Month: April 2022

HPLC of Formula: 22353-34-0. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 5-Chloropyridin-3-amine, is researched, Molecular C5H5ClN2, CAS is 22353-34-0, about First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. Author is Hamed, Mostafa M.; Darwish, Sarah S.; Herrmann, Jennifer; Abadi, Ashraf H.; Engel, Matthias.

The activation of the NF-κB transcription factor is a major adaptive response induced upon treatment with EGFR kinase inhibitors, leading to the emergence of resistance in nonsmall cell lung cancer and other tumor types. To suppress this survival mechanism, we developed new thiourea quinazoline derivatives that are dual inhibitors of both EGFR kinase and the NF-κB activity. Optimization of the hit compound, identified in a NF-κB reporter gene assay, led to compound 9b, exhibiting a cellular IC50 for NF-κB inhibition of 0.3 μM while retaining a potent EGFR kinase inhibition (IC50 = 60 nM). The dual inhibitors showed a higher potency than gefitinib to inhibit cell growth of EGFR-overexpressing tumor cell lines in vitro and in a xenograft model in vivo, while no signs of toxicity were observed An investigation of the mol. mechanism of NF-κB suppression revealed that the dual inhibitors depleted the transcriptional coactivator CREB-binding protein from the NF-κB complex in the nucleus.

There is still a lot of research devoted to this compound(SMILES：NC1=CC(=CN=C1)Cl)HPLC of Formula: 22353-34-0, and with the development of science, more effects of this compound(22353-34-0) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-(11bR)-Dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-yl-5H-dibenz[b,f]azepine( cas:1265884-98-7 ) is researched.Computed Properties of C34H22NO2P.Zhou, Yuan; Xiong, Tong; Zhou, Li-Yan; Li, Hong-Yan; Xiao, You-Cai; Chen, Fen-Er published the article 《Diastereo- and Enantioselective Synthesis of Borylated 3-Hydroxyoxindoles by Addition of gem-Diborylalkanes to Isatins》 about this compound( cas:1265884-98-7 ) in Organic Letters. Keywords: chiral hydroxyoxindole preparation reactivity stereoselective; crystal structure mol borylated hydroxyoxindole preparation; diastereoselective enantioselective stereoselective borylation hydroxyoxindole addition diborylalkane isatin. Let’s learn more about this compound (cas:1265884-98-7).

The catalytic asym. synthesis of borylated 3-hydroxyoxindoles by addition of gem-diborylalkanes to isatins is disclosed. Chiral 3-hydroxyoxindoles bearing two contiguous stereogenic centers were produced in up to >20:1 dr and 99% ee. The synthetic utility of the corresponding products is presented through several transformations of the boryl moiety. This report provides an efficient strategy to incorporate a boryl functional group toward the synthesis of 3-hydroxyoxindoles.

There is still a lot of research devoted to this compound(SMILES：N1(P2OC3=CC=C4C=CC=CC4=C3C5=C6C=CC=CC6=CC=C5O2)C7=CC=CC=C7C=CC8=CC=CC=C81)Computed Properties of C34H22NO2P, and with the development of science, more effects of this compound(1265884-98-7) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Wang, Haiqi; Song, Hongjian published an article about the compound: H-Trp-OMe.HCl( cas:7524-52-9,SMILESS:N[C@@H](CC1=CNC2=CC=CC=C12)C(OC)=O.[H]Cl ).Formula: C12H15ClN2O2. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:7524-52-9) through the article.

Previously, we reported for the first time that harmala alkaloids harmine and tetrahydroharmine exhibit activity against plant viruses, and we developed an analog, designated NK0209, that efficiently prevents and controls plant virus diseases. Here, to investigate the influence of the spatial configuration of NK0209 on its antiviral activities, we synthesized its four optical isomers, determined their configurations, and evaluated their activities against tobacco mosaic virus. All four isomers were significantly more active than ningnanmycin, which is one of the most successful com. antiviral agents, with in vivo inactivation, cure, and protection rates of 57.3±1.9%, 54.2±3.3%, 55.0±4.1% at 500μg/mL. Furthermore, anal. of structure-activity relationships demonstrated for the first time that the spatial conformation of NK0209 is an important determinant of its antiviral activity, and our results provide information about the possible optimum configuration for interaction of this mol. with its target protein.

