Tag: M.W=200-250

Lee, Hee-Yoon published the artcileStructure-activity relationship studies of the chromosome segregation inhibitor, Incentrom A, Application In Synthesis of 87179-40-6, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(16), 4670-4674, database is CAplus and MEDLINE.

A series of Incentrom A analogs that inhibit the chromosome segregation process in yeast were synthesized and tested for their effects on chromosome stability and cell proliferation. Pharmacophore and structure-activity relationship of Incentrom A for the anti-yeast activity were established.

Bioorganic & Medicinal Chemistry Letters published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Application In Synthesis of 87179-40-6.

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

Hatnapure, Girish D. published the artcileSynthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent, Formula: C13H18N2, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(20), 6385-6390, database is CAplus and MEDLINE.

A series of 6-methoxy-2-(piperazin-1-yl)-4H-chromen-4-one and 5,7-dimethoxy-2-(piperazin-1-ylmethyl)-4H-chromen-4-one derivatives of biol. interest were prepared and screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Among all the title compound screened, seven compounds, e.g., I, were found to have promising anti-inflammatory activity (up to 65-87% TNF-α and 70-93% IL-6 inhibitory activity) at concentration of 10 μM with reference to standard dexamethasone (71% TNF-a and 84% IL-6 inhibitory activities at 1 μM) while five compounds were found to be potent antimicrobial agent showing even 2 to 2.5-fold more potency than that of standard ciprofloxacin and miconazole at the same MIC value of 10 μg/mL.

Bioorganic & Medicinal Chemistry Letters published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Formula: C13H18N2.

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

Huang, Y. published the artcileSynthesis of potent and selective dopamine D₄ antagonists as candidate radioligands, Category: piperazines, the publication is Bioorganic & Medicinal Chemistry Letters (2001), 11(11), 1375-1377, database is CAplus and MEDLINE.

A series of dopamine D₄ antagonists, pyridinylpyrrolyl arylpiperazines I (R = F, MeO, R¹ = H; R = H, R¹ = F, MeO, MeS, CF₃, CH:CH₂, Et, Pr, Ph), was synthesized and evaluated as potential candidates for development as positron emission tomog. (PET) radioligands. Thus, azagramine II was reacted with the corresponding arylpiperazine in xylene under reflux to give I in 45 to 82% yield. All new compounds display high affinity and selectivity for the D₄ receptors and compounds I (R = H, R¹ = MeO; R = MeO, R1 = H; R = H, R¹ = MeS) were identified as candidates for radioligand development. The activity against serotonin receptors was also examined

Bioorganic & Medicinal Chemistry Letters published new progress about 180698-19-5. 180698-19-5 belongs to piperazines, auxiliary class Piperazine,Benzene, name is 1-Biphenyl-4-yl-piperazine, and the molecular formula is C16H18N2, Category: piperazines.

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

Rotstein, David M. published the artcileStereoisomers of ketoconazole: preparation and biological activity, SDS of cas: 67914-60-7, the publication is Journal of Medicinal Chemistry (1992), 35(15), 2818-25, database is CAplus and MEDLINE.

The four stereoisomers of the antifungal agent ketoconazole, (2S,4R)-, (2R,4R)-, (2R,4S)-, and (2S,4S)-(imidazolylmethyl)phenyl{[(acetylpiperazinyl)phenoxy]methyl}dioxolanes I, were prepared and evaluated for their selectivity in inhibiting a number of cytochrome P 450 enzymes. Thus, (bromomethyl)phenyldioxolanes II condensed with 4-(N-acetylpiperazino)phenol and imidazole to give I. II were prepared by bromination of 2′,4′-dichloroacetophenone followed by reaction with (S)- and (R)-solketal tosylate. Large differences in selectivity among the isomers were observed for inhibition of the cytochromes P 450 involved in steroid biosynthesis, whereas little difference was observed for inhibition of those associated with hepatic drug metabolism The cis-(2S,4R) and trans-(2R,4R) isomers are equipotent in inhibiting corticoid 11β-hydroxylase and much more effective than their antipodes. Little selectivity was observed for inhibition of cholesterol side chain cleavage or xenobiotic hydroxylases. These data indicate that the affinity of azoles for cytochrome P 450 enzymes involved in steroid synthesis is high dependent on the stereochem. of the entire mol., whereas binding to drug metabolizing enzymes is a less selective process.

Journal of Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, SDS of cas: 67914-60-7.

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

Amani, Amene published the artcileElectrochemical oxidation of acetaminophen and 4-(piperazin-1-yl)phenols in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone, Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Journal of the Electrochemical Society (2013), 160(1), H33-H40, database is CAplus.

A facile and 1-pot electrochem. method for the synthesis of mono and disubstituted 1,4-benzoquinones generated from the electrochem. oxidation of 1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone (1a), 4-(piperazin-1-yl)phenol (1b) and acetaminophen (8) in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone (3) as nucleophile is reported. The electrochem. generated electrophiles derived from the oxidation of 1a, 1b and 8 participate in Michael-addition reactions with 3. The authors report the synthesis of mono and diquinolone substituted of 1,4-benzoquinone in good yields based on controlled potential condition at C electrode in a divided cell.

Journal of the Electrochemical Society published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

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

Brebion, Franck published the artcileDiscovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis, HPLC of Formula: 180698-19-5, the publication is Journal of Medicinal Chemistry (2021), 64(6), 2937-2952, database is CAplus and MEDLINE.

