Category: amides-buliding-blocks

Odiaka, Timothy I. published the artcileNew tricarbonyl(amido-substituted-1,3-diene)iron complexes, Related Products of amides-buliding-blocks, the publication is Journal of Organometallic Chemistry (1985), 288(2), C30-C32, database is CAplus.

Benzamides I (R = H, 2-OH, 4-MeO, 3-MeO, 3,5-(MeO)₂, 4-Cl, 2,4-Cl₂) added reversibly to the dienyl rings of II (R¹ = H, MeO; n = 1, 2) to give III.

Journal of Organometallic 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 C7H5Cl2NO, Related Products of amides-buliding-blocks.

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

Sabeti Azad, Mahnaz published the artcileFluorescent Aminoglycoside Antibiotics and Methods for Accurately Monitoring Uptake by Bacteria, Recommanded Product: 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, the publication is ACS Infectious Diseases (2020), 6(5), 1008-1017, database is CAplus and MEDLINE.

Characterizing how multidrug-resistant bacteria circumvent the action of clin. used or novel antibiotics requires a detailed understanding of how the antibiotics interact with and cross bacterial membranes to accumulate in the cells and exert their action. When monitoring the interactions of drugs with bacteria, it remains challenging to differentiate functionally relevant internalized drug levels from nonspecific binding. Fluorescence is a method of choice for observing dynamics of biomols. In order to facilitate studies involving aminoglycoside antibiotics, we have generated fluorescently labeled aminoglycoside derivatives with uptake and bactericidal activities similar, albeit with a moderate loss, to those of the parent drug. The method combines fluorescence microscopy with fluorescence-activated cell sorting (FACS) using neomycin coupled to nonpermeable cyanine dyes. Fluorescence imaging allowed membrane-bound antibiotic to be distinguished from mols. in the cytoplasm. Patterns of uptake were assigned to different populations in the FACS anal. Our study illustrates how fluorescent derivatives of an aminoglycoside enable a robust characterization of the three components of uptake: membrane binding, EDPI, and EDPII. Because EDPI levels are weak compared to the two other types of accumulation and critical for the action of these drugs, the three components of uptake must be taken into account sep. when drawing conclusions about aminoglycoside function.

ACS Infectious Diseases 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

Pejman, Laleh published the artcileThe effect of adenosine A2A and A2B antagonists on tracheal responsiveness, serum levels of cytokines and lung inflammation in guinea pig model of asthma, Formula: C27H29N5O5, the publication is Advanced Pharmaceutical Bulletin (2014), 4(2), 131-138, 8 pp., database is CAplus and MEDLINE.

Nowadays adenosine is specified as an important factor in the pathophysiol. of asthma. For determining the effect of different A2 receptors, in this investigation the effect of single dose of selective adenosine A2A and A2B antagonists (ZM241385 and MRS1706) on different inflammatory parameters; tracheal responsiveness to methacholine and ovalbumin, total and differential cell count in bronchoalveolar lavage (BAL), blood levels of IL-4 and IFN-γ and lung pathol. of guinea pig model of asthma were assessed. All mentioned parameters were evaluated in 2 sensitized groups of guinea pigs pretreated with A2A and A2B antagonists (S+Anta A2A, S+Anta A2B) compared with sensitized (S) and control (C) groups. The tracheal responsiveness to methacholine and OA, total cell and eosinophil and basophil count in BAL, blood IL-4 level and pathol. changes in pretreated group with MRS1706 (S+Anta A2B) was significantly lower than those of sensitized group. In pretreated group with Anta A2A(S+Anta A2A), all the above changes were reversed. These results showed a preventive effect of A2B antagonist (MRS1706) on tracheal responsiveness to methacholine and OA, total and differential cell count in bronchoalveolar lavage, blood cytokines and pathol. changes. Administration of ZM241385, selective A2A antagonist, deteriorated the induction effect of ovalbumin.

Advanced Pharmaceutical Bulletin published new progress about 264622-53-9. 264622-53-9 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Adenosine Receptor, name is N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide, and the molecular formula is C27H29N5O5, Formula: C27H29N5O5.

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

Delledonne, Andrea published the artcileBis-isonicotinoyl linkers containing polyaromatic scaffolds: synthesis, structure and spectroscopic properties, Safety of Isonicotinamide, the publication is Physical Chemistry Chemical Physics (2022), 24(2), 1191-1201, database is CAplus and MEDLINE.

New synthesis of extended linkers containing different polyaromatic chromophores functionalized with isonicotinoyl moieties I (R = 3,7-naphthalene-diyl, biphenyl-4,4′-diyl, fluorene-2,7-diyl, etc.) have been synthesized by Pd-catalyzed cross-coupling reactions involving isonicotinamide and the appropriate aromatic dibromides such as 2,6-dibromonaphthalene, 2,7-dibromofluorene, 9,10-dibromoanthracene, etc. The optimized protocol led to the isolation of the target mols. in good yield and with high purity. Electronic absorption and emission spectra were collected both in solution (DMF) and in the solid state. TDDFT calculations were carried out to investigate the effect of the isonicotinoyl moieties on the spectral features of the central chromophores.

