Tag: M.W=100-150

Sato, Motohide published the artcileQuinolone Carboxylic Acids as a Novel Monoketo Acid Class of Human Immunodeficiency Virus Type 1 Integrase Inhibitors, SDS of cas: 924-99-2, the publication is Journal of Medicinal Chemistry (2009), 52(15), 4869-4882, database is CAplus and MEDLINE.

The synthesis and detailed structure-activity relationship of quinolonecarboxylic acids as a novel monoketo acid class of HIV-1 integrase inhibitors was presented. Compounds I (R = t-Bu), which showed an IC₅₀ of 5.8 nM in the strand transfer assay and an ED₅₀ of 0.6 nM in the antiviral assay, and I (R = i-Pr), which had an IC₅₀ of 7.2 nM and an ED₅₀ of 0.9 nM, were the most potent compounds in this class. The monoketo acid I (R = i-Pr) was much more potent at inhibiting integrase-catalyzed strand transfer processes than 3′-processing reactions, as is the case with the keto-enol acids. Elvitegravir I (R = i-Pr) was chosen as a candidate for further studies and was reported as being in phase 3 clin. trials.

Journal of Medicinal 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, SDS of cas: 924-99-2.

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

Miyauchi, Rie published the artcileDesign, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria, Quality Control of 924-99-2, the publication is Bioorganic & Medicinal Chemistry (2009), 17(19), 6879-6889, database is CAplus and MEDLINE.

A series of novel 6-desfluoro [des-F(6)] and 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methoxyquinolones bearing 3-(1-aminocycloalkyl)pyrrolidin-1-yl substituents at the C-7 position (1-6) was synthesized to obtain potent drugs for nosocomial infections caused by Gram-pos. pathogens. The des-F(6) compounds 4-6 exhibited at least four times more potent activity against representative Gram-pos. bacteria than ciprofloxacin or moxifloxacin. Among the derivatives, 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] derivative 4, which showed favorable profiles in preliminary toxicol. and non-clin. pharmacokinetic studies, exhibited potent antibacterial activity against clin. isolated Gram-pos. pathogens that had become resistant to one or more antibiotics.

Bioorganic & Medicinal 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, Quality Control of 924-99-2.

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

Taib, Layla Ahmed published the artcileSolvent-free synthesis of 4-substituted coumarins catalyzed by novel Bronsted acidic ionic liquids with perchlorate anion: a convenient and practical complementary method for pechmann condensation, Safety of 3-Acetyldihydrofuran-2(3H)-one, the publication is Reaction Kinetics, Mechanisms and Catalysis (2021), 133(1), 383-403, database is CAplus.

Herein, three novel sulfonic-functionalized Bronsted acidic ionic liquids containing perchlorate anion counterparts e.g., I were prepared These ionic liquid catalysts e.g., I were prepared through simple and ecofriendly procedures and then applied as efficient catalysts with high yields under solvent-free conditions for the synthesis of 4-substituted coumarins e.g., II through the Pechmann condensation of different phenols e.g., naphthalen-1-ol and β-ketoesters R(O)CH(R¹)C(O)OR² [R = Me, Ph; R¹ = H; R² = Et; R¹R² = -(CH₂)₂-]. Compared to previous works, the proposed method offers several benefits, such as cleaner reactions, decreased reaction times, high yields, and the lack of laborious workup or purification procedures. Particularly, these catalysts make the condensation of less activated phenols feasible. Besides the described benefits, this advanced protocol was applied successfully for the synthesis of coumarins e.g., III from γ-lactone as 3-acetyldihydrofuran-2(3H)-one. The simplicity in operation, applicability and feasibility of this protocol for diverse substrates make it an efficient alternative to conventional methods.

Reaction Kinetics, Mechanisms and Catalysis 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 C26H41N5O7S, Safety of 3-Acetyldihydrofuran-2(3H)-one.

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

Bock, H. published the artcileHumoral and cellular immune responses to SARS CoV-2 vaccination in People with Multiple Sclerosis and NMOSD patients receiving immunomodulatory treatments, Application In Synthesis of 624-49-7, the publication is Multiple Sclerosis and Related Disorders (2022), 103554, database is CAplus and MEDLINE.