There are currently no approved disease-modifying osteoarthritis (OA) drugs (DMOADs). The aggrecanase ADAMTS-5 is key in the degradation of human aggrecan (AGC), a component of cartilage. Therefore, ADAMTS-5 is a promising target for the identification of DMOADs. We describe the discovery of GLPG1972/S201086, a potent and selective ADAMTS-5 inhibitor obtained by optimization of a promising hydantoin series following an HTS. Biochem. activity against rat and human ADAMTS-5 was assessed via a fluorescence-based assay. ADAMTS-5 inhibitory activity was confirmed with human aggrecan using an AGC ELISA. The most promising compounds were selected based on reduction of glycosaminoglycan release after interleukin-1 stimulation in mouse cartilage explants and led to the discovery of GLPG1972/S201086. The anticatabolic activity was confirmed in mouse cartilage explants (IC₅₀ < 1.5μM). The cocrystal structure of GLPG1972/S201086 with human recombinant ADAMTS-5 is discussed. GLPG1972/S201086 has been investigated in a phase 2 clin. study in patients with knee OA (NCT03595618).

Journal of Medicinal Chemistry published new progress about 180698-19-5. 180698-19-5 belongs to piperazines, auxiliary class Piperazine,Benzene, name is 1-Biphenyl-4-yl-piperazine, and the molecular formula is C16H18N2, HPLC of Formula: 180698-19-5.

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

Boursalian, Gregory B. published the artcileCharge-transfer-directed radical substitution enables para-selective C-H functionalization, Product Details of C16H18N2, the publication is Nature Chemistry (2016), 8(8), 810-815, database is CAplus and MEDLINE.

Efficient C-H functionalization requires selectivity for specific C-H bonds. Progress has been made for directed aromatic substitution reactions to achieve ortho and meta selectivity, but a general strategy for para-selective C-H functionalization has remained elusive. Herein we introduce a previously unappreciated concept that enables nearly complete para selectivity. We propose that radicals with high electron affinity elicit arene-to-radical charge transfer in the transition state of radical addition, which is the factor primarily responsible for high positional selectivity. We demonstrate with a simple theor. tool that the selectivity is predictable and show the utility of the concept through a direct synthesis of aryl piperazines. Our results contradict the notion, widely held by organic chemists, that radical aromatic substitution reactions are inherently unselective. The concept of radical substitution directed by charge transfer could serve as the basis for the development of new, highly selective C-H functionalization reactions.

Nature Chemistry published new progress about 180698-19-5. 180698-19-5 belongs to piperazines, auxiliary class Piperazine,Benzene, name is 1-Biphenyl-4-yl-piperazine, and the molecular formula is C16H18N2, Product Details of C16H18N2.

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

Civiello, Rita L. published the artcileSynthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines, Synthetic Route of 180698-19-5, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(4), 1229-1232, database is CAplus and MEDLINE.

Calcitonin gene-related peptide (CGRP) is a potent neuropeptide implicated in the pathophysiol. of migraine. In seeking CGRP antagonists with improved oral bioavailability, metabolic stability, and pharmacokinetic properties, lower mol. weight, structurally simpler piperidine and piperazine analogs of BMS-<694153≥ were prepared Several have nM binding affinity in vitro. The synthesis and SAR of these substituted piperidine and piperazine CGRP antagonists are discussed.

Bioorganic & Medicinal Chemistry Letters published new progress about 180698-19-5. 180698-19-5 belongs to piperazines, auxiliary class Piperazine,Benzene, name is 1-Biphenyl-4-yl-piperazine, and the molecular formula is C16H18N2, Synthetic Route of 180698-19-5.

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

Sajiki, Hironao published the artcileThe Formation of a Novel Pd/C-Ethylenediamine Complex Catalyst: Chemoselective Hydrogenation without Deprotection of the O-Benzyl and N-Cbz Groups, Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is Journal of Organic Chemistry (1998), 63(22), 7990-7992, database is CAplus.

A Pd/C catalyst formed an isolable complex with ethylenediamine employed as the catalytic poison via one-to-one interaction between Pd metal and ethylenediamine, and this complex catalyst [Pd/C(en)] chemoselectively hydrogenated a variety of reducible functionalities such as olefin, acetylene, nitro, benzyl ester, and azido in the presence of an O-benzyl or N-Cbz protective group. These findings reinforce the versatility potential of O-benzyl and N-Cbz as protective groups in organic synthesis, and the Pd/C(en) catalyst has been identified as a novel and chemoselective catalyst for the hydrogenation.

Journal of Organic Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Recommanded Product: (E)-1-Cinnamylpiperazine.

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

Xiao, Jichao published the artcileRemote sp³ C-H Amination of Alkenes with Nitroarenes, Product Details of C13H18N2, the publication is Chem (2018), 4(7), 1645-1657, database is CAplus.

Direct installation of a functional group at remote, unfunctionalized sites in an alkyl chain is a synthetically valuable but rarely reported process. The remote relay hydroarylamination of distal and proximal olefins, and of olefin isomeric mixtures, has been achieved through NiH-catalyzed alkene isomerization and sequential reductive hydroarylamination with nitroarenes. This provides an attractive approach to the direct installation of a distal arylamino group within alkyl chains. The single-step conversion of simple olefins and nitro(hetero)arenes to value-added arylamines is a practical strategy for amine synthesis as well as the remote activation of sp³ C-H bonds. The value of this transformation is further supported by the regioconvergent arylamination of isomeric mixtures of olefins.

Chem published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C6H12N2O, Product Details of C13H18N2.

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