Category: amides-buliding-blocks

Raldua, Demetrio published the artcileBLT-1, a specific inhibitor of the HDL receptor SR-BI, induces a copper-dependent phenotype during zebrafish development, Formula: C12H23N3S, the publication is Toxicology Letters (2007), 175(1-3), 1-7, database is CAplus and MEDLINE.

Block lipid transport-1 (BLT-1) is a small chem. widely used to inhibit the transfer of lipids between high-d. lipoproteins (HDL) and cells mediated by scavenger receptor B, type 1 (SR-BI). This study demonstrated that BLT-1 induced in zebrafish (Danio rerio) embryos a copper-dependent phenotype with a twisted notochord, brain ventricle enlargement, and absence of melanization, phenocopying neocuproine-treated, or calamity mutants. This finding supports an unexpected link between copper availability and SR-BI activity. The copper-chelating activity of BLT-1, revealed by its dramatic effect during embryo development, should be considered in any evaluation of the pharmacol. effect of this thiosemicarbazone derivative on SR-BI activity and the potential therapeutic value of this mol.

Toxicology Letters published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Formula: C12H23N3S.

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

Dabaeva, V. V. published the artcileSynthesis and Neurotropic Activity of Novel Condensed Cyclopentanopyrido[3′,2′:4,5]-thieno[3,2-D]pyrimidine Derivatives, Recommanded Product: 2-Chloroacetamide, the publication is Pharmaceutical Chemistry Journal (2020), 54(7), 707-713, database is CAplus.

2-Oxo-2,5,6,7-tetrahydro-3-cyano-1H-cyclopenta[b]pyridine was used as the starting point to develop an accessible synthesis of condensed cyclopentanopyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine derivatives I [R = NHNH₂, SC₄H₉, SCH₂CONH₂, etc.] and II [R¹ = C₅H₁₁, CH₂CONH₂, CH₂CH₂OMe, etc.]. The neurotropic activity of these compounds was studied, and a number of them showed anticonvulsant activity as antagonism to corasol. 2-Chloro-6,7-dihydro-5H-cyclepenta[b]pyridine-3-carbonitrile like diazepam, had anti-anxiety and activating effects, while the other compounds had sedative activity.

Pharmaceutical Chemistry Journal published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Recommanded Product: 2-Chloroacetamide.

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

Dabaeva, V. V. published the artcileSynthesis, Neurotropic Activity, and Molecular Docking of New Condensed Thieno[2,3-b]pyridine Derivatives, SDS of cas: 79-07-2, the publication is Russian Journal of Bioorganic Chemistry (2022), 48(1), 125-134, database is CAplus.

Methods for the preparation of new condensed derivatives of pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines based on 5,6-dimethyl-2-oxo-1,2-dihydropyridine-3-carbonitrile were developed. Substitution reactions in the 3rd and 4th positions of 7,8-dimethylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-one were conducted. The neurotropic activity of 12 obtained compounds was studied in vivo in rats and mice. Eight compounds were found to have an anticonvulsant effect of antagonism with corazole. Four selected compounds had anxiolytic and behavior activating effects. Mol. docking of the synthesized compounds was performed to predict their interaction with the GABAA receptor. Five compounds were identified, the complexation of which with the GABAA receptor occurs in two places: the benzamidine site of subsite 1 and subsite 3 of the ECD interface, which indicates the inhibitory effect of the compounds on the target.

Russian Journal of Bioorganic Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, SDS of cas: 79-07-2.

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

Hou, Chunyan published the artcileA hyaluronan-based nanosystem enables combined anti-inflammation of mTOR gene silencing and pharmacotherapy, Quality Control of 1869-45-0, the publication is Carbohydrate Polymers (2018), 339-348, database is CAplus and MEDLINE.

Accompanied by overproduction of oxidants and reduction of pH, inflammation is closely related to many diseases such as cancer, atherosclerosis, and asthma. Besides chemotherapeutic agents, the potential regulative role of autophagy in inflammation is being actively investigated. RNA interference (RNAi)-based gene therapy is widely explored for clin. therapy but seriously restricted by lack of suitable carriers. In this study, we synthesized a hyaluronan-based ROS-sensitive polymer which was expected to release loaded chem. drugs in inflammatory environment and further developed a stable and nontoxic co-delivery nanosystem of siRNA targeting autophagy suppressive gene and chemotherapeutic agents. The in vitro transfection study of this nanosystem revealed improved intracellular accumulation of siRNA and excellent gene silencing efficacy comparable to that of conventional cationic liposome. Moreover, the mRNA expression of inflammatory cytokines was remarkably decreased by our nanosystem. Considering its biocompatibility, transfection efficacy, and anti-inflammatory capability, this co-delivery nanosystem proclaimed to be a promising combined therapeutic strategy for enhanced anti-inflammatory therapy.

