Tag: M.W=100-150

Bairagi, Keshab M. published the artcileAntidiabetic Activity of Dihydropyrimidine Scaffolds and Structural Insight by Single Crystal X-ray Studies, HPLC of Formula: 30414-53-0, the publication is Medicinal Chemistry (Sharjah, United Arab Emirates) (2020), 16(7), 996-1003, database is CAplus and MEDLINE.

This research project is designed to identify the anti-diabetic effects of the newly synthesized compounds to conclude the perspective of consuming one or more of these new synthetic compounds for diabetes management. A series of dihydropyrimidine (DHPM) derivative bearing electron releasing and electron-withdrawing substituent′s on Ph ring (a-j) were synthesized and screened for antihyperglycemic(anti-diabetic) activity on streptozotocin (STZ) induced diabetic rat model. The newly synthesized compounds were characterized by using FT-IR, m.p., ¹H and ¹³C NMR anal. The crystal structure and supramol. features were analyzed through single-crystal X-ray study. Anti-diabetic activity testing of newly prepared DHPM scaffolds was mainly based on their relative substituent on the Ph ring along with urea and thiourea. Among the synthesized DHPM scaffold, the test compound c having chlorine group on Ph ring at the ortho position to the hydropyrimidine ring with urea and Me acetoacetate derivative shows moderate lowering of glucose level. However, the title compounds Me 4-(4-hydroxy-3-methoxyphenyl)- 6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate(g) and Et 4-(3-ethoxy-4- hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate(h) having methoxy and ethoxy substituents on Ph ring show significant hypoglycemic activity compared to the remaining compounds from the Scheme 1. The exptl. rat models for the study were divided into 13 groups (n = 10); group 1 animals were treated with 0.5% CMC (0.5mL) (vehicle); group 2 were considered the streptozotocin (STZ)/nicotinamide diabetic control group (DC) and untreated, group 3 diabetic animals were administered with gliclazide 50 mg/kg and act as a reference drug group. The remaining groups of the diabetic animals were administered with the newly synthesized dihydropyrimidine compounds in a single dose of 50 mg/kg orally using the oral gavage, daily for 7 days continuously. The blood glucose level was measured before and 72 h after nicotinamide-STZ injection, for confirmation of hyperglycemia and type 2 diabetes development. Blood glucose levels were significantly (p<0.05) reduced after treatment with these derivatives The mean percentage reduction for gliclazide was 50%, while that of synthesized compounds were approx. 36%. Our result suggests that the synthesized new DHPM derivative containing alkoxy group on the Ph ring shows a significant lowering of glucose level compared to other derivatives

Medicinal Chemistry (Sharjah, United Arab Emirates) published new progress about 30414-53-0. 30414-53-0 belongs to esters-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Ketone,Ester, name is Methyl 3-oxovalerate, and the molecular formula is C6H10O3, HPLC of Formula: 30414-53-0.

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

Chan, Justin W. published the artcileThe nucleophilic, phosphine-catalyzed thiol-ene click reaction and convergent star synthesis with RAFT-prepared homopolymers, COA of Formula: C5H10O2S, the publication is Polymer (2009), 50(14), 3158-3168, database is CAplus.

The synthesis of 3-arm star polymers from reversible addition-fragmentation chain transfer (RAFT)-prepared precursor homopolymers in combination with thiol-ene click chem. is described. Homopolymers of Bu acrylate and N,N-diethylacrylamide were prepared with 1-cyano-1-methylethyl dithiobenzoate and 2,2′-azobis(2-methylpropionitrile) yielding materials with polydispersity indexes (M_w/M_n) ≤ 1.18 and controlled mol. weights as determined by a combination of NMR spectroscopy, size exclusion chromatog. (SEC), and matrix assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF MS). Subsequent one-pot reaction of homopolymer, hexylamine (HexAM), dimethylphenylphosphine (DMPP), and trimethylolpropane triacrylate (TMPTA) results in cleavage of the thiocarbonylthiol end-group (by HexAM) of the homopolymer yielding a macromol. thiol that undergoes DMPP-initiated thiol-Michael addition to TMPTA yielding 3-arm star polymers. The presence of DMPP is demonstrated to serve an important second role in effectively suppressing the presence of any polymeric disulfide as determined by SEC. Such phosphine-mediated thiol-ene reactions are shown to be extremely rapid, as verified by a combination of FTIR and NMR spectroscopies, with complete consumption of the C=C bonds occurring in a matter of min. MALDI-TOF MS and SEC were used to verify the formation of 3-arm stars. A broadening in the mol. weight distribution (M_w/M_n ∼ 1.35) was observed by SEC that was attributed to the presence of residual homopolymer and possibly 2-arm stars formed from trimethylolpropane diacrylate impurity. Interestingly, the MALDI anal. also indicated the presence of 1- and 2-arm species most likely formed from the fragmentation of the parent 3-arm star during anal. Finally, a control experiment verified that the consumption of C=C bonds does not occur via a radical pathway.

