Tag: M.W=150-200

Mayhoub, Abdelrahman S. published the artcileOptimization of thiazole analogues of resveratrol for induction of NAD(P)H:quinone reductase 1 (QR1), Name: 3-Methoxybenzothioamide, the publication is Bioorganic & Medicinal Chemistry (2012), 20(24), 7030-7039, database is CAplus and MEDLINE.

NAD(P)H:quinone reductase 1 (QR1) belongs to a class of enzymes called cytoprotective enzymes. It exhibits its cancer protective activity mainly by inhibiting the formation of intracellular semiquinone radicals, and by generating α-tocopherolhydroquinone, which acts as a free radical scavenger. It is therefore believed that QR1 inducers can act as cancer chemopreventive agents. Resveratrol (1) is a naturally occurring stilbene derivative that requires a concentration of 21 μM to double QR1 activity (CD = 21 μM). The stilbene double bond of resveratrol was replaced with a thiadiazole ring and the phenols were eliminated to provide a more potent and selective derivative 2 (CD = 2.1 μM). Optimizing the substitution pattern of the two Ph rings and the central heterocyclic linker led to a highly potent and selective QR1 inducer 9o with a CD value of 0.087 μM.

Bioorganic & Medicinal 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 C8H9NOS, Name: 3-Methoxybenzothioamide.

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

Mayhoub, Abdelrahman S. published the artcileOptimizing thiadiazole analogues of resveratrol versus three chemopreventive targets, Application of 3-Methoxybenzothioamide, the publication is Bioorganic & Medicinal Chemistry (2012), 20(1), 510-520, database is CAplus and MEDLINE.

Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biol. targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemopreventive agents with enhanced potencies and selectivities when evaluated as inhibitors of aromatase and NF-κB and inducers of quinone reductase 1 (QR1).

Bioorganic & Medicinal 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 C8H9NOS, Application of 3-Methoxybenzothioamide.

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

Haddad, Ibrahim published the artcilePoly(arylene sulfides) with pendant cyano groups as high-temperature laminating resins. II, Application of 2,4-Dichlorobenzamide, the publication is Journal of Polymer Science, Polymer Chemistry Edition (1974), 12(6), 1301-11, database is CAplus.

The phys. properties were studied of poly(phenylene sulfides) prepared from m-benzenedithiol and p-C6H4Br2, 2,4- or 3,5-dichlorobenzonitrile, optionally selfcrosslinked or crosslinked with anthracene-9,10-bisnitrile oxide [30862-16-9]. Nitrile-containing binary copolymers had higher m.p.s than other copolymers.

Journal of Polymer Science, Polymer Chemistry Edition 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

Bajaj, Megha published the artcileDiscovery of Novel Pneumococcal Surface Antigen A (PsaA) Inhibitors Using a Fragment-based Drug Design Approach, Related Products of amides-buliding-blocks, the publication is ACS Chemical Biology (2015), 10(6), 1511-1520, database is CAplus and MEDLINE.

Streptococcus pneumoniae is a leading cause of life-threatening bacterial infections, especially in young children in developing countries. Pneumococcal infections can be treated with β-lactam antibiotics, but rapid emergence of multidrug-resistant strains of S. pneumoniae over the past two decades has emphasized the need to identify novel drug targets. Pneumococcal surface antigen A (PsaA) is one such target, found on the cell surface of S. pneumoniae. It functions as a high-affinity substrate-binding protein, facilitating acquisition of Mn²⁺, which has an important role in protecting S. pneumoniae from reactive oxygen species and, hence, oxidative stress. Consequently, PsaA is essential for bacterial survival and an important virulence factor, which makes it a promising target for antibiotic drug development. To design novel PsaA inhibitors, we used a combination of de novo fragment-based drug discovery and in silico virtual screening methods. We profiled a collection of low mol. weight compounds that were selected based on their structural diversity and ability to bind to apo-PsaA in a virtual docking experiment The screening resulted in two initial hits that were further optimized by structural variation to improve their potency while maintaining their ligand efficiency and favorable physicochem. properties. The optimized hits were validated using a cell-based assay and mol. dynamics simulations. We found that virtual screening substantially augmented fragment-based drug design approaches, leading to the identification of novel pneumococcal PsaA inhibitors.

ACS Chemical Biology 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 C7H8FNO2S, Related Products of amides-buliding-blocks.

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

Thompson, Mark J. published the artcileImproved 2,4-Diarylthiazole-Based Antiprion Agents: switching the Sense of the Amide Group at C5 Leads to an Increase in Potency, COA of Formula: C8H9NOS, the publication is ChemMedChem (2010), 5(9), 1476-1488, database is CAplus and MEDLINE.

Amide derivatives of 2,4-diarylthiazole-5-carboxylic acids were synthesized and tested for efficacy in a cell line model of prion disease. A number of compounds demonstrating antiprion activity were thereby identified from the screening libraries, showing improved potency and reproducibility of results relative to amide derivatives of the related 2,4-diphenyl-5-aminothiazole, which have been documented previously. Thus, ‘switching’ the sense of the amide bond at thiazole C5 revealed a more promising lead series of potential prion disease therapeutics. Furthermore, 3,5-diaryl-1,2,4-thiadiazoles isolated as byproducts during library synthesis provided a handful of addnl. examples possessing an antiprion effect, thereby augmenting the set of newly identified active compounds Evaluation of binding to cellular prion protein (PrP^C) showed only weak affinities at best, suggesting that the newly identified antiprion agents do not mediate their biol. effect through direct interaction with PrP^C.