Physical Chemistry Chemical Physics 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 C6H6N2O, Safety of Isonicotinamide.

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

Gholivand, Khodayar published the artcileN-2,4-dichlorobenzoyl phosphoric triamides: Synthesis, spectroscopic and x-ray crystallography studies, Synthetic Route of 2447-79-2, the publication is Journal of Chemical Sciences (Bangalore, India) (2010), 122(4), 549-559, database is CAplus.

New phosphoric triamides (R¹P(O)Cl₂, 1; R¹P(O)(OH)₂, 2; R¹P(O)(NHCH₂CH=CH₂)₂, 3; R¹P(O)[NHCH(CH₃)₂]₂, 4; R¹P(O)[NH-C(CH₃)₃]₂, 5; R¹P(O)(NHCH₂-C₄H₃O)₂, 6; R¹P(O)(NHCH₂C₆H₅)₂, 7; R¹P(O)[N(CH₃)(CH₂C₆H₅)]₂, 8; R¹P(O)[NHCH(CH₃)(C₆H₅)]₂, 9; R¹ = 2,4-Cl₂-C₆H₃C(O)NH) were synthesized by the reaction of N-2,4-dichlorobenzoyl phosphoramidic dichloride with various cyclic aliphatic amines and the products were characterized by ¹H, ¹³C, ³¹P NMR, IR spectroscopy and elemental anal. Surprisingly, the ¹H NMR spectrum of 2 indicated long range ⁶J (P, H) coupling constant = 1.3, 1.4 Hz and those of mols. 3, 4, 6–8 display long-range ⁴J (H, H) coupling constants (1.8-1.9 Hz) for the coupling of aromatic protons in 2,4-dichlorophenyl rings. ¹H NMR spectra indicated ³J (PNCH) for enantiotopic and diastereotopic benzylic CH₂ protons in compounds 7 and 8. The spectroscopic data of newly synthesized compounds were compared with those related N-benzoyl derivatives The structures of compounds 5, 8 and 10 (2,4-Cl₂-C₆H₃C(O)NHP(O)[N(CH₂CH(CH₃)₂)₂]₂) have been determined by x-ray crystallog. The structures form centrosym. dimers through intermol. strong -P=O…H-N-hydrogen bonds. The dimers connect to each other via rather strong and weak C-H…O plus weak C-H…Cl H-bonds to produce a 1-D network for 5 while 3-D polymeric chains for 8 and 10.

Journal of Chemical Sciences (Bangalore, India) 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

Gholivand, Khodayar published the artcileNew phosphoric triamides: chlorine substituents effects and polymorphism, Safety of 2,4-Dichlorobenzamide, the publication is Heteroatom Chemistry (2010), 21(3), 168-180, database is CAplus.

New phosphoric triamides 1–10 were synthesized by the reaction of N-2,4-dichlorobenzoyl phosphoramidic dichloride with various cyclic aliphatic amines, and the products were characterized by ¹H, ¹³C, ³¹P NMR, and IR spectroscopy and elemental anal. Surprisingly, the ¹H NMR spectra of compounds 1–7 demonstrate long-range ⁴J(H,H) coupling constant from 1.5 to 1.9 Hz. Comparison of the NMR and IR spectra of N-benzoyl, N-4-chlorobenzoyl, and N-2,4-dichlorobenzoyl phosphoric triamide analogs indicates that N-2,4-dichlorobenzoyl derivatives have the most upfield δ(³¹P) and the highest ν(C=O) values. The crystal structures of 3, 4, 6, 6a, and 10 have been determined by x-ray crystallog. Interestingly, the structures of 6 and 6a are polymorphic. All structures form dimers through strong, intermol. -P=O···H-N- hydrogen bonds. The dimers connect to each other via weak C-H···Cl and C-H···OH- bonds to produce two-dimensional polymeric chains for 4 and three-dimensional networks for others. Among new synthesized N-2,4-dichlorobenzoyl phosphoric triamides, one indicated polymorphism. All structures were characterized by ¹H, ¹³C, ³¹P NMR, and IR spectroscopy and elemental anal. © 2010 Wiley Periodicals, Inc. Heteroatom Chem 21:168-180, 2010; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20592.

Heteroatom 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 C7H5Cl2NO, Safety of 2,4-Dichlorobenzamide.

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

Gholivand, Khodayar published the artcileNew N-nicotinyl and N-2,4-dichlorobenzoyl phosphorictriamides: syntheses, spectroscopic study, and crystal structures, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Main Group Chemistry (2008), 7(4), 251-269, database is CAplus.