Polymer published new progress about 19788-49-9. 19788-49-9 belongs to esters-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Ester, name is Ethyl 2-mercaptopropanoate, and the molecular formula is C5H10O2S, COA of Formula: C5H10O2S.

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

Qin, Zezhao published the artcileNonswellable and Tough Supramolecular Hydrogel Based on Strong Micelle Cross-Linkings, Related Products of esters-buliding-blocks, the publication is Biomacromolecules (2019), 20(9), 3399-3407, database is CAplus and MEDLINE.

Because of the difference in osmotic pressure, most tough hydrogels swell under physiol. conditions, which seriously weakens their mech. properties, limiting their applications in biomedicine. Herein, a novel strategy based on strong and high-d. micelle cross-linkings is proposed to prepare nonswellable and tough hydrogel. To realize a strong micelle cross-linker, the synergetic effect of hydrophobic and quadruple hydrogen-bonding interactions is employed by introducing an alkyl chain-protected ureido pyrimidinone moiety into a segmented copolymer backbone. The length of the alkyl is the key factor in determining the strength of the hydrophobic interaction, which was carefully tailored to gain micelles with high strength and suitable solubility A supramol. hydrogel was formed in situ by simply linking micelle cross-linkers with poly(ethylene glycol) chains. The strong and high-d. micelle cross-linkings restrain multiple effective chains outside the micelle from stretching during swelling, and the deformability of micelle cross-linkings disperses the local stress to maintain the network with high crosslinking d. upon loading. Therefore, the hydrogel exhibited an outstanding nonswelling behavior under physiol. conditions and excellent mech. properties with a compressive strength of 4 MPa. The rapid in situ gelation also facilitated injection and cell encapsulation. Meanwhile, it also showed good tissue adhesion, cytocompatibility, and suitable degradability. This novel and facile strategy can offer new insights into the exploitation of cross-linkings to prepare nonswellable hydrogels for biomedical applications.

Biomacromolecules published new progress about 517-23-7. 517-23-7 belongs to esters-buliding-blocks, auxiliary class Tetrahydrofuran,Ketone,Ester, name is 3-Acetyldihydrofuran-2(3H)-one, and the molecular formula is C6H8O3, Related Products of esters-buliding-blocks.

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

Qin, Zezhao published the artcileInjectable and Cytocompatible Dual Cross-Linking Hydrogels with Enhanced Mechanical Strength and Stability, SDS of cas: 517-23-7, the publication is ACS Biomaterials Science & Engineering (2020), 6(6), 3529-3538, database is CAplus and MEDLINE.

Injectable hydrogels have become increasingly important in the fields of tissue engineering and drug delivery. However, their biol. applications are greatly limited by the weak mechanics and poor stability under a physiol. environment. Herein, we developed a stable, strong, and injectable hydrogel by linking strong micelle crosslinking with tetra-armed PEG. This dual crosslinking strategy has not only made hydrogels nonswelling but also maintained the relative integrity of the gel network during the degradation process, both of which work together to ensure the mech. strength and stability of our hydrogel under a physiol. environment. A compressive stress of 40 MPa was achieved at 95% strain, and the mech. properties could remain stable even after immersion into a physiol. environment for two months. Besides, it also showed outstanding antifatigue properties, good tissue adhesion, and good cytocompatibility. On the basis of these characteristics, these dual crosslinking injectable hydrogels would find appealing application in biomedicine especially for the repair of load-bearing soft tissues.

ACS Biomaterials Science & Engineering published new progress about 517-23-7. 517-23-7 belongs to esters-buliding-blocks, auxiliary class Tetrahydrofuran,Ketone,Ester, name is 3-Acetyldihydrofuran-2(3H)-one, and the molecular formula is C6H8O3, SDS of cas: 517-23-7.