Vaccination against SARS CoV-2 results in excellent personal protection against a severe course of COVID-19. In People with Multiple Sclerosis (PwMS) vaccination efficacy may be reduced by immunomodulatory medications. To assess the vaccination induced cellular and humoral immune response in PwMS receiving disease modifying therapies. In a monocentric observational study on PwMS and patients with Neuromyelitis optica we quantified the cellular and humoral immune responses to SARS CoV-2. PwMS receiving glatiramer acetate, Interferon-ss, Dimethylfumarate, Cladribine or Natalizumab had intact humoral and cellular immune responses following vaccination against SARS CoV-2. B-cell depleting therapies reduced B-cell responses but did not affect T cell responses. Sphingosin-1-Phospate (S1P) inhibitors strongly reduced humoral and cellular immune responses. There was a good agreement between the Interferon gamma release assay and the T-SPOT assay used to measure viral antigen induced T-cell responses. This study demonstrates that S1P inhibitors impair the cellular and humoral immune response in SARS CoV-2 vaccination, whereas patients receiving B-cell depleting therapies mount an intact cellular immune response. These data can support clinicians in counselling their PwMS and NMOSD patients during the COVID 19 pandemic.

Multiple Sclerosis and Related Disorders 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 C6H8O4, Application In Synthesis of 624-49-7.

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

Shejul, Pravin B. published the artcileSynthesis of (Z)-2-alkylidene-4-oxo-thiazolidine derivatives under microwave irradiation, Recommanded Product: Ethyl 2-mercaptopropanoate, the publication is Asian Journal of Chemistry (2008), 20(7), 5427-5433, database is CAplus.

In comparison to conventional technique, exptl. evidence reveals the benefits of the microwave-promoted synthesis of functionalized 4-oxo-thiazolidine derivatives in terms of simple workup, efficiency and safe reproducibility.

Asian Journal of 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 C20H12N2O2, Recommanded Product: Ethyl 2-mercaptopropanoate.

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

Schwalbe, Thomas published the artcileSynthesis of a library of Ciprofloxacin analogues by means of sequential organic synthesis in microreactors, Name: Ethyl 3-(dimethylamino)acrylate, the publication is QSAR & Combinatorial Science (2005), 24(6), 758-768, database is CAplus.

The realm of combinatorial chem. is strongly based on the concept of parallel chem. and its ease of automation. Although this batch-type approach in general may be considered a success story, some limitations remain rarely addressable by conventional approaches. Particularly, scaling-up problems such as the resynthesis of multi-gram amounts of active compounds as well as the synthesis of building blocks and scaffolds in large amounts may prove to be problematic. The authors’ expertise in continuous chem. prompted them to develop a micro-reaction system for sequential organic synthesis that should overcome these limitations. In the present contribution a suitable system as well as its application to the first library approach towards (fluoro)quinolone antibiotics, such as Ciprofloxacin, solely using micro-reaction technol. is described. A known one-pot batch procedure for the synthesis of this compound class was split in its individual reaction steps, which were successfully adapted to a continuous conduct. After some optimization studies the overall sequence was suitable for chem. diversification. Particularly it was shown, that the first step of the synthesis – the acylation reaction of a β-dimethylamino acrylate with trifluoro-benzoic acid chloride – was accessible to synthesis of high quantities without any difficulties to yield a primary building block suitable for subsequent library synthesis. In a first diversification step, the Michael addition of a set of primary amines was followed by nucleophilic ring closure providing the difluoroquinolone system, which was subjected to a second diversification step by means of a nucleophilic aromatic substitution reaction. Thus, a number of Ciprofloxacin analogs could be synthesized in good overall yield and purity. Isolated yields ranged from 71 to 85% in the first diversification step and from 59 to 99% in the second step.

QSAR & Combinatorial Science 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 C12H13NO3, Name: Ethyl 3-(dimethylamino)acrylate.

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

Meng, Qi published the artcileQuantification and odor contribution of volatile thiols in Japanese soy sauce, Related Products of esters-buliding-blocks, the publication is Food Science and Technology Research (2012), 18(3), 429-436, database is CAplus.