ChemMedChem 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 C7H11N, COA of Formula: C8H9NOS.

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

Yoshimura, Akira published the artcile(Tosylimino)phenyl-λ³-iodane as a reagent for the synthesis of methyl carbamates via Hofmann rearrangement of aromatic and aliphatic carboxamides, Name: 2,4-Dichlorobenzamide, the publication is Journal of Organic Chemistry (2012), 77(4), 2087-2091, database is CAplus and MEDLINE.

A mild procedure for the Hofmann rearrangement of aromatic and aliphatic carboxamides using (tosylimino)phenyl-λ³-iodane, PhINTs, as a reagent is reported. Because of the mild reaction conditions, this method is particularly useful for the Hofmann rearrangement of substituted benzamides, which usually afford complex reaction mixtures with other hypervalent iodine oxidants. The mild reaction conditions and high selectivity in the reaction of carboxamides with PhINTs allow the isolation of the initially formed labile isocyanates or their subsequent conversion to stable carbamates by treatment with alcs.

Journal of Organic 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 C18H35NO, Name: 2,4-Dichlorobenzamide.

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

Marce, Patricia published the artcileA mild hydration of nitriles catalysed by copper(II) acetate, HPLC of Formula: 2447-79-2, the publication is Chemical Communications (Cambridge, United Kingdom) (2016), 52(7), 1436-1438, database is CAplus and MEDLINE.

A simple, mild and general procedure for the hydration of nitriles to amides using copper as catalyst and promoted by N,N-diethylhydroxylamine is described. The reaction can be conducted in water at low temperature in short reaction times. This new procedure allows amides to be obtained from a wide range of substrates in excellent yields.

Chemical Communications (Cambridge, United Kingdom) 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, HPLC of Formula: 2447-79-2.

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

Waisser, Karel published the artcileBiological side effects of potential antituberculotics. XV. Quantitative relations between chemical structure and hepatotoxicity of thiobenzamides, Safety of 3-Methoxybenzothioamide, the publication is Collection of Czechoslovak Chemical Communications (1988), 53(11B), 2957-61, database is CAplus.

¹H NMR chem. shifts. of thioamide protons have been determined for a group of thiobenzamides, and the values obtained have been correlated with the Hammett constants From the relations found, the σ_m and σ_p values of the thioamide group and some other σ constants describing the total effect of 2 substituents in the Ph group have been calculated The relation between the hepatotoxicity for rats [expressed as log ALT (serum alaninoaminotransferase)] and the Hammett constants is described by the parabolic equation.

Collection of Czechoslovak Chemical Communications 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 C7H10N2O2, Safety of 3-Methoxybenzothioamide.

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

Oda, Kazuaki published the artcileBenzannulation of heteroaromatics by photoreaction of arenecarbothioamides with 2-methoxyfuran, Quality Control of 64559-06-4, the publication is Journal of the Chemical Society, Chemical Communications (1994), 1477-8, database is CAplus.

Irradiation of arenecarbothioamides R¹C(:CHR)CSNH₂ [RR¹ = CH:CHCR²:CH, OCH:CH, SCH:CH,CH:CHN:CH, CH:NCH:CH; R² = H, Me, OMe] with 2-methoxyfuran in benzene solution gives benzo-fused arene derivatives I in moderate yields. Regioisomers I [RR¹ = CH:CR²CH:CH, CH:CHCH:N] were also obtained.

Journal of the Chemical Society, Chemical Communications 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, Quality Control of 64559-06-4.

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

Pal, Manojit published the artcileSynthesis and Cyclooxygenase-2 Inhibiting Property of 1,5-Diarylpyrazoles with Substituted Benzenesulfonamide Moiety as Pharmacophore: Preparation of Sodium Salt for Injectable Formulation, Safety of 4-Fluoro-2-methylbenzenesulfonamide, the publication is Journal of Medicinal Chemistry (2003), 46(19), 3975-3984, database is CAplus and MEDLINE.

A series of 1,5-diarylpyrazoles having a substituted benzenesulfonamide moiety as pharmacophore, e.g. (I; Ar = 2 or 3-fluoro-4-sulfamoylphenyl, 3-methyl-4-sulfamoylphenyl; R = OMe, SMe) and (II; R¹ = 4-methoxyphenyl, 4-methylthiophenyl, 4-fluorophenyl; R²= propanoyl, butyryl) was synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities. Through SAR and mol. modeling, it was found that fluorine substitution on the benzenesulfonamide moiety along with an electron-donating group at the 4-position of the 5-aryl ring yielded selectivity as well as potency for COX-2 inhibition in vitro. Among such compounds 3-fluoro-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-1-pyrazolyl]-1-benzenesulfonamide 3 displayed interesting pharmacokinetic properties along with antiinflammatory activity in vivo. Among the sodium salts tested in vivo, 10, the propionyl analog of 3, showed excellent antiinflammatory activity and therefore represents a new lead structure for the development of injectable COX-2 specific inhibitors.

Journal of Medicinal 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 C7H8FNO2S, Safety of 4-Fluoro-2-methylbenzenesulfonamide.

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