Tag: M.W=200-250

Bruncko, Milan published the artcileStructure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity, Product Details of C12H16N2O2, the publication is Journal of Medicinal Chemistry (2015), 58(5), 2180-2194, database is CAplus and MEDLINE.

Myeloid cell leukemia 1 (MCL-1) is a BCL-2 family protein that has been implicated in the progression and survival of multiple tumor types. Herein the authors report a series of MCL-1 inhibitors that emanated from a high throughput screening (HTS) hit and progressed via iterative cycles of structure-guided design. Advanced compounds from this series exhibited subnanomolar affinity for MCL-1 and excellent selectivity over other BCL-2 family proteins as well as multiple kinases and GPCRs. In a MCL-1 dependent human tumor cell line, administration of compound I rapidly induced caspase activation with associated loss in cell viability. The small mols. described herein thus comprise effective tools for studying MCL-1 biol.

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, Product Details of C12H16N2O2.

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

Lodha, Kamlesh K. published the artcileExploring new tetrahydrothienopyridine derivatives as platelet agglutination inhibitors: synthesis, biological evaluation and In silico study, Quality Control of 67914-60-7, the publication is ChemistrySelect (2022), 7(2), e202103428, database is CAplus.

The P2Y12 receptor is the major target for antithrombic drugs which plays a key role in platelet activation. New derivatives of 4,5,6,7-tetrahydrothieno[3,2-c]pyridine (THP) were designed targeting P2Y12 receptor. An efficient route was developed for synthesis of THP derivatives and subsequently evaluated for their antiplatelet agglutination activity. Amongst the synthesized THP derivatives (4 a-4 g), the compounds 4 a and 4 g displayed significant activity (with 88.25 and 70.17 % inhibition) as compared to other analogs and comparable with that of the reference drugs, aspirin and prasugrel. Data extracted from computational chem. techniques such as mol. docking, provided the structural rationale for the observed platelet agglutination inhibition by the newly synthesized tetrahydrothienopyridine analogs. We proposed the involvement of residues such as Cys-194 in the formation of the covalent adduct with the active metabolite of tetrahydrothienopyridine derivatives This study also put forward the possibility of the existence of an alternate pathway for metabolizing the tetrahydrothienopyridine compounds The structural data presented in this study is expected to accelerate the research on developing a tetrahydrothienopyridine scaffold as an effective antithrombotic therapeutic modality.

ChemistrySelect 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, Quality Control of 67914-60-7.

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

Sanz Sharley, Daniel D. published the artcileAcetic acid as a catalyst for the N-acylation of amines using esters as the acyl source, Related Products of piperazines, the publication is Chemical Communications (Cambridge, United Kingdom) (2017), 53(12), 2020-2023, database is CAplus and MEDLINE.

Authors report a cheap and simple method for the acetylation of a variety of amines using catalytic acetic acid and either Et acetate or Bu acetate as the acyl source. Catalyst loadings as low as 10 mol% afforded acetamide products in excellent yields at temperatures ranging from 80-120°. The methodol. can also be successfully applied for the synthesis of a broad range of other amides, including the formation of formamides at 20°.

Chemical Communications (Cambridge, United Kingdom) 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, Related Products of piperazines.

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

Xie, Chao published the artcileNatural Product Glycine Betaine as an Efficient Catalyst for Transformation of CO₂ with Amines to Synthesize N-Substituted Compounds, Safety of (E)-1-Cinnamylpiperazine, the publication is ACS Sustainable Chemistry & Engineering (2017), 5(8), 7086-7092, database is CAplus.

Transformation of carbon dioxide (CO₂) into value-added chems. is of great importance, and use of natural products as a catalyst is very interesting. Herein, we used the naturally occurring glycine betaine as an efficient and renewable catalyst for the formation of a C-N bond between CO₂ and amines using PhSiH₃ as the reductant. The effects of different factors on the reaction were studied. It was demonstrated that the catalyst was very active for the reactions, and a broad range of amine substrates could be converted with satisfactory yields. Moreover, the selectivity to different N-substituted compounds could be controlled by the molar ratio of reactants (i.e., CO₂, amines, and PhSiH₃) and the reaction temperature In the catalytic cycle, the carbon oxidation state of CO₂ could be reduced to +2, 0, and -2, resp., and thus, the corresponding formamides, aminals, and methylamines were produced via successive two-electron reduction steps.

ACS Sustainable Chemistry & Engineering 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 C2H5BF3K, Safety of (E)-1-Cinnamylpiperazine.

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

Manojkumar, K. E. published the artcileSynthesis, characterization and biological evaluation of novel substituted acid amides containing piperazine-1,2,4-oxadiazole nucleus, Product Details of C10H17N3O2, the publication is Journal of Applicable Chemistry (Lumami, India) (2013), 2(4), 730-737, database is CAplus.

Some new (substituted)(4-{5-[3-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-3-yl}piperazin-1-yl)methanone was synthesized using piperazine containing 1,2,4-oxadiazole as core moiety with substituted acids. The newly synthesized compounds were characterized by spectroscopic evidences such as IR, ¹H NMR, ¹³C NMR and CHN elemental anal. All the synthesized compounds were screened for their in vitro antibacterial activity, some of them showed good activity.

Journal of Applicable Chemistry (Lumami, India) published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, Product Details of C10H17N3O2.

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

Nadigar, Mohan R. published the artcileSynthesis and in vitro antibacterial activity of some novel sulfonamide derivatives bearing 1,4-disubstituted-1,2,4-oxadiazole moiety, SDS of cas: 113534-02-4, the publication is Journal of Applicable Chemistry (Lumami, India) (2013), 2(4), 722-729, database is CAplus.

