Tag: M.W=150-200

Jagerovic, Nadine published the artcileDiscovery of 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole, a Novel in Vivo Cannabinoid Antagonist Containing a 1,2,4-Triazole Motif, Computed Properties of 2447-79-2, the publication is Journal of Medicinal Chemistry (2004), 47(11), 2939-2942, database is CAplus and MEDLINE.

A new series of 1,2,4-triazoles have been prepared and the evaluation of their cannabinoid properties have been carried out. The title compound, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole (I) showed cannabinoid silent antagonist activity in mouse vas deferens and guinea pig ileum preparations and in vivo assays (cannabinoid tetrad) in mouse. It did not have intrinsic activity in these bioassays, and therefore, it did not behave as a partial agonist or an inverse agonist. Mol. modeling of I was carried out on Δ⁹-tetrahydrocannabinoic acid B.

Journal of Medicinal Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Computed Properties of 2447-79-2.

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

Smith, Christine C. published the artcileThe synthesis and application of a diazirine-modified uridine analogue for investigating RNA-protein interactions, COA of Formula: C6H10F3NO, the publication is RSC Advances (2014), 4(89), 48228-48235, database is CAplus.

The roles played by many ncRNAs remain largely unknown. Similarly, relatively little is known about the RNA binding proteins involved in processing ncRNA. Identification of new RNA/RNA binding protein (RBP) interactions may pave the way to gain a better understanding of the complex events occurring within cells during gene expression and ncRNA biogenesis. The development of chem. tools for the isolation of RBPs is of paramount importance. In this context, we report on the synthesis of the uridine phosphoramidite U^Dz that bears a diazirine moiety on the nucleobase. RNA probes containing U^Dz units were irradiated in the presence of single-stranded DNA binding protein (SSB), which is also known to bind ssRNAs, and shown to efficiently (15% yield) and selectively cross-link to the protein. The corresponding diazirine-modified uridine triphosphate U^DzTP was synthesized and its capacity to act as a substrate for the T7 RNA polymerase was tested in transcription assays. U^DzTP was accepted with a maximum yield of 38% for a 26mer RNA containing a single incorporation and 28% yield for triple consecutive incorporations. Thus, this uridine analog represents a convenient biochem. tool for the identification of RNA binding proteins and unraveling the role and function played by ncRNAs.

RSC Advances published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C7H13ClNNaO5S, COA of Formula: C6H10F3NO.

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

Morita, Mikio published the artcileFacile synthesis of 2-azaazulenes from thiobenzoyl isocyanates using trimethylsilyldiazomethane, Related Products of amides-buliding-blocks, the publication is Tetrahedron (2008), 64(8), 1753-1758, database is CAplus.

The reaction of trimethylsilyldiazomethane with thiobenzoyl isocyanates, in situ generated from thiazole-4,5-diones, yielded diazo ketones, which were converted into 2-azaazulenes by the intramol. Buchner reaction.

Tetrahedron published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Related Products of amides-buliding-blocks.

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

Albrecht, Brian K. published the artcileDiscovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase, Product Details of C8H9BFNO3, the publication is Journal of Medicinal Chemistry (2008), 51(10), 2879-2882, database is CAplus and MEDLINE.

Tumorigenesis is a multistep process in which oncogenes play a key role in tumor formation, growth, and maintenance. MET was discovered as an oncogene that is activated by its ligand, hepatocyte growth factor. Deregulated signaling in the c-Met pathway has been observed in multiple tumor types. Herein we report the discovery of potent and selective triazolopyridazine small mols. that inhibit c-Met activity.

Journal of Medicinal Chemistry published new progress about 849833-86-9. 849833-86-9 belongs to amides-buliding-blocks, auxiliary class Fluoride,Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester, name is (3-Fluoro-4-(methylcarbamoyl)phenyl)boronic acid, and the molecular formula is C8H9BFNO3, Product Details of C8H9BFNO3.

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

Fier, Patrick S. published the artcileSelective C-H Fluorination of Pyridines and Diazines Inspired by a Classic Amination Reaction, Name: N,N-Diethylisonicotinamide, the publication is Science (Washington, DC, United States) (2013), 342(6161), 956-960, database is CAplus and MEDLINE.

Fluorinated heterocycles are prevalent in pharmaceuticals, agrochems., and materials. However, reactions that incorporate fluorine into heteroarenes are limited in scope and can be hazardous. The authors present a broadly applicable and safe method for the site-selective fluorination of a single carbon-hydrogen bond in pyridines and diazines using com. available silver(II) fluoride. The reactions occur at ambient temperature within 1 h with exclusive selectivity for fluorination adjacent to nitrogen. The mild conditions allow access to fluorinated derivatives of medicinally important compounds, as well as a range of 2-substituted pyridines prepared by subsequent nucleophilic displacement of fluoride. Mechanistic studies demonstrate that the pathway of a classic pyridine amination can be adapted for selective fluorination of a broad range of nitrogen heterocycles.

Science (Washington, DC, United States) published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H14N2O, Name: N,N-Diethylisonicotinamide.

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

Wang, Jinhui published the artcileFar-red light-mediated programmable anti-cancer gene delivery in cooperation with photodynamic therapy, Synthetic Route of 1869-45-0, the publication is Biomaterials (2018), 72-82, database is CAplus and MEDLINE.

