Tag: M.W=150-200

Pailer, Matthias published the artcileDetermination of primary and secondary amines as amides by means of gas chromatography on packed and capillary columns, COA of Formula: C6H10F3NO, the publication is Monatshefte fuer Chemie (1966), 97(6), 1541-53, database is CAplus.

A very large number of phthalyl, succinyl, trifluoroacetyl, and pentafluoropropionyl derivatives of primary and secondary amines were prepared in order to investigate their suitability for gas-chromatog. separation, in studies on tobacco smoke amines. The best results were obtained with trifluoroacetyl derivatives (Makisumi and Saroff, CA 62, 13847b). Cooled 0.01 mole amine in 5 ml. absolute Et2O was treated with 0.01 mole (CF3CO)2O at -5°. The mixture was kept for 1 hr. and treated with 20 ml. Et2O (CH2Cl2 for difficultly soluble derivatives) and processed as usual to give 90-5% of the following F3CCONR1R2 (R1, R2, m.p., b.p./mm., and n20D given): Me, H, 48-49.5°, 80°/11, -; Et, H, -, 90°/11, 1.3600; Pr, H, -, 100°/11, 1.3718; iso-Pr, H, 52-3°, 60°/0.01, -; allyl, H, -, 100°/11, 1.3849; CH:CH2, H, -, 95°/11, 1.3932; MeO(CH2)3, H, -, 110°/11, 1.3900; Bu, H, -, 105°/11, 1.3803; EtMeCH, H, -, 95°/11, 1.3802; iso-Bu, H, -, 95°/11, 1.3792; tert-Bu, H, 44-5°, 70°/11, -; Am, H, -, 110°/11, 1.3901; PrMeCH, H, -, 45°/0.001, 1.3879; Et2CH, H, 52-3°, 105°/11, -; EtMeCHCH2, H, -, 115°/11, 1.3910; iso-Am, H, -, 115°/11, 1.3890; n-C6H13, H, -, 120°/11, 1.3969; n-C7H15, H, -, 135°/11, 1.4031; n-C8H17, H, -, 160°/11, 1.4089; EtBuCHCH2, H, -, 80°/0.001, 1.4117; n-C13H27, H, 62-3°, 100°/0.001, -; n-C15H31, H, 72-3°, 120°/0.001, -; n-C16H33, H, 69-70°, 140°/0.001, -; n-C18H37, H, 70-2°, 150°/0.001, -; 9-octadecenyl, H, -, 140°/0.001, -; cyclopentyl, H, 73°, 80°/0.001, -; cyclohexyl, H, 94-4.5°, 80°/0.001, -; cycloheptyl, H, 61-2°, 80°/0.001, -; MePhCH, H, -, 70°/0.001, -; PhCH2CH2, H, 55-6°, 70°/0.001, -; PhCH2, H, 73.5-4.5°, 70°/0.001, -; styryl, H, 105-7°, 110°/0.001, -; Me, Me, -, 50°/11, 1.3632; Me, Et, -, 60°/11, 1.3741; Et, Et, -, 65°/11, 1.3798; Pr, Pr, -, 85°/11, 1.3938; iso-Pr, iso-Pr, 52-3°, 85°/11, -; Pr, iso-Pr, -, 85°/11, 1.3929; allyl, allyl, -, 90°/11, 1.4124; Bu, Bu, -, 110°/11, 1.4045; sec-Bu, sec-Bu, -, 95°/11, 1.4072; iso-Bu, iso-Bu, -, 95°/11, 1.4031; iso-Bu, Bu, -, 100°/11, 1.4052; tert-Bu, iso-Pr, -, 80°/11, 1.4035; Am, Am, -, 120°/11, 1.4121; n-C8H17, Et, -, 150°/11, 1.4146; n-C8H17, n-C8H17, -, 130°/0.05, 1.4305; n-C18H37, Me, 31-3°, 160°/0.001, -; cyclohexyl, cyclohexyl, sublimes 210°, 120°/0.05, -; PhCH2, PhCH2, -, 125°/0.05, 1.5278; (R1R2N =) Δ3-pyrrolyl, -, 90°/11, 1.4195; (R1R2N =) pyrrolidinyl, -, 90°/11, 1.4082; (R1R2N =) 2-methylpyrrolidinyl, -, 100°/11, -; (R1R2N =) 3-methylpyrrolidinyl, -, 100°/11, 1.4094; (R1R2N =) 2-ethylpyrrolidinyl, -, 105°/11, 1.4141; (R1R2N =) 2-propylpyrrolidinyl, -, 110°/11, 1.4188; (R1R2N =) 2-phenylpyrrolidinyl, -, 115°/0.05, 1.4911; (R1R2N =) 2-pyrridylpyrrolidinyl, -, 125°/0.05, 1.4962; (R1R2N =) 2,3-dimethylpyrrolidinyl, -, 100°/11, 1.4129; (R1R2N =) 2,4-dimethylpyrrolidinyl, -, 95°/11, 1.4080; (R1R2N =) 2,5-dimethylpyrrolidinyl, -, 