A strategic synthesis of 1-[(2,5-dimethoxyphenyl)sulfonyl]-4-{5-[substituted]-1,2,4-oxadiazol-3-yl}piperazine, involves construction of 1,2,4-oxadiazole ring by intermol. condensation of tert-butyl-4-(N-hydroxycarbamimidoyl)piperazine-1-carboxylate with 3-(trifluromethoxy)benzoic acid. Structures of the newly synthesized compounds were established by IR, ¹H NMR, ¹³C NMR, LC-MS and CHNS spectroscopic evidences. All the newly synthesized compounds were tested for their in vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus cereus. Tested compounds showed good antibacterial activities when compared to the reference ciprofloxacin. Five compounds showed good activity against tested organisms.

Journal of Applicable Chemistry (Lumami, India) published new progress about 113534-02-4. 113534-02-4 belongs to piperazines, auxiliary class Piperazine,Nitrile,Amide, name is tert-Butyl 4-cyanopiperazine-1-carboxylate, and the molecular formula is C10H17N3O2, SDS of cas: 113534-02-4.

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

Corsano, Stefano published the artcileSynthesis and pharmacological evaluation of some analogs of the calcium-antagonist cinnarizine, Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is Archiv der Pharmazie (Weinheim, Germany) (1988), 321(3), 171-4, database is CAplus and MEDLINE.

Title compounds, e.g. I, II, and Ph₂CHNHCH₂CH₂OC₆H₃(OMe)₂-2,6, were prepared Thus, 1-benzhydrylpiperazine was treated with o-MeOC₆H₄OCH₂CH₂Br to give I. The new compounds had lower Ca antagonist activity than cinnarizine.

Archiv der Pharmazie (Weinheim, Germany) 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

Takeuchi, Isao published the artcileSyntheses and antimicrobial activities of cis-1-[2-phenyl-4-(phenoxy or phenylthio)methyl-1,3-dioxolan-2-ylmethyl]-1H-imidazole derivatives, SDS of cas: 67914-60-7, the publication is Yakugaku Zasshi (1985), 105(6), 554-61, database is CAplus and MEDLINE.

Substitution reactions of glycerol ketals I (R, R¹ = H, MeO; Br, Br; Cl, Cl) with heterocycles gave II (R² = 1-imidazolyl, 1-pyrazolyl, 1,2,4-triazol-1-yl) which underwent successive saponification, mesylation, and substitution reaction with R³R⁴C₆H₃XH (R³, R⁴ = H, MeO, Cl, Me, Br; X = O, S) to give ketoconazole analogs III. Antimicrobial test of the synthesized compounds III (R² = 1-imidazolyl; R, R¹, R³, R⁴, X = Cl, Cl, H, 4-Cl, S; Cl, Cl, 2-Cl, 6-Cl, S; Br, Br, 2-Cl, 6-Cl, S) showed strong antimicrobial activities against Penicillium chrysogenum and Trichophyton rubrum. Most compounds synthesized had strong preventive effects against downy mildew and sheath blight. Triazole derivatives III (R² = 1-triazolyl; R = R¹ = Cl; R³ = H, 2-Cl; R⁴ = Cl; X = S, O) showed similar effects against not only such diseases but gray mold rot.

Yakugaku Zasshi 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 C38H74Cl2N2O4, SDS of cas: 67914-60-7.

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

Chan, Kin-Fai published the artcileEfficient Synthesis of Amine-Linked 2,4,6-Trisubstituted Pyrimidines as a New Class of Bacterial FtsZ Inhibitors, Quality Control of 87179-40-6, the publication is ACS Omega (2017), 2(10), 7281-7292, database is CAplus and MEDLINE.

We have recently identified a new class of FtsZ-interacting compounds that possess a 2,4,6-trisubstituted pyrimidine-quinuclidine scaffold with moderate antibacterial activity. Employing this scaffold as a mol. template, a compound library of amine-linked 2,4,6-trisubstituted pyrimidines with ninety-nine candidates was successfully established by employing an efficient convergent synthesis designed to explore its structure activity relationship. The results of min. inhibitory concentration (MIC) assay against S. aureus strains and cytotoxicity assay against mouse L929 cell line identified those compounds with potent anti-staphylococcal properties (MIC ranges from 3 to 8 μg/mL) and some extent of cytotoxicity against normal cell (IC₅₀ ranges from 6 to 27 μM). Importantly, three compounds also exhibited potent antibacterial activities against nine clin. isolated MRSA strains. One of the compounds, I, exhibited low spontaneous frequency of resistance, low toxicity against G. mellonella larvae as well as the ability to rescue G. mellonella larvae (20% survival rate at dosage of 100 mg/Kg) infected with LD of MRSA ATCC 43300 strain. Biol. characterization of compound I by saturation transfer difference NMR, light scattering assay and GTPase hydrolysis assay with purified S. aureus FtsZ protein verified that it interacted with the FtsZ protein. Such property of FtsZ inhibitor was further confirmed by observations of iconic filamentous cell phenotype and mislocalization of the Z-ring formation of B. subtilis. Taken together, these 2,4,6-trisubstituted pyrimidine derivatives represent a novel scaffold of S. aureus FtsZ inhibitors.

ACS Omega 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, Quality Control of 87179-40-6.

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

Srikanth Reddy, T. published the artcileSemi-synthesis and bio-evaluation of polybrominated diphenyl ethers from the sponge Dysidea herbacea, Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(14), 4900-4906, database is CAplus and MEDLINE.

The sponge Dysidea herbacea was collected from the Mandapam Coast, Tamilnadu, India. Isolated gram quantities of hydroxylated polybrominated di-Ph ether (HO-PBDE) and semi-synthesized a series of new PBDEs derivatives and tested them for antibacterial and cytotoxic activities.

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 C22H21N3O3S, Recommanded Product: (E)-1-Cinnamylpiperazine.

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