Month: December 2022

Ling, Xiaoxi published the artcileSynthesis of a reactive oxygen species responsive heterobifunctional thioketal linker, Application In Synthesis of 1869-45-0, the publication is Tetrahedron Letters (2015), 56(37), 5242-5244, database is CAplus and MEDLINE.

A new heterobifunctional reactive oxygen species (ROS) responsive thioketal linker and its synthesis are described. This linker allows for developing new ROS-responsive agents with two distinct functionalities using universal bioconjugation methods. The reaction kinetics of the thioketal cleavage in the presence of ROS is also described.

Tetrahedron Letters 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 C4H6F3NOS, Application In Synthesis of 1869-45-0.

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

Wang, Da-Wei published the artcileDiscovery of Novel N-Isoxazolinylphenyltriazinones as Promising Protoporphyrinogen IX Oxidase Inhibitors, SDS of cas: 372136-76-0, the publication is Journal of Agricultural and Food Chemistry (2019), 67(45), 12382-12392, database is CAplus and MEDLINE.

Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) is a promising target for herbicide discovery. Search for new compounds with novel chemotypes is a key objective for agrochemists. Here, we describe the discovery and systematic SAR-based structure optimization of novel N-isoxazolinyl-phenyl-triazinones as PPO inhibitors. The in vivo herbicidal activity and in vitro Nicotiana tabacum PPO (NtPPO) inhibitory activity were explored in detail. A number of the new synthetic compounds displayed strong PPO inhibitory activity with Ki values in the nanomolar range. Some compounds exhibited excellent and broad-spectrum weeds control at the rate of 9.375-37.5 g ai/ha by postemergence application, and showed improved monocotyledonous weeds control compared to saflufenacil. Most promisingly, Et 3-(2-chloro-5-(3,5-dimethyl-2,6-dioxo-4-thioxo-1,3,5-triazinan-1-yl)-4-fluorophenyl)-5-methyl-4,5-dihydroisoxazole-5-carboxylate (I), with a Ki value of 4.9 nM, displayed over 2- and 6-fold higher potency than saflufenacil (Ki = 10 nM) and trifludimoxazin (Ki = 31 nM), resp. Moreover, I showed excellent and broad-spectrum weeds control against 32 kinds of weeds at 37.5-75 g ai/ha. Rice exhibited relative tolerance to I at 150 g ai/ha by post-emergence application, indicated that I could be a potential herbicide candidate for weed control in paddy fields.

Journal of Agricultural and Food Chemistry published new progress about 372136-76-0. 372136-76-0 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Amine,Aliphatic hydrocarbon chain, name is N-Methyl-N-isopropylsulfamoyl amide, and the molecular formula is C22H32O2, SDS of cas: 372136-76-0.

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

Qian, Xuhong published the artcileSyntheses and insecticidal activities of novel 2,5-disubstituted-1,3,4-oxadiazoles, Application of 2,4-Dichlorobenzamide, the publication is Journal of Chemical Technology & Biotechnology (1996), 67(2), 124-130, database is CAplus.

A series of sym. and asym. 2,5-disubstituted-1,3,4-oxadiazoles were prepared Thus, title compound I (preparation given) gave 91% kill of Drosophila melanogaster eggs at 100 ppm. Insecticidal activities of title compounds against Drosophila melanogaster were recorded and anal. of structure-activity relationships showed that the HOMO energy (E_H) was the main factor affecting bioactivity.

Journal of Chemical Technology & Biotechnology 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, Application of 2,4-Dichlorobenzamide.

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

Qin, Xiaohan published the artcileA carrier-free photodynamic nanodrug to enable regulation of dendritic cells for boosting cancer immunotherapy, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Acta Biomaterialia (2022), 366-376, database is CAplus and MEDLINE.