90°/11, 1.4116; (R1R2N =) 3,4-dimethylpyrrolidinyl, -, 130°/11, -; (R1R2N =) piperidino, -, 90°/11, 1.4170; (R1R2N =) 2-methylpiperidino, -, 105°/11, 1.4205; (R1R2N =) 3-methylpiperidino, -, 100°/11, 1.4175; (R1R2N =) 4-methylpiperidino, -, 105°/11, 1.4181; (R1R2N =) 2-ethylpiperidino, -, 110°/11, 1.4246; (R1R2N =) 2,3-dimethylpiperidino, -, 115°/11, 1.4246; (R1R2N =) 2,4-dimethylpiperidino, -, 110°/11, 1.4201; (R1R2N =) 2,6-dimethylpiperidino, -, 110°/11, 1.4262; (R1R2N =) morpholino, -, 115°/11, 1.4182; Ph, H, 89-90°, 50°/0.001, -; 2-MeC6H4, H, 78-9°, 60°/0.001, -; 3-MeC6H4, H, 64.5-5.5°, 70°/0.001, -; 4-MeC6H4, H, 111°, 70°/0.001, -; 2-EtC6H4, H, 92-3°, 80°/0.001, -; 4-EtC6H4, H, 103-4°, 80°/0.001, -; 2,3-Me2C6H3, H, 97°, 80°/0.001, -; 2,4-Me2C6H3, H, 91°, 75°/0.001, -; 2,5-Me2C6H3, H, 84-6°, 75°/0.001, -; 2,6-Me2C6H3, H, 89-90°, 80°/0.001, -; 3,4-Me2C6H3, H, 73°, 80°/0.001, -; 3,5-Me2C6H3, H, 83-5°, 80°/0.001, -; 2,4,6-Me3C6H2, H, 139-40°, 90°/0.001, -; 2-HOC6H4, H, sublimes 167-9°, 110°/0.001, -; 3-HOC6H4, H, 131-2°, 115°/0.001, -; 4-HOC6H4, H, 172-3°, 120°/0.001, -; 2-MeOC6H4, H, 50-50.5°, 90°/0.001, -; 3-MeOC6H4, H, 75°, 105°/0.001, -; 4-MeOC6H4, H, 112°, 105°/0.001, -; 2-EtOC6H4, H, 141-2°, 110°/0.001, -; 1-C10H7, H, 102-3°, 100°/0.001, -; 2-C10H7, H, 146-7.5°, 120°/0.001, -; 2-fluorenyl, H, 201-2°, 160°/0.001, -; 9-fluorenyl, H, sublimes, 160°/0.001, -; 4-stilbenyl, H, 213-14°, 180°/0.001, -; azobenzene, H, 178-9°, 120°/0.001, -; 1-(2-HOC10H6), H, 168-9.5°, 140°/0.001, -; 2-PhC6H4, H, 99-101°, 100°/0.001, -; 4-PhC6H4, H, 200°, 190°/0.001, -; 2-pyridyl, H, 75-7°, 75°/0.001, -; 3-pyridyl, H, 127-8°, 110°/0.001, -; 5-isoquinolyl, H, 202-4°, 155°/0.001, -; 8-isoquinolyl, H, 215°, 140°/0.001, -; Ph, Me, 26-7°, 120°/11, 1.4681; Ph, Et, -, 120°/11, 1.4680; Ph, iso-Pr, 88-9°, 80°/0.001, -; PhCH2, Ph, 88-9°, 80°/0.001, -; 2-MeC6H4, Me, -, 125°/11, 1.4729; 2-MeC6H4, Et, -, 130°/11, 1.4731; 1-C10H7, Ph, 97-9°, 130°/0.001, -; 2-C10H7, Ph, 75-7°, 140°/0.001, -; Ph, Ph, 71-2°; 100°/0.001, -. Following (F3CCONH)2R were also prepared (R, m.p., and b.p./mm. given): CH2CH2, 204-6°, 140°/0.001; (CH2)3, 116-17°, 110°/0.005; (CH2)4, 155-7°, 120°/0.002; (CH2)5, 110-12°, 140°/0.002; (CH2)6, 121-3°, 150°/0.002; 1,2-C6H4, 158-8.5°, 130°/0.002; 1,3-C6H4, sublimes 225-8°, 140°/0.002; 1,4-C6H4, 249-50°, 160°/0.01; 4-methyl-1,2-phenylene, sublimes 197-9°, 150°/0.002; 4-methyl-1,3-phenylene, 183-4°, 160°/0.002; 5-methyl-1,4-phenylene, 190.5-1.5°, 150°/0.008; 2,2′-C6H4C6H4, 161-2°, 160°/0.001; 2,2′-C6H4CH:CHC6H4, sublimes 270°, 195°/0.01, -. Following CF3CF2CONHR were prepared (R, m.p., and b.p./0.001 mm. given): Ph, 98-9°, 65°; 2-MeC6H4, 78-9°, 65°; 3-MeC6H4, 52-3°, 70°; 4-MeC6H4, 111-12°, 75°; 2-EtC6H4, 64-5°, 70°; 4-EtC6H4, 121-2°, 80°; 2,3-Me2C6H3, 89-90°, 80°; 2,4-Me2C6H3, 55-7°, 75°; 2,5-Me2C6H3, 101-2°, 80°; 2,6-Me2C6H3, 108-9°, 80°; 3,4-Me2C6H3, 82-3°, 80°; 3,5-Me2C6H3, 94-5°, 80°; 2,4,6-Me3C6H2, 90-1°, 90°. Also prepared were: 2-trifluoroacetylpyrrole, m. 48.5°, 1,4-bis(trifluoroacetyl)piperazine, m. 111.5-12.5°, and 3-trifluoroacetylinodle m. 215-16°.