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

Franzini, Maurizio published the artcileTriazolopyridazine LRRK2 kinase inhibitors, Safety of Ethyl 2-mercaptopropanoate, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(7), 1967-1973, database is CAplus and MEDLINE.

Leucine-rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson’s disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series of [1,2,4]triazolo[4,3-b]pyridazines that are potent against both wild-type and mutant LRRK2 kinase activity in biochem. assays and show an unprecedented selectivity towards the G2019S mutant. A structural rational for the observed selectivity is proposed.

Bioorganic & Medicinal Chemistry Letters published new progress about 19788-49-9. 19788-49-9 belongs to esters-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Ester, name is Ethyl 2-mercaptopropanoate, and the molecular formula is C5H10O2S, Safety of Ethyl 2-mercaptopropanoate.

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

Yildirim, Hatice published the artcileNatural-product-inspired design and synthesis of thiolated coenzyme Q analogs as promising agents against Gram-positive bacterial strains: insights into structure-activity relationship, activity profile, mode of action, and molecular docking, Name: Ethyl 2-mercaptopropanoate, the publication is RSC Advances (2022), 12(32), 20507-20518, database is CAplus and MEDLINE.

In an attempt to develop effective and potentially active antibacterial and/or antifungal agents, we designed, synthesized, and characterized thiolated CoQ analogs (CoQ1-8) with an extensive antimicrobial study. The antimicrobial profile of these analogs was determined using four Gram-neg. bacteria, three Gram-pos. bacteria, and three fungi. Because of the fact that the thiolated CoQ analogs were quite effective on all tested Gram-pos. bacterial strains, including Staphylococcus aureus (ATCC 29213) and Enterococcus faecalis (ATCC 29212), the first two thiolated CoQ analogs emerged as potentially the most desirable ones in this series. Importantly, after the evaluation of the antibacterial and antifungal activity, we presented an initial structure-activity relationship for these CoQ analogs. In addition, the most promising thiolated CoQ analogs (CoQ1 and CoQ2) having the lowest MIC values on all tested Gram-pos. bacterial strains, were further evaluated for their inhibition capacities of biofilm formation after evaluating their in vitro potential antimicrobial activity against each of 20 clin. obtained resistant strains of Gram-pos. bacteria. CoQ1 and CoQ2 exhibited potential mol. interactions with S. aureus DNA gyrase in addition to excellent pharmacokinetics and lead-likeness profiles. Our findings offer important implications for a potential antimicrobial drug candidate, in particular for the treatment of infections caused by clin. resistant MRSA isolates.

RSC Advances published new progress about 19788-49-9. 19788-49-9 belongs to esters-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Ester, name is Ethyl 2-mercaptopropanoate, and the molecular formula is C24H20Ge, Name: Ethyl 2-mercaptopropanoate.

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

Hu, Deqing published the artcileBiaryl and atropisomeric biaryl aldehyde synthesis by one-step, metal-free benzannulation of aryl enals and propiolates, Formula: C7H13NO2, the publication is Green Chemistry (2020), 22(20), 6773-6777, database is CAplus.

A new method involving the benzannulation of aromatic enals ArCH=CHCHO (Ar = C₆H₅, 2-furyl, 1-naphthyl, etc.) and two alkyl propiolate mols. CHCC(O)₂R (R = Me, Et, t-Bu) has been developed as a powerful route to biaryl aldehydes I simply via the promotion of di-Me amine. The benzannulation process in the absence of an oxidant additive tolerates successfully the formyl group in the enal component, leading to a straightforward one-step synthesis of biaryl and atropisomeric aldehydes I. An enamine activation based on the aza-Michael addition of di-Me amine to the propiolate and the amine elimination-based generation of cyclohexadiene intermediate constitute the major factors enabling the titled reactions.

Green Chemistry published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, Formula: C7H13NO2.

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

Shen, Yanjia published the artcileThe histone deacetylase inhibitor belinostat ameliorates experimental autoimmune encephalomyelitis in mice by inhibiting TLR2/MyD88 and HDAC3/ NF-κB p65-mediated neuroinflammation, Quality Control of 624-49-7, the publication is Pharmacological Research (2022), 105969, database is CAplus and MEDLINE.