Immune response is initiated by dendritic cells (DCs), where the cross-presentation of antigens by DCs determines the activating of cytotoxic T cells. However, the efficacy of DCs-initiated immune response is governed by multiple (cascade) steps of immunogenic cell death (ICD), recruitment of DCs, and cross-presentation of DCs. It is urgent but challenging to achieve a platform for simultaneously regulating these multiple steps, amplifying the immune response against tumors. Herein, we reported a photodynamic nanodrug enabling simultaneous regulation of these multiple steps for realizing powerful immune response. The nanodrug was designed by the co-assembling of chlorin e6 (Ce6), celecoxib and 6-thio-2’deoxyguanosine (6-thio-dG). In our nanodrug, Ce6 enables induction of ICD, while celecoxib down-regulates the prostaglandin E2 (PGE2) for promoting recruitment of DCs enabled by chemokine CCL5 produced from natural killer (NK) cells. Moreover, 6-thio-dG triggers DNA damages in the tumor cells, which in turn activates STING/interferon I pathway for enhancing the cross-presentation ability of DCs. Therefore, an amplified immune therapeutic effect against tumors is achieved, thanks to the simultaneous regulation of these multiple steps. The nanodrug effectively inhibits tumor growth and postoperative recurrence, demonstrating a new approach for boosting immune response initiated by DCs in cancer therapy. The dendritic cells (DCs)-initiated immune response against tumors is dominated by multiple (cascade) steps including the process of (I) immunogenic cell death (ICD), (II) recruitment of DCs, and (III) cross-presentation of antigens by DCs. Based on this, it is urgent to design a nanoplatform enabling simultaneous regulation of these multiple steps for achieving a potent therapeutic efficacy. A carrier-free photodynamic nanodrug, engineered by a co-assembling approach, was designed to regulate DCs for realizing a powerful DCs-initiated immune response against tumors, thanks to the simultaneous regulation of the above multiple steps. Our nanodrug demonstrated a boosted immune response against tumors, powerfully suppressing primary/abscopal tumor growth and postoperative recurrence, which offers a conceptually innovative strategy for amplifying immunity against tumors.

Acta Biomaterialia published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

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

You, Tingjie published the artcileRuthenium(II)-catalyzed reductive N-O bond cleavage of N-OR (R = H, alkyl, or acyl) substituted amides and sulfonamides, Category: amides-buliding-blocks, the publication is Organic Chemistry Frontiers (2021), 8(1), 112-119, database is CAplus.

With a com. available ruthenium(II) catalyst and a mixture of HCOOH/NEt₃ as the hydride source under an air atm., a convenient method for the reductive cleavage of N-O bonds was described. This catalytic system was applicable for a variety of N-oxygen-substituted amides, as well as N-alkoxy sulfonamides, efficiently delivering the corresponding amide RCONHR¹R² [R = Ph, 1-naphthyl, 2-thienyl, etc.; R¹ = H, Me; R² = OH, OMe, OEt, etc.] or primary sulfonamide R³SO₂NH₂ [R³ = Ph, 2-MeC₆H₄, 4-MeC₆H₄, Bn] products with good functional group tolerance in moderate to good yields.

Organic Chemistry Frontiers published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C12H6NNaO4, Category: amides-buliding-blocks.

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

Wang, Man published the artcileNeighboring Thioether Participation in Bioinspired Radical Oxidative C(sp³)-H α-Oxyamination of Pyruvate Derivatives, Name: 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, the publication is Organic Letters (2020), 22(22), 8941-8946, database is CAplus and MEDLINE.

A bioinspired radical oxidative α-oxyamination of pyruvate with an oxoammonium salt through multiple-site concerted proton-electron transfer process has been developed, which was facilitated by anchoring the mercapto chains as a “hopping” site at the γ-position of α-keto esters.

Organic Letters 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 C11H15NOS, Name: 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide.

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

Fu, Niankai published the artcileAsymmetric Sulfa-Michael Addition to α-Substituted Vinyl Ketones Catalyzed by Chiral Primary Amine, HPLC of Formula: 1869-45-0, the publication is Organic Letters (2014), 16(17), 4626-4629, database is CAplus and MEDLINE.

The first effective example of asym. conjugate addition-protonation reactions of thiols to α-substituted vinyl ketones by chiral primary amine catalysis is reported. A simple chiral primary-tertiary diamine catalyst derived from L-phenylalanine, I, was found to promote the sulfa-Michael addition-protonation reactions with good to excellent enantioselectivity. Thus, reacting thiol F₃CCONH(CH₂)₂SH with MeC(COPh):CH₂ in the presence of I gave sulfur-containing amide-ketone II.