Monatshefte fuer Chemie 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 C6H10F3NO, COA of Formula: C6H10F3NO.

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

Fritz, H. published the artcileStudies on organophosphorus compounds. XXVI. Synthesis and carbon-13 NMR spectra of N,N-dialkyl thioamides, Category: amides-buliding-blocks, the publication is Bulletin des Societes Chimiques Belges (1978), 87(7), 525-34, database is CAplus.

By a new sulfuration reagent, the dimer of p-methoxyphenylthionophosphine sulfide, a series of thioamides were prepared in almost quant. yields from the corresponding amides. Carbon-13 NMR spectra of tertiary thioamides of formic, acetic, trifluoroacetic, propionic, and butyric acids were completely assigned with the aid of extensive double resonance and shift reagent experiments and the data obtained were compared with those of the analogous amides. A linear relation between the carbon-13 chem. shifts of the C:S of ethylthioamides and C:O of the corresponding amide was found.

Bulletin des Societes Chimiques Belges 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 C6H10F3NO, Category: amides-buliding-blocks.

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

Ghidu, Victor P. published the artcileA new and efficient synthetic route for the anxiolytic agent CL285032, Synthetic Route of 325715-13-7, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(1), 259-261, database is CAplus and MEDLINE.

CL285032, i.e. 6-[3-(acetylmethylamino)phenyl]-3-methyl[1,2,4]triazolo[4,3-b]pyridazine, is an anxiolytic compound currently under investigation as a possible treatment for canine noise phobia associated anxiety. A robust scale-up and manufacturing process is essential for the development and marketability of the drug. The current synthetic route, although reliable, requires 7 steps and has a low overall yield (18%), leaving opportunity for improvement. The authors present an efficient alternative approach toward the synthesis of CL285032 from 3-AcMeNC₆H₄Ac over 3 steps with 65% overall yield.

Bioorganic & Medicinal Chemistry Letters published new progress about 325715-13-7. 325715-13-7 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Ketone,Amide, name is N-(3-Acetylphenyl)-N-methylacetamide, and the molecular formula is C11H13NO2, Synthetic Route of 325715-13-7.

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

Luo, Zhongli published the artcileOne-Pot Synthesis of Tertiary Amides from Organic Trichlorides through Oxygen Atom Incorporation from Air by Convergent Paired Electrolysis, Computed Properties of 360-92-9, the publication is Journal of Organic Chemistry (2021), 86(8), 5983-5990, database is CAplus and MEDLINE.