Effective anti-cancer therapy is hurdled by the complicated extracellular and intracellular barriers, and thus a smart gene vector that can enable programmable gene delivery is highly demanded. Photo-manipulation of gene delivery processes features spatial and temporal precision, while majority of current strategies utilizes short-wavelength UV/visible light with poor tissue penetration or high-power-d. near-IR (NIR) light that would cause undesired heat damage. Herein, an ROS-degradable polycation was designed and co-delivered with a photosensitizer (PS), thus realizing photo-programmable gene delivery using far-red light (661 nm) at low optical power d. (down to 5 mW cm^-2). Thioketal-crosslinked polyethylenimine (TK-PEI) was synthesized to condense p53 gene to form nanocomplexes (NCs), and hyaluronic acid (HA) modified with pheophytin a (Pha) was coated onto NCs to enhance their colloidal stability and enable cancer cell targeting. Short-time (8-min) light irradiation produced non-lethal amount of ROS to disrupt the endosomal membranes and facilitate p53 gene release via degradation of TK-PEI, which collectively enhanced p53 expression levels toward anti-cancer gene therapy. Long-time (30-min) light irradiation at the post-transfection state generated lethal amount of ROS, which cooperatively killed cancer cells to strengthen p53 gene therapy. To the best of our knowledge, this study represents the first example of an “one stone, three birds” approach to realize cooperative anti-cancer gene therapy using low-power-d., long-wavelength visible light as a single stimulus.

Biomaterials published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H4N2O2, Synthetic Route of 1869-45-0.

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

Reed, Kathryn L. published the artcileA mild and convenient oxidation of aryl nitriles to aryl amides by aqueous sodium perborate, Formula: C7H5Cl2NO, the publication is Synthetic Communications (1990), 20(4), 563-71, database is CAplus.

Treatment of aryl nitriles with NaBO₃.4H₂O in aqueous dioxane gives the corresponding benzamides in 13-85% yields. E.g., 3,5-Cl₂C₆H₃CN gives 74% 3,5-Cl₂C₆H₃CONH₂. The effect of substrate structure on yield is discussed.

Synthetic Communications published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Formula: C7H5Cl2NO.

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

Wang, Changliu published the artcileYnamide-Mediated Thioamide and Primary Thioamide Syntheses, Safety of 3-Methoxybenzothioamide, the publication is Journal of Organic Chemistry (2022), 87(9), 5617-5629, database is CAplus and MEDLINE.

Environmentally friendly ynamide-mediated thioamidation of monothiocarboxylic acids with amines or ammonium hydroxide for the synthesis of thioamides was described. Simple and mild reaction conditions tolerate a wide variety of functional groups such as hydroxyl, ester, tertiary amine, ketone, and amide moieties. Readily available NaSH served as the sulfur source, avoiding the use of toxic, expensive, and malodorous organic sulfur reagents and making this strategy environmentally friendly and practical. Importantly, the stereochem. integrity of α-chiral monothiocarboxylic acids was maintained during the activation step and subsequent aminolysis process, which offers a racemization-free strategy for peptide and protein C-terminal modification. Furthermore, a number of thioamide-modified drugs were prepared in good yields by this protocol and the synthesized primary thioamides were transformed into backbone thiazolyl modification peptides.

Journal of Organic Chemistry published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C15H20O6, Safety of 3-Methoxybenzothioamide.

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

Lin, Songwen published the artcileIdentification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors, Synthetic Route of 100377-32-0, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(3), 790-793, database is CAplus and MEDLINE.

Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors. Design, synthesis and structure activity relationship are reported.

Bioorganic & Medicinal Chemistry Letters published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C8H10N2O2, Synthetic Route of 100377-32-0.

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

Wu, Zining published the artcileCell-Based Selection Expands the Utility of DNA-Encoded Small-Molecule Library Technology to Cell Surface Drug Targets: Identification of Novel Antagonists of the NK3 Tachykinin Receptor, Computed Properties of 475216-25-2, the publication is ACS Combinatorial Science (2015), 17(12), 722-731, database is CAplus and MEDLINE.

DNA-encoded small-mol. library technol. has recently emerged as a new paradigm for identifying ligands against drug targets. To date, this technol. has been used with soluble protein targets that are produced and used in a purified state. Here, we describe a cell-based method for identifying small-mol. ligands from DNA-encoded libraries against integral membrane protein targets. We use this method to identify novel, potent, and specific inhibitors of NK3, a member of the tachykinin family of G-protein coupled receptors (GPCRs). The method is simple and broadly applicable to other GPCRs and integral membrane proteins. We have extended the application of DNA-encoded library technol. to membrane-associated targets and demonstrate the feasibility of selecting DNA-tagged, small-mol. ligands from complex combinatorial libraries against targets in a heterogeneous milieu, such as the surface of a cell.

ACS Combinatorial Science published new progress about 475216-25-2. 475216-25-2 belongs to amides-buliding-blocks, auxiliary class Fluoride,Nitro Compound,Amine,Benzene,Amide,Benzene Compounds, name is 4-Fluoro-N-methyl-3-nitrobenzamide, and the molecular formula is C9H9ClN2, Computed Properties of 475216-25-2.

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