Tag: M.W=150-200

Zhang, Rui-Bo published the artcileDesign, Synthesis, and Molecular Mechanism Studies of N-Phenylisoxazoline-thiadiazolo[3,4-a]pyridazine Hybrids as Protoporphyrinogen IX Oxidase Inhibitors, Synthetic Route of 372136-76-0, the publication is Journal of Agricultural and Food Chemistry (2020), 68(47), 13672-13684, database is CAplus and MEDLINE.

Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) is an important target for green agrochem. discovery. Herein, a novel N-phenylisoxazoline-thiadiazolo[3,4-a]pyridazine herbicidal active scaffold was designed by the scaffold hybridization strategy. Systematic structural optimization enabled the discovery of a series of derivatives with excellent weed control at 9.375-150 g ai/ha by the post-emergent application. Some derivatives exhibited improved Nicotiana tabacum PPO (NtPPO)-inhibitory activity than fluthiacet-Me. Of these, I, with K_i = 21.8 nM, displayed higher weed control than fluthiacet-Me at the rate of 12-75 g ai/ha, and selective to maize at 75 g ai/ha. In planta, I was converted into a bioactive metabolite II (K_i = 4.6 nM), which exhibited 4.6-fold more potency than I in inhibiting the activity of NtPPO. Mol. dynamics simulation explained that II formed stronger π-π interaction with Phe392 than that of I. This work not only provides a promising lead compound for weed control in maize fields but is also helpful to understand the mol. mechanism and basis of the designed hybrids.

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 C38H74Cl2N2O4, Synthetic Route of 372136-76-0.

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

Qiu, Xinyi published the artcileRemodeling the periodontitis microenvironment for osteogenesis by using a reactive oxygen species-cleavable nanoplatform, Computed Properties of 1869-45-0, the publication is Acta Biomaterialia (2021), 593-605, database is CAplus and MEDLINE.

Modestly removing the excessive reactive oxygen species (ROS) plays a crucial role in regulating the microenvironment of periodontitis and provides favorable conditions for osteogenesis. However, the current strategy for scavenging ROS is not controllable, substantially limiting the outcomes in periodontitis. Herein, we introduced a controllable ROS-scavenging nanoplatform by encasing N-acetylcysteine NAC, (a well-known ROS scavenger) into tailor-made ROS-cleavable amphiphilic polymer nanoparticles (PEG-ss-PCL NPs) as an intracellular delivery carrier. The existing ROS in the inflammatory microenvironment facilitated polymer degradation via breakage of thioketal bonds, and then led to encapsulated NAC release. NAC eliminated all ROS induced by lipopolysaccharide (LPS), while PssL-NAC adjusted the ROS level slightly higher than that of the control group. The percentage of apoptotic cells cultured with NAC and PssL-NAC decreased observably compared with that of cells cultured with 10 Μg/mL LPS. The microenvironment regulated by PssL-NAC was highly suitable for osteogenic differentiation based on PCR and Western blot results, which showed higher expression levels of BMP2, Runx2, and PKA. Anal. of ALP activity and Alizarin red S staining showed consistent results. Addnl., the injection of PssL-NAC into the periodontitis area could alleviate the tissue destruction induced by ligation of the maxillary second molar. PssL-NAC showed a better ability to decrease osteoclast activity and inflammation, consequently improving the restoration of destroyed tissue. Our study suggests that ROS-responsive polymer nanoparticles loaded with NAC (PssL-NAC) can be new promising materials for the treatment of periodontitis. More and more studies indicate that periodontal tissue damage is closely related to the high reactive oxygen species (ROS) environment. Excessive ROS will aggravate periodontal tissue damage and is not conducive to tissue repair. However, as an essential signal mol. in human physiol. activities, ROS absence is also useless for tissue repair. In this study, we proposed to improve ROS imbalance in the environment of periodontitis as a strategy to promote periodontal regeneration and successfully synthesized a smart drug-releasing nanoplatform that can respond to ROS. Besides, we validated its ability to regulate the ROS environment and promote osteogenesis through exptl. data in vivo and in vitro.

Acta Biomaterialia 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, Computed Properties of 1869-45-0.

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

Spagnolo, Piero published the artcileOne-pot preparation of isomeric acetyl- and 2,2,2-trifluoroacetylazidothiophenes by selective bifunctionalization of dibromothiophenes via halogen-lithio exchange, COA of Formula: C6H10F3NO, the publication is Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1996), 963-964, database is CAplus.

A series of isomeric acetyl- (I, R = H) and 2,2,2-trifluoroacetylazidothiophenes (I, R = F) are prepared from 2,3-, 3,4-, and 2,5-dibromothiophenes via a one-pot procedure entailing stepwise halogen-lithium exchange and successive reaction of the resulting thienyllithium derivatives with tosyl azide and either N,N-dimethylacetamide or N,N-diethyl-2,2,2-trifluoroacetamide.

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry 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 C7H6BF3O2S, COA of Formula: C6H10F3NO.

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

Zeng, Hongyun published the artcileMethod for synthesis of 2,5-diaryl substituted thiazoles, Recommanded Product: 3-Methoxybenzothioamide, the publication is Youji Huaxue (2020), 40(8), 2535-2542, database is CAplus.