There is still a lot of research devoted to this compound(SMILES：N[C@@H](CC1=CNC2=CC=CC=C12)C(OC)=O.[H]Cl)Formula: C12H15ClN2O2, and with the development of science, more effects of this compound(7524-52-9) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Development, characterization and pharmacological evaluation of amino acid prodrugs of (+)-Ibuprofen.Formula: C12H15ClN2O2.

The current research work investigate the neuronal pathway associated with NSAIDs that lead to the reduction in the initiation and progression of neurodegenerative diseases such as Alzheimer’s disease, Parkinsonism, etc. This research was developed amino acid prodrugs of the active enantiomer of ibuprofen, (+)-IBN and checks the pharmacol. effects, neuroprotective effect, anti inflammatory effect and anti-ulcerogenic effect. The treatment using (+)-IBN reduced the action of micoglia and the release of cytokine especially TNFα that are mainly involved in the neurodegenerative process. (+)- IBN reduced the deposition of soluble beta amyloid plaque by inhibiting the amyloid precursor protein, beta-secretase 1 and also enhancing the degradation process of beta amyloid via induction of insulin degrading enzyme. (+)-IBN also showed the property that the reduction in the TAU misfolding process. Therefore, the synthesized (+)-IBN amino acid prodrugs treatment effectively produce neuroprotective action, both restoring memory realed risk factors and reversing multiple brain neuropathol. hallmarks. The current research study developed the three amino acid prodrugs of (+)-ibuprofen by conjugating with L-Ph alanine, L-tryptophan and L-tyrosine also the physico-chem. characterization and spectral characterization was done. This study modify the carboxylic acid functional group present in the NSAIDs that lead to the formation of prodrugs with enhanced anti-inflammatory activity, reduced side effects and protective effect against neurodegenerative processes.

There is still a lot of research devoted to this compound(SMILES：N[C@@H](CC1=CNC2=CC=CC=C12)C(OC)=O.[H]Cl)Formula: C12H15ClN2O2, and with the development of science, more effects of this compound(7524-52-9) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

COA of Formula: C5H5ClN2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 5-Chloropyridin-3-amine, is researched, Molecular C5H5ClN2, CAS is 22353-34-0, about The synthesis, structure-toxicity relationship of cisplatin derivatives for the mechanism research of cisplatin-induced nephrotoxicity.

Cisplatin is a widely used antineoplastic drug, while its nephrotoxicity limits the clin. application. Although several mechanisms contributing to nephrotoxicity are reported, the direct protein targets are unclear. Herein the authors reported the synthesis of 29 cisplatin derivatives and the structure-toxicity relation (STR) of these compounds with MTT assay in human renal proximal tubule cells (HK-2) and pig kidney epithelial cells (LLC-PK1). To the best of the authors’ knowledge, this study represented the 1st report regarding the structure-toxicity relation (STR) of cisplatin derivatives The potency of biotin-pyridine conjugated derivative 3 met the requirement for target identification, and the preliminary chem. proteomics results suggested that it is a promising tool for further target identification of cisplatin-induced nephrotoxicity.

There is still a lot of research devoted to this compound(SMILES：NC1=CC(=CN=C1)Cl)COA of Formula: C5H5ClN2, and with the development of science, more effects of this compound(22353-34-0) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Feng, Rui; Jie, Suyun; Braunstein, Pierre; Li, Bo-Geng published an article about the compound: 5-Chloropyridin-3-amine( cas:22353-34-0,SMILESS:NC1=CC(=CN=C1)Cl ).Name: 5-Chloropyridin-3-amine. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:22353-34-0) through the article.

