Tag: M.W=150-200

Dai, Hong published the artcileSynthesis and biological activity of 1-{4-[(2-cyanoimino-1,3-thiazolidine-3-yl)methyl]thiazol-2-yl}-3-aroyl ureas, Safety of 2,4-Dichlorobenzamide, the publication is Youji Huaxue (2013), 33(7), 1568-1572, database is CAplus.

In search of novel thiazole derivatives with potent biol. activities, a series of new thiazole compounds I (R = 4-Me, 4-Et, 3-F, 4-F, 2-Cl, 4-Cl, 4-Br, 2,4-Cl₂, 3,4-Cl₂) containing acyl urea moiety were synthesized by the condensation of 2-cyanoimino-3-(2-aminothiazol-4-ylmethyl)thiazolidine with various arylacylisocyanates. The structures of the target compounds were determined by ¹H NMR, MS and elemental anal. The structures of I (R = 4-Me, 2-Cl, 2,4-Cl₂) were further characterized by ¹³C NMR spectra. The bioassay data indicated that some of the title compounds showed fungicidal activities to some extent at the concentration of 50 μg/mL. For example, compound I (R = 4-F)displayed 65.3% inhibition rate against Gibberella zeae, compound I (R = 4-Cl) exhibited 67.3% inhibition rate against Cercospora arachidicola, and compound I (R = 4-Br) showed 56.1% inhibition rate against Physalospora piricola.

Youji Huaxue 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, Safety of 2,4-Dichlorobenzamide.

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

Wang, Yu-Hao published the artcilePhosphine-Catalyzed Annulations Based on [3+3] and [3+2] Trapping of Ketene Intermediates with Thioamides, Formula: C8H9NOS, the publication is Organic Letters (2021), 23(21), 8147-8152, database is CAplus and MEDLINE.

A novel annulation via ketene intermediates, allenyl imide I and alkynoates RC₆H₄CCC(O)OC₆H₄-4-NO₂ (R = H, 4-MeC₆H₄, 2-ClC₆H₄, 3-BrC₆H₄, 4-FC₆H₄, 4-ClC₆H₄) bearing good leaving groups is used for their function in a tandem conjugate addition-elimination reaction (SN2′ type) promoted by nucleophilic phosphine catalysts and developed. By utilizing thioamides as R¹C(S)NH₂ (R¹ = 4-chlorophenyl, thiophen-2-yl, naphthalen-2-yl, etc.) 1S,3N-bis-nucleophiles, [3+3] and [3+2] annulations have been established to allow rapid access to 1,3-thiazin-4-ones II and 5-alkenyl thiazolones III in high yields, resp. Furthermore, the possible reaction mechanisms are proposed on the basis of deuterium labeling experiments and d. functional theory calculations

Organic Letters 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 C13H16O2, Formula: C8H9NOS.

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

Zhang, Min published the artcileSynthesis and bioactivities of novel pyrazole amides carrying oxazole moiety, Application In Synthesis of 2447-79-2, the publication is Youji Huaxue (2020), 40(6), 1772-1778, database is CAplus.

In order to find new pyrazole amides with wonderful bioactivities, a series of novel pyrazole amide derivatives were synthesized by introducing substituted oxazole ring into the C-5 position of pyrazole skeleton based on the lead chlorantraniliprole. The aimed compounds were structurally characterized through ¹H NMR, ¹³C NMR and elemental anal. The preliminary bioassay results exhibited that all the title compounds displayed more than 90% insecticidal activities against Mythimna separata (Walker) at 500μg/mL. At the dosage of 100μg/mL, five compounds possessed 90%∼100% insecticidal activities against Mythimna separata (Walker), and three compounds exhibited insecticidal property against Aphis craccivora with 90%∼100%. Addnl., at the dosage of 500μg/mL, two compounds possessed insecticidal activity against Tetranychus cinnabarinus with 80%∼100%.

Youji Huaxue 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 C7H8BBrO3, Application In Synthesis of 2447-79-2.

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

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

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

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

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

Cheng, Dong-Bing published the artcileEndogenous Reactive Oxygen Species-Triggered Morphology Transformation for Enhanced Cooperative Interaction with Mitochondria, Product Details of C4H6F3NOS, the publication is Journal of the American Chemical Society (2019), 141(18), 7235-7239, database is CAplus and MEDLINE.

The morphol. controlled mol. assemblies play vital roles in biol. systems. Here we present endogenous reactive oxygen species (ROS)-triggered morphol. transformation of polymer-peptide conjugates (PPCs) for cooperative interaction with mitochondria, exhibiting high tumor therapeutic efficacy. The PPCs are composed of (i) a β-sheet-forming peptide KLVFF conjugated with poly(ethylene glycol) through ROS-cleavable thioketal, (ii) a mitochondria-targeting cytotoxic peptide KLAK, and (iii) a poly(vinyl alc.) backbone. The self-assembled PPCs nanoparticles can enter cells and target mitochondria. Because of overgenerated ROS around mitochondria in most cancer cells, the thioketal linker can be cleaved, leading to transformation from nanoparticles to fibrous nanostructures. As a result, the locational nanofibers with exposure of KLAK exhibit enhanced multivalent cooperative interactions with mitochondria, which causes selective cytotoxicity against cancer cells and powerful tumor suppression efficacy in vivo. As the first example of ROS-triggered intracellular transformation, the locational assembly strategy in vivo may provide a new insight for disease diagnosis and therapy through enhanced interaction with targeting site.

Journal of the American Chemical Society 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, Product Details of C4H6F3NOS.

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

Shen, Lan published the artcileSynthesis and structure-activity relationships of thiadiazole-derivatives as potent and orally active peroxisome proliferator-activated receptors α/δ dual agonists, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Bioorganic & Medicinal Chemistry (2008), 16(6), 3321-3341, database is CAplus and MEDLINE.

Replacement of the methyl-thiazole moiety of GW501516 (a PPARδ selective agonist) with [1,2,4]thiadiazole gave compound 21 (I) which unexpectedly displayed submicromolar potency as a partial agonist at PPARα in addition to the high potency at PPARδ. A structure-activity relationships study of 21 resulted in the identification of 40 as a potent and selective PPARα/δ dual agonist. Compound 40 and its close analogs represent a new series of PPARα/δ dual agonists. The high potency, high selectivity, significant gene induction, excellent PK profiles, low P 450 inhibition or induction, and good in vivo efficacy in four animal models support 40 being selected as a pre-clin. study candidate, and may render 40 as a valuable pharmacol. tool in elucidating the complex roles of PPARα/δ dual agonists, and the potential usage for the treatment of metabolic syndrome.

Bioorganic & 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 C30H32ClN7O2, Recommanded Product: 2,4-Dichlorobenzamide.

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