A convergent paired electrolysis catalyzed by a B12 complex for the one-pot synthesis of a tertiary amide from organic trichlorides has been developed. Various readily available organic trichlorides, such as benzotrichloride and its derivatives, chloroform, dichlorodiphenyltrichloroethane (DDT), trichloro-2,2,2-trifluoroethane (CFC-113a), and trichloroacetonitrile (CNCCl₃), were converted to amides in the presence of tertiary amines through oxygen incorporation from air at room temperature The amide formation mechanism in the paired electrolysis, which was mediated by a cobalt complex, was proposed.

Journal of 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 C6H10F3NO, Computed Properties of 360-92-9.

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

Collins, Scott published the artcileAdditions of alkyllathanum triflates to carbonyl compounds: reactive organometallic nucleophiles, Name: N,N-Diethylisonicotinamide, the publication is Journal of Organic Chemistry (1990), 55(11), 3565-8, database is CAplus.

Addition of alkyl- or aryllithium compounds to lanthanum(III) triflate in ethereal solvents produces the title reagents RLa(O₃SCF₃)₂ (R = Me, Bu, Ph) that undergo nucleophilic addition to carbonyl compounds under mild conditions. These reagents resemble alkylcerium halides in their reactions with enolizable carbonyl compounds but are more reactive. In particular, they are useful for the conversion of hindered, tertiary amides to ketones. ¹H NMR spectroscopy was employed to clarify mechanistic aspects of this addition process. The title reagents actually appear to be a mixture of several species; formulation of their structure has proven elusive. However, in the presence of a tertiary amide, these species react to give a single, tetrahedral intermediate, which is quite stable in solution

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, Name: N,N-Diethylisonicotinamide.

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

Fu, Zhangyu published the artcileDesign, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure, Recommanded Product: N-Methoxy-N-methylisonicotinamide, the publication is Bioorganic & Medicinal Chemistry (2018), 26(8), 2061-2072, database is CAplus and MEDLINE.

Based on the co-crystal structures of tubulin with plinabulin and Compound 1 ((3Z,6Z)-3-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)-6-(3-benzoylbenzylidene)piperazine-2,5-dione, a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biol. activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d ((3Z,6Z)-3-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)-6-(3-(thiophene-3-carbonyl)benzylidene)piperazine-2,5-dione) and 13e ((3Z,6Z)-3-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)-6-(3-(thiophene-2-carbonyl)benzylidene)piperazine-2,5-dione) exhibited potent activities with IC₅₀ at 1.56 and 1.72 nM, resp. The tubulin polymerization assay indicated that these derivatives could inhibit microtubule polymerization Furthermore, the interaction between tubulin and these compounds were elucidated by mol. docking. The binding modes of Compounds 13d and 13e were similar to the co-crystal structure of Compound 1. H-π interaction was observed between the aromatic hydrogen of thiophene moiety with Phe 20, which could enhance their binding affinities.

Bioorganic & Medicinal Chemistry 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, Recommanded Product: N-Methoxy-N-methylisonicotinamide.

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

Martin, John r. published the artcileOxidation-Responsive, Tunable Growth Factor Delivery from Polyelectrolyte-Coated Implants, Recommanded Product: 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, the publication is Advanced Healthcare Materials (2021), 10(9), 2001941, database is CAplus and MEDLINE.

Polyelectrolyte multilayer (PEM) coatings, constructed on the surfaces of tissue engineering scaffolds using layer-by-layer assembly (LbL), promote sustained release of therapeutic mols. and have enabled regeneration of large-scale, pre-clin. bone defects. However, these systems primarily rely on non-specific hydrolysis of PEM components to foster drug release, and their pre-determined drug delivery schedules potentially limit future translation into innately heterogeneous patient populations. To trigger therapeutic delivery directly in response to local environmental stimuli, an LbL-compatible polycation solely degraded by cell-generated reactive oxygen species (ROS) was synthesized. These thioketal-based polymers were selectively cleaved by physiol. doses of ROS, stably incorporated into PEM films alongside growth factors, and facilitated tunable release of therapeutic bone morphogenetic protein-2 (BMP-2) upon oxidation These coatings′ sensitivity to oxidation was also dependent on the polyanions used in film construction, providing a simple method for enhancing ROS-mediated protein delivery in vitro. Correspondingly, when implanted in critically-sized rat calvarial defects, the most sensitive ROS-responsive coatings generated a 50% increase in bone regeneration compared with less sensitive formulations and demonstrated a nearly threefold extension in BMP-2 delivery half-life over conventional hydrolytically-sensitive coatings. These combined results highlight the potential of environmentally-responsive PEM coatings as tunable drug delivery systems for regenerative medicine.