Thiazole ring is an important five-membered aromatic heterocyclic ring, and its derivatives have various biol. activities and are widely used in medicine. The synthesis of 2,5-diarylthiazole derivatives by acylation, thiolation, cyclization and Heck reaction using inexpensive and readily available substituted benzoic acid as raw materials was developed. The key point was to optimize the Heck reaction conditions and explore the possible reaction mechanism. The method has mild reaction conditions, simple operation, and good substrate universality, which provides a new direction for the synthesis of 2,5-diaryl substituted thiazoles.

Youji Huaxue 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 C6H12N2O, Recommanded Product: 3-Methoxybenzothioamide.

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

Hu, Jingyan published the artcileAmidation Reaction of Quinoline-3-carboxylic Acids with Tetraalkylthiuram Disulfides under Simple Conditions: A facile Synthesis of Quinoline-3-carboxamides, SDS of cas: 530-40-5, the publication is Asian Journal of Organic Chemistry (2020), 9(12), 2191-2195, database is CAplus.

A highly efficient and simple procedure for the synthesis quinoline-3-carboxamides and their analogs via amidation reaction of quinoline-3-carboxylic acids with tetraalkylthiuram disulfides was developed. The reaction proceeded efficiently under simple reaction conditions and featured the generality of broad scope of substrates with good yields. This protocol provides a convenient procedure for the synthesis of various aza-heteroaromatic carboxamides, which is of pharmaceutical interest.

Asian Journal of Organic Chemistry 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, SDS of cas: 530-40-5.

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

Teo, Yong-Chua published the artcileEfficient Manganese/Copper Bimetallic Catalyst for N-Arylation of Amides and Sulfonamides Under Mild Conditions in Water, Formula: C7H8FNO2S, the publication is European Journal of Organic Chemistry (2013), 2013(3), 515-524, database is CAplus.

An efficient and mild method using a bimetallic MnF₂/CuI catalyst at 60 °C in water was developed for the N-arylation of amides and sulfonamides with aryl halides. A variety of functionalized amides and sulfonamides were coupled with different substituted aryl halides to afford the corresponding N-arylated products in good to excellent yields (up to 97 %).

European Journal of Organic Chemistry published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C5H5N3S, Formula: C7H8FNO2S.

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

Teo, Yong-Chua published the artcileEfficient ligand-free, copper-catalyzed N-arylation of sulfonamides, HPLC of Formula: 489-17-8, the publication is Synlett (2011), 837-843, database is CAplus.

An efficient and convenient protocol has been developed for the N-arylation of sulfonamides with differently substituted aryl iodides using ligand-free copper iodide to afford the arylated products in good to excellent yields (up to 91%).

Synlett published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C25H47NO8, HPLC of Formula: 489-17-8.

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

Lei, Peng published the artcileDesign, synthesis and fungicidal activity of N-substituted benzoyl-1,2,3,4-tetrahydroquinolyl-1-carboxamide, Product Details of C7H5Cl2NO, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(10), 2544-2546, database is CAplus and MEDLINE.

To find a new lead compound with high biol. activity, a series of N-substituted benzoyl-1,2,3,4-tetrahydroquinolyl-1-carboxamide were designed using linking active substructures method. The target compounds were synthesized from substituted benzoic acid by four steps and their structures were confirmed by ¹H NMR, IR spectrum and elemental anal. The in vitro bioassay results indicated that some target compounds exhibited excellent fungicidal activities, and the position of the substituents played an important role in fungicidal activities. Especially, 4-t-Bu-substituted compound , exhibited better fungicidal activities than the com. fungicide flutolanil against two tested fungi Valsa mali and Sclerotinia sclerotiorum, with EC₅₀ values of 3.44 and 2.63 mg/L, resp. And it also displayed good in vivo fungicidal activity against S. sclerotiorum with the EC₅₀ value of 29.52 mg/L.

Bioorganic & Medicinal Chemistry Letters 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, Product Details of C7H5Cl2NO.

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

Cao, Yu-Qing published the artcileOne-pot synthesis of dehydrating reagent and its application in preparation of nitriles from amides, Synthetic Route of 2447-79-2, the publication is Organic Chemistry: An Indian Journal (2013), 9(4), 132-136, database is CAplus.

A new efficient, eco-friendly and economic method for the preparation of imine cation containing composite organic salt as a dehydrating reagent was reported. N,N-dimethylformamide (DMF) was reacted with oxalyl chloride [(COCl)₂], and the resultant imine cation reacted with phenol in the presence of triethylamine (Et₃N) to give the corresponding product in high yield. The use of the composite organic salt as an efficient dehydrating reagent has been demonstrated via the preparation of nitriles from amides.

Organic Chemistry: An Indian Journal 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, Synthetic Route of 2447-79-2.

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

Katritzky, Alan R. published the artcileAn efficient conversion of carboxylic acids into Weinreb amides, Name: N-Methoxy-N-methylisonicotinamide, the publication is ARKIVOC (Gainesville, FL, United States) [online computer file] (2002), 39-44, database is CAplus.

Efficient conversions of carboxylic acids into Weinreb amides were achieved by treatment of N-acylbenzotriazoles 2a-i with N,O-dimethylhydroxylamine hydrochloride under mild conditions. No racemization was found when optically active acids were employed.

ARKIVOC (Gainesville, FL, United States) [online computer file] 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, Name: N-Methoxy-N-methylisonicotinamide.

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