds, representing a wide range of potencies, were characterized crystallog. but no correlations between effectiveness and structures were obvious.

Organometallics published new progress about 4584-49-0. 4584-49-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Salt,Amine,Aliphatic hydrocarbon chain, name is 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, and the molecular formula is C5H13Cl2N, Recommanded Product: 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride.

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

Lukin, Alexey published the artcileExploration of the nitrogen heterocyclic periphery around the core of the advanced FFA1 agonist fasiglifam (TAK-875), Name: 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is Archiv der Pharmazie (Weinheim, Germany) (2021), 354(4), 2000275, database is CAplus and MEDLINE.

Three types of heterocyclic moieties-piperidines fused to a heteroaromatic moiety-were explored as potential periphery motifs for the pharmacophoric core of fasiglifam (TAK-875), with fasiglifam being the most advanced agonist of free fatty acid receptor 1, a promising target for therapeutic intervention in type 2 diabetes. Several observed structure-activity relationship trends were corroborated by in silico docking results. Balanced selection based on potency and Caco-2 permeability advanced six compounds to cellular efficacy tests (glucose-stimulated insulin secretion in rat insulinoma INS1E cells). This led to the nomination of compound I·HCl (LK1408, 3-[4-({4-[(3-{[(2-fluorobenzyl)oxy]methyl}-1-methyl-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)methyl]benzyl}oxy)phenyl]propanoic acid hydrochloride) as the lead for further development.

Archiv der Pharmazie (Weinheim, Germany) published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Name: 1-(Chloromethyl)-4-(trifluoromethyl)benzene.

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

Baldwin, Ian published the artcileKinase array design, back to front: Biaryl amides, Quality Control of 6313-54-8, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(19), 5285-5289, database is CAplus and MEDLINE.

New kinase inhibitors can be found by synthesis of targeted arrays of compounds designed using system-based knowledge as well as through screening focused or diverse compounds Most array strategies aim to add functionality to a fragment that binds in the purine subpocket of the ATP-site. Here, an alternative pharmacophore-guided array approach is described which set out to discover novel purine subpocket-binding groups. Results are shown for p38α and cFMS kinase, for which multiple distinct series with nanomolar potency were discovered. Some of the compounds showed potency in cell-based assays and good pharmacokinetic properties.

Bioorganic & Medicinal Chemistry Letters 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, Quality Control of 6313-54-8.

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

Jagadeesh, Rajenahally V. published the artcileHighly selective transfer hydrogenation of functionalised nitroarenes using cobalt-based nanocatalysts, SDS of cas: 350-30-1, the publication is Green Chemistry (2015), 17(2), 898-902, database is CAplus.

Anilines are important feedstock for the synthesis of a variety of chems. such as dyes, pigments, pharmaceuticals and agrochems. The chemoselective catalytic reduction of nitro compounds represents the most important and prevalent process for the manufacture of functionalized anilines. Consequently, the development of selective catalysts for the reduction of nitro compounds in the presence of other reducible groups is a major challenge and is crucial. In this regard, herein we show that the cobalt oxide (Co₃O₄-NGr@C) based nano-materials, prepared by the pyrolysis of cobalt-phenanthroline complexes on carbon constitute highly selective catalysts for the transfer hydrogenation of nitroarenes to anilines using formic acid as a hydrogen source. Applying these catalysts, a series of structurally diverse and functionalized nitroarenes have been reduced to anilines with unprecedented chemo-selectivity tolerating halides, olefins, aldehyde, ketone, ester, amide and nitrile functionalities.

Green Chemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, SDS of cas: 350-30-1.

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

Sato, Takahiro published the artcileDiscovery of 3-(3-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 – a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia, Product Details of C6H4ClNO2, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(21), 6225-6229, database is CAplus and MEDLINE.

A previous study identified 2-[2-(2-methoxy-ethoxy)-ethoxy]-5-[5-(2-methyl-4-pyridyl)-1H-[1,2,4]triazol-3-yl]-benzonitrile as a safe and potent xanthine oxidoreductase (XOR) inhibitor for the treatment of hyperuricemia. A series of 3,5-dipyridyl-1,2,4-triazole derivatives were synthesized and their in vivo activity in lowering the serum uric acid levels in rats was examined As a result, 3-(3-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole (FYX-051) to be one of the most potent XOR inhibitors; it exhibited an extremely potent in vivo activity, weak CYP3A4-inhibitory activity and a better pharmacokinetic profile than the previously identified compound FYX-051 is currently being evaluated in a phase 2 clin. trial.

Bioorganic & Medicinal Chemistry Letters 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, Product Details of C6H4ClNO2.

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

Sato, Takahiro published the artcileDesign, synthesis, and pharmacological and pharmacokinetic evaluation of 3-phenyl-5-pyridyl-1,2,4-triazole derivatives as xanthine oxidoreductase inhibitors, Related Products of chlorides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(1), 184-187, database is CAplus and MEDLINE.

In an effort to find a potent xanthine oxidoreductase (XO) inhibitor, we discovered the best compound I. Here, we describe the following: (1) the design, synthesis, and structure-activity relationship of a series of 3-phenyl-5-pyridyl-1,2,4-triazole derivatives by in vitro studies of XO inhibitory activity in bovine milk and in vivo studies of serum uric acid (UA) reductive activity in rats, (2) a drug interaction study by a cytochrome P 450 3A4 (CYP3A4) assay, and (3) a pharmacokinetic (PK) study. Compound I exhibits potent XO inhibitory activity, serum UA-lowering activity in rats, weak CYP3A4 inhibitory activity, and moderate PK profile.

Bioorganic & Medicinal Chemistry Letters 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

Patil, Vrushali published the artcileBiological evaluation of some synthesized benzothiazole derivatives and their characterization, Application In Synthesis of 3696-23-9, the publication is World Journal of Pharmaceutical Research (2015), 4(2), 842-850, database is CAplus.

Synthesis, characterization and biol. evaluation of [(1,3-benzothiazol-2-yl)-3,3-phenyl-1H-pyrazol-4-yl]methylidene thioureas I [R = H, 4-HO, 4-Cl, 4-C₂H₅O, 3,5-(MeO)₂] was reported. The compounds containing benzothiazole nucleus were treated with hydrazine hydrate to form hydrazone derivative followed by reaction with acetophenone and further cyclization via Vilsmeier-Haack reaction using DMF/POCl₃ and thus obtained intermediates were finally condensed with substituted thiourea. The structure of compounds I were confirmed by spectral anal. such as FT-IR, NMR, mass spectrophotometer and were further screened for various in-vitro biol. activities such as anti-oxidant, anti-inflammatory, anti-microbial activities. It was found that compounds I showed enhancing biol. activity.

World Journal of Pharmaceutical Research 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 C7H7ClN2S, Application In Synthesis of 3696-23-9.

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