Advanced Healthcare Materials 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, Recommanded Product: 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide.

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

Zhang, Ning published the artcileDesign, synthesis, and insecticidal/acaricidal evaluation of novel pyrimidinamine derivatives containing phenyloxazole moiety, Synthetic Route of 2447-79-2, the publication is Chemical Papers (2020), 74(3), 963-970, database is CAplus.

A series of novel pyrimidinamine derivatives containing phenyloxazole moiety I (R¹ = H, 2-Cl, 4-CF₃, etc.; R² = Me, Et) was designed and synthesized, and their structures were characterized by ¹H NMR, MS, and elemental analyses. The bioassay results displayed that some compounds exhibited remarkable insecticidal activities against Aphis fabae and Tetranychus cinnabarinus. Especially, I (R¹ = 4-Me; R² = Et) showed potent activity against A. fabae, superior to that of the com. insecticide, imidacloprid. In addition, I (R¹ = 4-CF₃; R² = Et) showed potent activities against T. cinnabarinus, inferior to that of the com. insecticide spirotetramat. The structure-activity relationship study for the target compounds was also discussed.

Chemical Papers 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 C7H13BrSi, Synthetic Route of 2447-79-2.

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

Eccles, Peter J. published the artcileOrganophosphorus compounds as potential fungicides. Part IV. The preparation and properties of some novel N-(1-substituted-2,2,2-trichloroethyl)phosphoramidates, Synthetic Route of 2447-79-2, the publication is Phosphorus, Sulfur and Silicon and the Related Elements (1995), 105(1-4), 33-44, database is CAplus.

A series of 20 di-Et N-(1-substituted-2,2,2-trichloroethyl)phosphoramidates (EtO)₂P(O)NHCH(CCl₃)X was prepared containing N-heterocyclic, carboxamide, phosphoramide, dithiocarbamate, xanthate, and hydroxyethylthio substituents X in the 1-position of the 2,2,2-trichloroethyl group. Screening in vitro at 500 ppm showed the dithiocarbamates (EtO)₂P(O)NHCH(CCl₃)SCSNR₂ (R = Me, Et) to be the most active, giving complete control of Fusarium spp., Helminthosporium spp., and Ophiobolus graminis under these conditions. High activity was also observed against Fusarium culmorum for the triazole, hydroxyethylthio, and xanthate derivatives, and for an imidazole analog in which one ethoxy and one dimethylamino group were attached to phosphorus. The carboxamide derivatives were the least active. The dithiocarbamates also gave ca. 50% control of Piricularia oryzae and Rhizoctonia solani at 300 ppm in vitro. Lower levels of activity were recorded when the compounds were applied to seeds infected with Drechslera teres and Septoria nodorum and slight inhibition of germination and plant development was observed The compounds were all weak inhibitors of acetylcholinesterase.

Phosphorus, Sulfur and Silicon and the Related Elements 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

Steffek, Micah published the artcileA multifaceted hit-finding approach reveals novel LC3 family ligands, Synthetic Route of 475216-25-2, the publication is Biochemistry, database is CAplus and MEDLINE.

Autophagy-related proteins (Atgs) drive the lysosome-mediated degradation pathway, autophagy, to enable the clearance of dysfunctional cellular components and maintain homeostasis. In humans, this process is driven by the mammalian Atg8 (mAtg8) family of proteins comprising the LC3 and GABARAP subfamilies. The mAtg8 proteins play essential roles in the formation and maturation of autophagosomes and the capture of specific cargo through binding to the conserved LC3-interacting region (LIR) sequence within target proteins. Modulation of interactions of mAtg8 with its target proteins via small-mol. ligands would enable further interrogation of their function. Here we describe unbiased fragment and DNA-encoded library (DEL) screening approaches for discovering LC3 small-mol. ligands. Both strategies resulted in compounds that bind to LC3, with the fragment hits favoring a conserved hydrophobic pocket in mATG8 proteins, as detailed by LC3A-fragment complex crystal structures. Our findings demonstrate that the malleable LIR-binding surface can be readily targeted by fragments; however, rational design of addnl. interactions to drive increased affinity proved challenging. DEL libraries, which combine small, fragment-like building blocks into larger scaffolds, yielded higher-affinity binders and revealed an unexpected potential for reversible, covalent ligands. Moreover, DEL hits identified possible vectors for synthesizing fluorescent probes or bivalent mols. for engineering autophagic degradation of specific targets.

Biochemistry 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 C9H13NO2, Synthetic Route of 475216-25-2.

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