The ring-opening polymerization (ROP) of lactones is an effective method for the preparation of biocompatible and biodegradable aliphatic polyesters, for which the development of efficient organocatalysts with high activity and good controllability is highly desirable. A series of novel pyridyl-urea catalysts was synthesized and applied in the solvent-free ROP of lactones and trimethylene carbonate. Combined with 7-methyl-1,5,7-triazabicyclo[4.4.0]dec-5-ene (MTBD), the pyridyl-urea/MTBD systems showed a fast and living/controlled behavior in the ROP, generating polymers with narrow mol. weight distributions. The influences of catalyst structure, type of base, pyridyl-urea/base ratio, feed ratio of monomer/initiator and reaction temperature on the catalytic properties were investigated. A possible mechanism was proposed on the basis of NMR titration and dilution experiments

There is still a lot of research devoted to this compound(SMILES：NC1=CC(=CN=C1)Cl)Name: 5-Chloropyridin-3-amine, and with the development of science, more effects of this compound(22353-34-0) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 2-Bromo-6-(bromomethyl)naphthalene( cas:305798-02-1 ) is researched.HPLC of Formula: 305798-02-1.Zore, Matej; Gilbert-Girard, Shella; Reigada, Ines; Patel, Jayendra Z.; Savijoki, Kirsi; Fallarero, Adyary; Yli-Kauhaluoma, Jari published the article 《Synthesis and Biological Evaluation of Fingolimod Derivatives as Antibacterial Agents》 about this compound( cas:305798-02-1 ) in ACS Omega. Keywords: fingolimod preparation antibacterial anticancer human. Let’s learn more about this compound (cas:305798-02-1).

To study if the antibacterial activity of fingolimod could be further improved and to explore in-depth structure-activity relationships, 28 novel fingolimod derivatives I [R1 = 4-PhCH2C6H4, 4-OBnC6H4, 5-octyl-2-pyridyl, etc.; n = 1, 2], II [R2 = octyl, decyl] and III [R3 = H, octyl, decyl; R4 = H, octyl; Z = CH, N; m = 1, 2] were synthesized and evaluated their efficacy against Staphylococcus aureus grown in planktonic/single cell and biofilms. The most effective derivatives were tested on preformed S. aureus biofilms and against Gram-neg. bacteria Acinetobacter baumannii and Pseudomonas aeruginosa, using fingolimod as the reference compound Seven derivatives were more effective against S. aureus, while five other derivatives showed improved activity against P. aeruginosa and/or A. baumannii, with no apparent change in cytotoxicity on human cells. The most interesting derivatives, compounds I [R1 = 3-octylphenyl, n = 2] and II [R2 = decyl], displayed a broader spectrum of antibacterial activity, possibly exerted by the change of the para-hydrocarbon chain to a meta position for compound I [R1 = 3-octylphenyl, n = 2] and by an addnl. hydroxyl group for compound II [R2 = decyl].

There is still a lot of research devoted to this compound(SMILES：BrCC1=CC2=CC=C(Br)C=C2C=C1)HPLC of Formula: 305798-02-1, and with the development of science, more effects of this compound(305798-02-1) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Novel synthesis and structure of phosphanyl sugar derivatives, published in 1997-07-31, which mentions a compound: 707-61-9, Name is 4-Methyl-1-phenyl-2,3-dihydro-1H-phosphole 1-oxide, Molecular C11H13OP, Category: dioxole.

Some phosphanyl sugars, e.g. I, which are analogs of sugars having a phosphorus atom in place of the ring oxygen, were synthesized from 2- and 3-phospholenes as starting materials. Catalytic cis-dihydroxylation of 2-phospholene or 3-phospholene 1-oxide derivatives with osmium(VIII) oxide in the presence of a Co-oxidant afforded 3-deoxy- or 1-deoxy-tetrofuranose-type phosphanyl sugar derivatives, resp. Cis-Dihydroxylation of 4-acyloxy-2-phospholene 1-oxide derivatives gave tetrofuranose type phosphanyl sugar derivatives Some of these derivatives of phosphanyl sugars were subjected to structural analyses using 1H NMR and X-ray crystallog.