New phosphoric triamides, ArC(O)NHP(O)(NR₂)₂ [R = iBu, Ar = 3-pyridyl (1), Ph (6); Ar = 2,4-Cl₂C₆H₄, R = Et (2), n-Pr (3), n-Bu (4), iBu (5)] were synthesized and characterized by ¹H, ¹³C, ³¹P NMR, IR spectroscopy and elemental anal. It is noteworthy that as far as is known there were not any efforts for the synthesis of phosphoric triamides with nicotinamide substituent up to now and compound 1 is the 1st example of this series. Compounds 1, 5, 6 indicate the coupling of diastereotopic CH₂ protons with each other, CH proton and the corresponding P atom in ¹H NMR spectra as well as two separated signals for the two CH₃ moieties in ¹³C NMR spectra. The ¹H NMR spectrum of compound 5 demonstrates long-range ⁶J_P,H coupling constant Also, long-range ⁴J_H,H coupling constant appeared for the aromatic protons of mols. 1–4. Also, the structures were determined for 2–4 by x-ray crystallog.

Main Group 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 C7H5Cl2NO, Recommanded Product: 2,4-Dichlorobenzamide.

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

Hamoud, Mohamed M. S. published the artcileDesign and Synthesis of Novel 1,3,4-Oxadiazole and 1,2,4-Triazole Derivatives as Cyclooxygenase-2 Inhibitors with Anti-inflammatory and Antioxidant activity in LPS-stimulated RAW264.7 Macrophages, SDS of cas: 169590-42-5, the publication is Bioorganic Chemistry (2022), 105808, database is CAplus and MEDLINE.

In an attempt to obtain new candidates with potential anti-inflammatory activity, two series of 1,3,4-oxadiazole based derivatives (8a-g) and 1,2,4-triazole based derivatives (10a,b and 11a-g) were synthesized and evaluated for their COX-1/COX-2 inhibitory activity. In vitro assays showed potent COX-2 inhibitory activity and selectivity of the novel designed compounds (IC₅₀ = 0.04 – 0.16 μM, SI = 60.71 – 337.5) compared to celecoxib (IC₅₀ = 0.045 μM, SI = 326.67). The anti-inflammatory and antioxidant activity of the synthesized compounds was investigated via testing their ability to inhibit pro-inflammatory [tumor necrosis factor (TNF-α) and interleukin-6 (IL-6)] and oxidative stress [nitric oxide (NO) and reactive oxygen species (ROS)] markers production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages. Most of the novel compounds exhibited potent anti-inflammatory and antioxidant activity. In particular, the novel compounds showed excellent IL-6 inhibitory activity (IC₅₀ = 0.96 – 11.14 μM) when compared to celecoxib (IC₅₀ = 13.04 μM) and diclofenac sodium (IC₅₀ = 22.97 μM). Moreover, the most potent and selective COX-2 inhibitor 11c (IC₅₀ = 0.04 μM, SI = 337.5) displayed significantly higher activity against NO and ROS production compared to celecoxib (IC₅₀ = 2.60 and 3.01 μM vs. 16.47 and 14.30 μM, resp.). Mol. modeling studies of the novel designed mols. into COX-2 active sites analyzed their binding affinity. In-silico simulation studies indicated their acceptable physicochem. properties and pharmacokinetic profiles. This study suggests that the novel synthesized COX-2 inhibitors exert potent anti-inflammatory and antioxidant activity, highlighting their potential as promising therapeutic agents for the treatment of inflammation and oxidative stress-related diseases.

Bioorganic Chemistry 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, SDS of cas: 169590-42-5.

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

Kirin, Srecko I. published the artcileCellular uptake quantification of metalated peptide and peptide nucleic acid bioconjugates by atomic absorption spectroscopy, Quality Control of 186046-83-3, the publication is Angewandte Chemie, International Edition (2008), 47(5), 955-959, database is CAplus and MEDLINE.

At. absorption spectroscopy (AAS) of cobalt atoms is used as an accurate method to determine the cellular uptake and nuclear localization of metal bioconjugates. Surprisingly, the PNA conjugates show highest uptake efficiency, and an accumulation 150% higher than in the culture medium is achieved.

Angewandte Chemie, International Edition 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 C40H35N7O8, Quality Control of 186046-83-3.

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

Heard, Nina E. published the artcileThe synthesis of several novel triazine ring hydrolysis products of N-[[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)amino]carbonyl]-2-(3,3,3-trifluoropropyl)benzenesulfonamide, Computed Properties of 94125-42-5, the publication is Journal of Heterocyclic Chemistry (1995), 32(5), 1621-4, database is CAplus.

The syntheses of four hydrolysis products, 2-F₃C(CH₂)₂C₆H₄SO₂NHCOR (R = NHCONHCONHAc, NHCONHCONH₂, NHCONH₂, NH₂), isolated from environmental studies on the title compound (CGA-152005) are reported. Spectral comparison of these synthetic standards with study isolates provided proof for sulfonyl urea intact triazine ring hydrolysis.

Journal of Heterocyclic Chemistry published new progress about 94125-42-5. 94125-42-5 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Sulfamide,Amine,Benzene, name is 2-(3,3,3-Trifluoropropyl)benzenesulfonamide, and the molecular formula is C9H10F3NO2S, Computed Properties of 94125-42-5.

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