Organic Letters 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 C4H6F3NOS, HPLC of Formula: 1869-45-0.

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

Hankore, Erome Daniel published the artcileGenetic incorporation of noncanonical amino acids using two mutually orthogonal quadruplet codons, Safety of H-Lys(Boc)-OH, the publication is ACS Synthetic Biology (2019), 8(5), 1168-1174, database is CAplus and MEDLINE.

Genetic incorporation of noncanonical amino acids has emerged as a powerful tool for the study of protein structure and function. While the three triplet nonsense codons have been widely explored, quadruplet codons have attracted attention for the potential of creating addnl. blank codons for noncanonical amino acid mutagenesis. Here we demonstrated for the first time that two orthogonal quadruplet codons could be used to simultaneously encode two different noncanonical amino acids within a single protein in bacterial cells. To achieve this, we fine-tuned the interaction between aminoacyl-tRNA synthetase and tRNA, which afforded up to 21-fold improvement in quadruplet codon decoding efficiency. This work represents a significant step toward the use of multiple quadruplet codons for noncanonical amino acid mutagenesis. Simultaneous incorporation of two or more noncanonical amino acids is of significant importance for biol. applications that can benefit from multiple unique functional groups, such as fluorescence resonance energy transfer and NMR studies, and ultimately for the synthesis of completely unnatural biopolymers as new biomaterials.

ACS Synthetic Biology published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Safety of H-Lys(Boc)-OH.

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

Zheng, Deqiang published the artcileSynthesis of regorafenib, Synthetic Route of 1019206-88-2, the publication is Zhongguo Yiyao Gongye Zazhi (2016), 47(5), 528-530, database is CAplus.

Regorafenib was synthesized from 3-fluoro-4-nitrophenol (2) via reduction nitro group, nucleophilic substitution with N-methyl-4-chloropyridine-2-carboxamide (5), condensation with 4-chloro-3-(trifluoromethyl) Ph isocyanate (8), and then recrystallization by salt formation and neutralization with an overall yield of 63.8% (based on 2).

Zhongguo Yiyao Gongye Zazhi published new progress about 1019206-88-2. 1019206-88-2 belongs to amides-buliding-blocks, auxiliary class Protein Tyrosine Kinase/RTK,VEGFR, name is 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydrate, and the molecular formula is C15H14O3, Synthetic Route of 1019206-88-2.

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

Wang, Zhenghui published the artcileImaging mRNA expression levels in living cells with PNA·DNA binary FRET probes delivered by cationic shell-crosslinked nanoparticles, Safety of 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, the publication is Organic & Biomolecular Chemistry (2013), 11(19), 3159-3167, database is CAplus and MEDLINE.

Optical imaging of gene expression through the use of fluorescent antisense probes targeted to the mRNA has been an area of great interest. The main obstacles to developing highly sensitive antisense fluorescent imaging agents have been the inefficient intracellular delivery of the probes and high background signal from unbound probes. Binary antisense probes have shown great promise as mRNA imaging agents because a signal can only occur if both probes are bound simultaneously to the mRNA target site. Selecting an accessible binding site is made difficult by RNA folding and protein binding in vivo and the need to bind two probes. Even more problematic, has been a lack of methods for efficient cytoplasmic delivery of the probes that would be suitable for eventual applications in vivo in animals. Herein we report the imaging of iNOS mRNA expression in live mouse macrophage cells with PNA·DNA binary FRET probes delivered by a cationic shell crosslinked knedel-like nanoparticle (cSCK). We first demonstrate that FRET can be observed on in vitro transcribed mRNA with both the PNA probes and the PNA·DNA hybrid probes. We then demonstrate that the FRET signal can be observed in live cells when the hybrid probes are transfected with the cSCK, and that the strength of the FRET signal is sequence specific and depends on the mRNA expression level.

Organic & Biomolecular Chemistry published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C14H14, Safety of 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid.

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