Carbohydrate Polymers 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, Quality Control of 1869-45-0.

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

Wang, Jun-Xia published the artcileLy6G ligation blocks recruitment of neutrophils via a β2-integrin-dependent mechanism, SDS of cas: 321673-30-7, the publication is Blood (2012), 120(7), 1489-1498, database is CAplus and MEDLINE.

Ly6G is a glycosylphosphatidylinositol (GPI)-anchored protein of unknown function that is commonly targeted to induce exptl. neutrophil depletion in mice. In the present study, we found that doses of anti-Ly6G Abs too low to produce sustained neutropenia remained capable of inhibiting exptl. arthritis, leaving joint tissues free of infiltrating neutrophils. Thioglycollate-stimulated peritonitis was also attenuated. No alteration in neutrophil apoptosis was observed, implicating impaired recruitment. Indeed, Ly6G ligation abrogated neutrophil migration toward LTB₄ and other chemoattractants in a transwell system. Exploring the basis for this blockade, we identified colocalization of Ly6G and β2-integrins by confocal microscopy and confirmed close association by both coimmunoprecipitation and fluorescence lifetime imaging microscopy. Anti-Ly6G Ab impaired surface expression of β2-integrins in LTB₄-stimulated neutrophils and mimicked CD11a blockade in inhibiting both ICAM-1 binding and firm adhesion to activated endothelium under flow conditions. Correspondingly, migration of β2-integrin-deficient neutrophils was no longer inhibited by anti-Ly6G. These results demonstrate that exptl. targeting of Ly6G has functional effects on the neutrophil population and identify a previously unappreciated role for Ly6G as a modulator of neutrophil migration to sites of inflammation via a β2-integrin-dependent mechanism.

Blood published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C4H6O3, SDS of cas: 321673-30-7.

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

Cooper, Geoffrey K. published the artcileAn ortho-directing effect in the nucleophilic aromatic substitution reactions of primary and secondary 2,4-dichloro- and 2,3,4-trichlorobenzamides with ethanethiolate, Computed Properties of 2447-79-2, the publication is Synthetic Communications (1995), 25(6), 899-906, database is CAplus.

The reactions of the primary and secondary 2,4-dichlorobenzamides and 2,3,4-trichlorobenzamides with potassium ethanethiolate in DMF were shown to proceed with a remarkable degree of ortho-regioselectivity. This effect was found to be absent using related tertiary amides as substrates. For example, treatment of 2,3,4-trichlorobenzamide with potassium ethanethiolate in DMF gave 3,4-dichloro-2-(ethylthio)benzamide.

Synthetic Communications 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, Computed Properties of 2447-79-2.

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

Abuelhassan, Suzan published the artcileSynthesis, characterization, and biological activities of some novel thienylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines and related heterocycles, Formula: C2H4ClNO, the publication is Journal of Heterocyclic Chemistry (2021), 58(9), 1784-1801, database is CAplus.