There is still a lot of research devoted to this compound(SMILES：CC1=CP(CC1)(C2=CC=CC=C2)=O)Category: dioxole, and with the development of science, more effects of this compound(707-61-9) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Origin of Stereodivergence in Cooperative Asymmetric Catalysis with Simultaneous Involvement of Two Chiral Catalysts, published in 2015-12-23, which mentions a compound: 1265884-98-7, Name is 5-(11bR)-Dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-yl-5H-dibenz[b,f]azepine, Molecular C34H22NO2P, Name: 5-(11bR)-Dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-yl-5H-dibenz[b,f]azepine.

Accomplishing high diastereo- and enantioselectivities simultaneously is a persistent challenge in asym. catalysis. The use of two chiral catalysts in one-pot conditions might offer new avenues to this end. Chirality transfer from a catalyst to product gets increasingly complex due to potential chiral match-mismatch issues. The origin of high enantio- and diastereoselectivities in the reaction between a racemic aldehyde and an allyl alc., catalyzed by using axially chiral iridium phosphoramidites PR/S-Ir and cinchona amine is established through transition-state modeling. The multipoint contact anal. of the stereocontrolling transition state revealed how the stereodivergence could be achieved by inverting the configuration of the chiral catalysts that are involved in the activation of the reacting partners. While the enantiocontrol is identified as being decided in the generation of PR/S-Ir-π-allyl intermediate from the allyl alc., the diastereocontrol arises due to the differential stabilizations in the C-C bond formation transition states. The anal. of the weak interactions in the transition states responsible for chiral induction revealed that the geometric disposition of the quinoline ring at the C8 chiral carbon of cinchona-enamine plays an anchoring role. The quinolone ring is noted as participating in a π-stacking interaction with the Ph ring of the Ir-π-allyl moiety in the case of PR with the (8R,9R)-cinchona catalyst combination, whereas a series of C-H···π interactions is identified as vital to the relative stabilization of the stereocontrolling transition states when PR is used with (8S,9S)-cinchona.

There is still a lot of research devoted to this compound(SMILES：N1(P2OC3=CC=C4C=CC=CC4=C3C5=C6C=CC=CC6=CC=C5O2)C7=CC=CC=C7C=CC8=CC=CC=C81)Name: 5-(11bR)-Dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-yl-5H-dibenz[b,f]azepine, and with the development of science, more effects of this compound(1265884-98-7) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 6,7-Dichlorobenzo[d]thiazol-2-amine( cas:25150-27-0 ) is researched.HPLC of Formula: 25150-27-0.Baldaniya, B. B. published the article 《Synthesis and characterizations of N2-(aryl)-N4,N6-bis(6,7-dichloro-1,3-benzothiazol-2-yl)-1,3,5-triazine-2,4,6-triamines as biological potent agents》 about this compound( cas:25150-27-0 ) in E-Journal of Chemistry. Keywords: cyanuric chloride condensation thiazolamine; thiazolyl cyanuric chloride preparation reaction aryl amine; arylamino chlorobenzothiazolylamino triazine preparation antibacterial antifungal activity. Let’s learn more about this compound (cas:25150-27-0).

Some novel N2-(aryl)-N4,N6-bis(6,7-dichloro-1,3-benzothiazol-2-yl)-1,3,5-triazine-2,4,6-triamines were synthesized and characterized by elemental analyses, IR, NMR, and mass spectra. The products were tested for their antibacterial activity against gram (+)ve and gram (-)ve bacteria and also on different strains of fungi. Introduction of -OH, -OCH3, -NO2, -Cl and -Br groups to the heterocyclic frame work enhanced antibacterial and antifungal activities.

There is still a lot of research devoted to this compound(SMILES：NC1=NC2=CC=C(Cl)C(Cl)=C2S1)HPLC of Formula: 25150-27-0, and with the development of science, more effects of this compound(25150-27-0) can be discovered.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem