Tag: M.W=250-300

Zhi, Yunbao published the artcileLead compounds and key residues of ribosomal protein S1 in drug-resistant Mycobacterium tuberculosis, Recommanded Product: 4-Iodo-3-(trifluoromethyl)-1H-pyrazole, the publication is Bioorganic Chemistry (2019), 58-67, database is CAplus and MEDLINE.

Ribosomal protein S1 (RpsA) has been identified as a novel target of pyrazinoic acid (POA), which is the active form of pyrazinamide (PZA), in vivo. RpsA plays a crucial role in trans-translation, which is widespread in microbes. In our investigation, we first described the discovery of promising RpsA antagonists for drug-resistant mycobacterium (MtRpsAd438A) and M. smegmatis, as well as wild-type M. tuberculosis. These antagonists were discovered via structure/ligand-based virtual screening approaches. A total of 21 targeted compounds were selected by virtual screening, combined scores, affinity, similarities and rules for potential as drugs. Next, the affinities of these compounds for three targeted proteins were tested in vitro by applying various technologies, including fluorescence quenching titration (FQT), saturation transfer difference (STD), and chem. shift perturbation (CSP) assays. The results showed that seven compounds had a high affinity for the targeted proteins. Our discovery set the stage for discovering new chem. entities (NCEs) for PZA-resistant tuberculosis and providing key residues for rational drug design to target RpsA.

Bioorganic Chemistry published new progress about 866638-72-4. 866638-72-4 belongs to iodides-buliding-blocks, auxiliary class Trifluoromethyl,Pyrazole,Fluoride,Iodide, name is 4-Iodo-3-(trifluoromethyl)-1H-pyrazole, and the molecular formula is C22H18O2, Recommanded Product: 4-Iodo-3-(trifluoromethyl)-1H-pyrazole.

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

Valero, Julian published the artcileA tetraguanidinium macrocycle for the recognition and cavity expansion of calix[4]arene tetraoxoanions, Synthetic Route of 606-55-3, the publication is Supramolecular Chemistry (2013), 25(9-11), 728-740, database is CAplus.

Mol. containers have raised an increased interest over the last decade. These supramol. architectures have found applications in catalysis, mol. sensing or as insulators for key intermediates, among others. In this study, we describe the synthesis and binding properties of a tetraguanidinium macrocycle which forms robust complexes with diverse calix[4]arene tetraoxoanions through hydrogen bonding and electrostatic interactions. The binding behavior and affinity strength of these constructs have been measured by NMR and isothermal titration calorimetry. Besides, VT NMR experiments show that this novel cyclic tetracation is able to stabilize the cone conformation of these calix[4]arenes. Preliminary NMR-binding experiments between a tetraguanidinium calix[4]arenate and quinolinium or isoquinolinium salts suggest an effective increase in the cavity volume of these supramol. constructs.

Supramolecular Chemistry published new progress about 606-55-3. 606-55-3 belongs to iodides-buliding-blocks, auxiliary class Quinoline,Salt, name is 1-Ethyl-2-methylquinolin-1-ium iodide, and the molecular formula is C7H8BFO2, Synthetic Route of 606-55-3.

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

Grignon-Dubois, Micheline published the artcileConvenient synthesis of (trichloromethyl)dihydroquinolines and -isoquinolines, SDS of cas: 606-55-3, the publication is Synthesis (1994), 800-4, database is CAplus.

The reaction of a series of N-alkylquinolinium and N-alkylisoquinolinium iodides towards sodium trichloroacetate in acetonitrile has been investigated under reflux or ultrasonication. In all cases, addition of trichloromethyl anion was observed, and trichloromethyldihydroquinoline or -isoquinoline derivatives were obtained in good yields. Depending on the activation process, addition occurred at the 2- or the 4-position with quinolines and at the 1-position with isoquinolines.

Synthesis published new progress about 606-55-3. 606-55-3 belongs to iodides-buliding-blocks, auxiliary class Quinoline,Salt, name is 1-Ethyl-2-methylquinolin-1-ium iodide, and the molecular formula is C12H14IN, SDS of cas: 606-55-3.

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

Kramer, Claus Ruediger published the artcileKinetics of reaction of formation of 2-amino-5-aryl-1,3,4-oxadiazoles from m- and p-substituted benzhydrazides and cyanogen bromide, Related Products of iodides-buliding-blocks, the publication is Zeitschrift fuer Chemie (1977), 17(12), 451-2, database is CAplus.

Kinetic data for the reaction of RC₆H₄CONHNH₂ (R = H, m– or p-Me, -NH₂, -NO₂, -OH, -OMe, -Cl, -Br, -I) with BrCN to form I indicated a dipolar addition mechanism with a cyclic transition state. A Hammett correlation yielded ρ = -0.215.

Zeitschrift fuer Chemie published new progress about 39115-95-2. 39115-95-2 belongs to iodides-buliding-blocks, auxiliary class Iodide,Hydrazine,Amine,Benzene,Hydrazide,Amide, name is 4-Iodobenzohydrazide, and the molecular formula is C7H7IN2O, Related Products of iodides-buliding-blocks.

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

Trofymchuk, Serhii published the artcileDeoxofluorination of (Hetero)aromatic Acids, Name: 2-Chloro-4-iodobenzoic acid, the publication is Journal of Organic Chemistry (2020), 85(5), 3110-3124, database is CAplus and MEDLINE.

Diverse trifluoromethyl-substituted compounds were synthesized by deoxofluorination of cinnamic and (hetero)aromatic carboxylic acids with sulfur tetrafluoride. The obtained products were used as starting materials in the preparation of novel fluorinated amino acids, anilines, and aliphatic amines – valuable building blocks for medicinal chem. and agrochem. Of note, sulfur tetrafluoride (SF4) and hydrogen fluoride (HF) are toxic, therefore, safety and addnl. tech. training must be taken before working with them.

Journal of Organic Chemistry published new progress about 145343-76-6. 145343-76-6 belongs to iodides-buliding-blocks, auxiliary class Chloride,Iodide,Carboxylic acid,Benzene, name is 2-Chloro-4-iodobenzoic acid, and the molecular formula is C13H18BClO2, Name: 2-Chloro-4-iodobenzoic acid.

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

Varinelli, Luca published the artcile4-IPP, a selective MIF inhibitor, causes mitotic catastrophe in thyroid carcinomas, Synthetic Route of 41270-96-6, the publication is Endocrine-Related Cancer (2015), 22(5), 759-775, database is CAplus and MEDLINE.

Macrophage migration inhibitory factor (MIF) is a pro-inflammatory cytokine that is over-expressed in several human neoplastic cells. When MIF binds its receptor (CD74) and co-receptor (CD44), it initiates signaling cascades that orchestrate cell proliferation and survival, and it can directly modulate the activity of AMPK. These activities indicate that MIF potentially regulates cell survival and metabolism We found that MIF was primarily co-expressed with CD74 in 16 out of 23 papillary thyroid carcinoma (PTC) and in all the 27 available anaplastic thyroid carcinoma (ATC) biopsy samples. MIF and CD74 were co-expressed in TPC-1 and HTC-C3 cell lines. The selective MIF inhibitor, 4-iodo-6-phenylpyrimidine (4-IPP), blocked MIF/CD74 internalization, activated JNK, and dose-dependently inhibited proliferation inducing apoptosis and mitotic cell death. In two CD74-neg. cell lines, NIM-1 and K1, 4-IPP treatment partially reduced proliferation. Coordinated MIF and CD74 expression appeared to confer in tumor cells the plasticity necessary to escape cell cycle regulation, metabolic changes, and stress conditions. MIF/CD74 signaling removal made cells susceptible to apoptosis and mitotic cell death. This finding suggests a possible avenue for targeting DNA endoreduplication, thus preventing the proliferation of therapy-resistant cell subpopulations. This study highlights MIF/CD74 axis as an important player in the biol. of aggressive thyroid neoplasms.

Endocrine-Related Cancer published new progress about 41270-96-6. 41270-96-6 belongs to iodides-buliding-blocks, auxiliary class Pyrimidine,Iodide,Benzene,Immunology/Inflammation,MIF, name is 4-Iodo-6-phenylpyrimidine, and the molecular formula is C8H15ClN2, Synthetic Route of 41270-96-6.

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

Zoraghi, Roya published the artcileDiscovery of a 1,2-bis(3-indolyl)ethane that selectively inhibits the pyruvate kinase of methicillin-resistant Staphylococcus aureus over human isoforms, Name: 4-Iodo-3-nitrobenzonitrile, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(21), 5059-5062, database is CAplus and MEDLINE.

Methicillin-resistant Staphylococcus aureus pyruvate kinase (MRSA PK) has recently been identified as a target for development of novel antibacterial agents. Testing a series of 1,2-bis(3-indolyl)ethanes against MRSA PK has led to the discovery of a potent inhibitor that is selective over human isoforms.

Bioorganic & Medicinal Chemistry Letters published new progress about 101420-79-5. 101420-79-5 belongs to iodides-buliding-blocks, auxiliary class Nitrile,Nitro Compound,Iodide,Benzene,Benzene Compounds, name is 4-Iodo-3-nitrobenzonitrile, and the molecular formula is C2H3N3, Name: 4-Iodo-3-nitrobenzonitrile.

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

Rizzo, M. Barbosa de Souza published the artcileOral squamous carcinoma cells promote macrophage polarization in an MIF-dependent manner, Application of 4-Iodo-6-phenylpyrimidine, the publication is QJM (2018), 111(11), 769-778, database is CAplus and MEDLINE.

Tumor-associated macrophages (TAMs) are important determinants of intratumoral immune evasion, neoangiogenesis, extracellular matrix remodeling and dysregulated tumor cell proliferation. Our prior studies revealed that macrophage-derived, but not tumor cell-derived, macrophage migration inhibitory factor (MIF), is an important determinant of TAM alternative activation and M2 polarization. Because MIF is historically thought to initiate signaling via a receptor-dependent, outside-in mode of action, we wished to investigate the specific contributions of tumor-derived vs. macrophage-derived MIF to M2 marker expression during macrophage polarization. Murine oral squamous cell-carcinoma cells (SCCVII) were co-cultured with either the RAW 264.7 mouse macrophage cell line or mouse primary bone marrow-derived macrophages in the context of MIF genetic loss/inhibition individually or in combination each cell type. Twelve well Transwell plates were used to co-culture SCCVII cells and RAW 264.7, MIF⁺/⁺ or MIF^–/^– macrophages treated with/without the small mol. MIF inhibitor, 4-iodo-6-phenylpyrimidine and incubated in the presence or absence of interleukin (IL-4) for 48 h. Macrophages were analyzed by quant. real-time polymerase chain reaction and/or immunoblotting for relative macrophage polarization marker expression. IL-4 treatment synergizes with SCCVII co-culture in inducing the expression of macrophage M2 markers and loss or inhibition of macrophage-derived MIF significantly reduces both IL-4 alone and IL-4/SCCVII co-culture-induced macrophage M2 marker expression. These studies identify an important and dominant requirement for macrophage MIF in maximal Th2-cytokine and oral squamous carcinoma cell-induced macrophage polarization and M2 marker expression.

QJM published new progress about 41270-96-6. 41270-96-6 belongs to iodides-buliding-blocks, auxiliary class Pyrimidine,Iodide,Benzene,Immunology/Inflammation,MIF, name is 4-Iodo-6-phenylpyrimidine, and the molecular formula is C10H7IN2, Application of 4-Iodo-6-phenylpyrimidine.

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

Niranjan, M. S. published the artcileSynthesis of 1,3,4-oxadiazole incorporated thiofibrates from substituted benzoic acids, Category: iodides-buliding-blocks, the publication is World Journal of Pharmacy and Pharmaceutical Sciences (2017), 6(11), 1085-1093, database is CAplus.

The present article describes the synthesis of 1,3,4-oxadiazole incorporated thiofibrates I (R = 4-NO₂, 4-Cl, 4-I, 3-Br, 4-Br) from substituted benzoic acids. Substituted benzoic acids reacted with methanol to obtain corresponding Me esters which was further converted into hydrazides by refluxing with hydrazine hydrate. Reaction of the above hydrazides with carbon disulfide in 10% potassium hydroxide yielded corresponding thiophenols incorporated with 1,3,4-oxadiazole. Ethyl-2-bromoisobutyrate in DMF converts these thiophenols into thiofibrates in presence of anhydrous potassium carbonate.

World Journal of Pharmacy and Pharmaceutical Sciences published new progress about 39115-95-2. 39115-95-2 belongs to iodides-buliding-blocks, auxiliary class Iodide,Hydrazine,Amine,Benzene,Hydrazide,Amide, name is 4-Iodobenzohydrazide, and the molecular formula is C7H7IN2O, Category: iodides-buliding-blocks.

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

Bao, Wenhu published the artcileSynthesis of 2-Amino-1,3,4-oxadiazoles through Elemental Sulfur Promoted Cyclization of Hydrazides with Isocyanides, Related Products of iodides-buliding-blocks, the publication is Chinese Journal of Chemistry (2017), 35(10), 1611-1618, database is CAplus.

A novel sulfur-promoted cyclization of hydrazides and isonitriles to produce 1,3,4-oxadiazoles has been developed. The method is operationally simple and compatible with a wide scope of substrates and various 2-amino-1,3,4-oxadiazoles are efficiently obtained in good yields.

Chinese Journal of Chemistry published new progress about 39115-95-2. 39115-95-2 belongs to iodides-buliding-blocks, auxiliary class Iodide,Hydrazine,Amine,Benzene,Hydrazide,Amide, name is 4-Iodobenzohydrazide, and the molecular formula is C7H7IN2O, Related Products of iodides-buliding-blocks.

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