Multiple sclerosis (MS) is a Th cell-mediated inflammatory demyelinating autoimmune disease. MS cannot be cured, and long-term drug treatment is still needed for MS patients. In this study, we examined the effect of belinostat, a pan-histone deacetylase inhibitor (HDACi), on exptl. autoimmune encephalomyelitis (EAE) and elucidated its mechanism of action. We found that belinostat alleviates the clin. symptoms, histopathol. central nervous system (CNS) inflammation and demyelination outcomes in EAE mice. Compared to the MS oral drug di-Me fumarate (DMF) (100 mg/kg), belinostat (30 mg/kg) treatment exhibited better efficacy in improving the clin. symptoms of EAE mice. Belinostat treatment significantly suppressed the activation of M1 microglia and the proinflammatory cytokine expression; but it had no effects on the M2 microglial polarization. Belinostat also decreased both NO and iNOS levels in LPS-stimulated BV2 microglia. Accordingly, belinostat treatment of EAE mice significantly inhibited activation of the TLR2/MyD88 signaling pathway and downregulated the expression of HDAC3 while upregulating the acetylated NF-κB p65 levels. Taken together, these data demonstrate for the first time that belinostat ameliorates EAE in mice through inhibiting neuroinflammation via suppressing M1 microglial polarization, and implicating belinostat as a potential candidate for the treatment of multiple sclerosis.

Pharmacological Research published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C9H7NO4, Quality Control of 624-49-7.

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

Cao, Jilei published the artcileMetal-free hydrogen evolution cross-coupling enabled by synergistic photoredox and polarity reversal catalysis, Application of Ethyl 2-mercaptopropanoate, the publication is Green Chemistry (2021), 23(22), 8988-8994, database is CAplus.

A synergistic combination of photoredox and polarity reversal catalysis enabled a hydrogen evolution cross-coupling of silanes with H₂O, alcs., phenols, and silanols, which afforded the corresponding silanols, monosilyl ethers, and disilyl ethers, resp., in moderate to excellent yields. The dehydrogenative cross-coupling of Si-H and O-H proceeded smoothly with broad substrate scope and good functional group compatibility in the presence of only an organophotocatalyst 4-CzIPN and a thiol HAT catalyst, without the requirement of any metals, external oxidants and proton reductants, which is distinct from the previously reported photocatalytic hydrogen evolution cross-coupling reactions where a proton reduction cocatalyst such as a cobalt complex is generally required. Mechanistically, a silyl cation intermediate is generated to facilitate the cross-coupling reaction, which therefore represents an unprecedented approach for the generation of silyl cation via visible-light photoredox catalysis.

Green Chemistry published new progress about 19788-49-9. 19788-49-9 belongs to esters-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Ester, name is Ethyl 2-mercaptopropanoate, and the molecular formula is C5H10O2S, Application of Ethyl 2-mercaptopropanoate.

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

Wang, Mengdan published the artcileSelective Synthesis of Pyrano[3,2-b]indoles or Cyclopenta[b]indoles Tethered with Medium-Sized Rings via Cascade C-C σ-Bond Cleavage and C-H Functionalization, Application of 3-Acetyldihydrofuran-2(3H)-one, the publication is Journal of Organic Chemistry (2021), 86(1), 683-692, database is CAplus and MEDLINE.

Highly atom-economical tandem reactions have been developed for the synthesis of pyrano[3,2-b]indoles or cyclopenta[b]indoles tethered with 7-, 8-, or 9-membered rings. These reactions first undergo a carbon-carbon σ-bond cleavage reaction of cyclic β-ketoesters. Next, in the presence of CuCl₂ and Ag₂CO₃, intramol. O-H/C-H coupling occurs to give pyrano[3,2-b]indoles. This is the first example for capture of the enoloxyl radical of the intramol. C-O bond formation reaction, whereas C3 nucleophilic addition afforded cyclopenta[b]indoles using TsOH·H₂O.

Journal of Organic Chemistry published new progress about 517-23-7. 517-23-7 belongs to esters-buliding-blocks, auxiliary class Tetrahydrofuran,Ketone,Ester, name is 3-Acetyldihydrofuran-2(3H)-one, and the molecular formula is C8H6ClN, Application of 3-Acetyldihydrofuran-2(3H)-one.

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