3-Cyano-5-ethoxycarbonyl-6-methyl-4-(2′-thienyl)-pyridine-2(1H)-thione was synthesized and reacted with chloroacetonitrile or chloroacetamide to give I [R¹ = cyano, carbamoyl; R² = amino], resp. Cyclocondensation of I [R¹ = carbamoyl; R² = amino] with triethylorthoformate produced the corresponding pyridothienopyrimidineone II [R³ = hydroxy], which on heating with phosphorus oxychloride gave 4-chloropyrimidine derivative II [R³ =chloro]. Compound II [R³ = chloro] was used as key intermediate for synthesizing compounds II [R³ = sulfanyl, hydrazino, piperidyl, morpholino, (3-phenyl-1H-1,2,4-triazol-5-yl)sulfanyl] upon treatment with some nucleophilic reagents such as thiourea, hydrazine hydrate, piperidine, morpholine, or 5-phenyl-s-triazole-3(1H)-thione, resp. Reaction of pyridothienopyrimidinethione II [R³ = sulfanyl] with N-(4-tolyl)-2-chloroacetamide or Et bromoacetate afforded the corresponding S-substituted methylsulfanylpyrimidines II [R³ = [2-(4-methylanilino)-2-oxo-ethyl]sulfanyl, (2-ethoxy-2-oxo-ethyl)sulfanyl]. The condensation of I [R¹ = cyano; R² = amino] with triethylorthoformate gave azomethine derivative I [R¹ = cyano; R² = ethoxymethyleneamino], which was reacted with hydrazine hydrate to give compound III [R⁴ = amino]. Compounds II [R³ = hydrazino] and III [R⁴ = amino] were used as precursors for synthesizing other new thienylpyridothienopyrimidines as well as isomeric thienyl-s-triazolopyridothieno- pyrimidines. All synthesized compounds were characterized by elemental and spectral analyses such as IR, ¹H NMR, and ¹³C NMR. In addition, majority of synthesized compounds were tested for their antifungal activity against five strains of fungi. Moreover, compounds I [R¹ = carbamoyl; R² = amino], II [R³ = chloro, sulfanyl, (2-ethoxy-2-oxo-ethyl)sulfanyl], and III [R⁴ = 2-thienylmethyleneamino] were screened for their anticancer activity against HEPG-2 and MCF-7 cell lines.

Journal of Heterocyclic Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Formula: C2H4ClNO.

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

Alexander, Rikki published the artcile4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase, Quality Control of 14294-10-1, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(15), 4316-4320, database is CAplus and MEDLINE.

4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo profiling of compound 18 (I) is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth.

Bioorganic & Medicinal Chemistry Letters published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Quality Control of 14294-10-1.

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

Li, Huifang published the artcileDiscovery of Small-Molecule Inhibitors Selectively Targeting the DNA-Binding Domain of the Human Androgen Receptor, COA of Formula: C5H10N2OS, the publication is Journal of Medicinal Chemistry (2014), 57(15), 6458-6467, database is CAplus and MEDLINE.

The human androgen receptor (AR) is considered as a master regulator in the development and progression of prostate cancer (PCa). As resistance to clin. used anti-AR drugs remains a major challenge for the treatment of advanced PCa, there is a pressing need for new anti-AR therapeutic avenues. In this study, we identified a binding site on the DNA binding domain (DBD) of the receptor and utilized virtual screening to discover a set of micromolar hits for the target. Through further exploration of the most potent hit (1), a structural analog (6) was identified demonstrating 10-fold improved anti-AR potency. Further optimization resulted in a more potent synthetic analog (25) with anti-AR potency comparable to a newly FDA-approved drug Enzalutamide. Site-directed mutagenesis demonstrated that the developed inhibitors do interact with the intended target site. Importantly, the AR DBD inhibitors could effectively inhibit the growth of Enzalutamide-resistant cells as well as block the transcriptional activity of constitutively active AR splice variants, such as V7.

Journal of Medicinal Chemistry published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, COA of Formula: C5H10N2OS.

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

Li, Huifang published the artcileCorrection to Discovery of Small-Molecule Inhibitors Selectively Targeting the DNA-Binding Domain of the Human Androgen Receptor [Erratum to document cited in CA161:328452], Application of Morpholine-4-carbothioamide, the publication is Journal of Medicinal Chemistry (2017), 60(3), 1225, database is CAplus and MEDLINE.

In the original publication on page 6458, The abstract graphic shows the incorrect isomer; the correction is provided here. In the original publication on Page 6460, In line 22 of the right-hand column, the group should be “-OCH₃” instead of “-OCHH₃“; the correction is provided here. In the original publication, on page 6461,In lines 9 and 35 of the left-hand column, the compound should be “2,4-dibromoimidazole” instead of “4,5-dibromoimidazole”; the correction is provided here. In the original publication, on page 6462, in table 3, the structure for ring A in the compound is incorrect; the correction is provided here. In the original publication on Page 6463, Figure 3D is incorrect; the correction is provided here. In the original publication, ob Page 6464, In the right-hand column in the second line from the bottom, the compound should be “4-(4-(2,4-Dibromo-1Himidazol-1-yl)thiazol-2-yl)morpholine instead of “4-(4-(4,5-Dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine”; the correction is provided here.

Journal of Medicinal Chemistry published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Application of Morpholine-4-carbothioamide.

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