Three compounds of volatile thiols, 2-furanmethanethiol (2FM) with a strong roast coffee aroma, benzenemethanethiol (BM) with a strong empyreumatic aroma reminiscent of smoke and Et 2-mercaptopropionate (ET2MP) with a tropical fruit-like aroma, were identified for the first time in four types of heat-treated soy sauce and raw soy sauce. 2FM, BM and ET2MP were present in these soy sauce samples at considerably higher concentrations than their perception thresholds. Their concentrations also increased when the raw soy sauce was heated for pasteurization. A triangle test on the raw soy sauce and heat-treated soy sauce showed that the aroma of the raw soy sauce became similar to that of the heat-treated soy sauce after the addition of the three volatile thiols to the raw soy sauce. The volatile thiols thus contributed to the aroma of heat-treated soy sauce.

Food Science and Technology Research 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, Related Products of esters-buliding-blocks.

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

Hero, Devid published the artcileFree- and reversible deactivation radical (co)polymerization of isobutylene in water under environmentally benign conditions, COA of Formula: C5H10O2S, the publication is European Polymer Journal (2021), 110336, database is CAplus.

The synthesis of a linear polyisobutylene is achieved for the first time by free radical polymerization The reaction was performed in environmentally friendly conditions, i.e., in an aqueous medium using cyclodextrin solubilizer, around room temperature This mild and straightforward radical polymerization resulted in a predominantly linear polymer with low dispersity. Isobutylene was also copolymerized with acrylamide via this cyclodextrin assisted aqueous free-radical polymerization, leading to new poly(isobutylene-co-acrylamide) amphiphilic copolymers. The feed composition of copolymerization had a huge effect on the composition and, therefore, the resulting copolymers solubility Reversible addition-fragmentation chain transfer radical polymerization (RAFT) of isobutylene was also carried out using a PEG-based sym. macro chain transfer agent. Poly(PEG-b-isobutylene-b-PEG) block-copolymer was formed in this one-pot reaction. This novel polymerization method for isobutylene opens new, environmentally benign routes to produce novel copolymers for various applications.

European Polymer Journal 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

Bossart, Jonas published the artcileReal-world disease-modifying therapy usage in persons with relapsing-remitting multiple sclerosis: Cross-sectional data from the Swiss Multiple Sclerosis Registry, Quality Control of 624-49-7, the publication is Multiple Sclerosis and Related Disorders (2022), 103706, database is CAplus and MEDLINE.

Several disease-modifying therapies (DMTs), covering a broad spectrum of mechanisms of action, have been approved by regulatory agencies for the treatment of relapsing-remitting multiple sclerosis (RRMS). However, only little is known about the current real-world treatment situation in Switzerland. Based on data from a diverse population of 668 persons with RRMS from the Swiss Multiple Sclerosis Registry (SMSR), the present study aims to fill this gap with a descriptive, cross-sectional approach. Data originated from the SMSR baseline questionnaire and follow-up surveys. Data on current health status and life situation in the last 6 mo were extracted from the survey distributed throughout 2020 and 2021, while data on disease-modifying therapy (DMT) histories were included from preceding surveys. Initially, data was stratified into three DMT groups according to the current DMT status (NO (No DMT), CONTINUED (DMT started more than 6 mo ago), and NEW (DMT started less than 6 mo ago)). In a subsequent anal., the sample was stratified into groups corresponding to the five most frequently prescribed DMTs. Self-reported outcomes including therapy discontinuation or interruption, relapses and side-effects in the last 6 mo were analyzed per group. Life and health situation parameters were also determined and analyzed. The study population consisted of 445 (66.6%) individuals belonging to the CONTINUED, 84 (12.6%) to the NEW, and 139 (20.8%) to the NO group. Within the NO group, 24 (17.3%) reported relapses. Furthermore, self-reported relapses (28 (33.3%)), side-effects (39 (46.4%)), and treatment discontinuations or interruptions (30 (35.7%)) occurred more frequently in the NEW compared to the CONTINUED group (37 (8.3%), 125 (28.1%), 8 (1.8%), resp.). The three groups also differed with respect to age, time since diagnosis, number of symptoms, DMT history, and health-related quality of life. The five most frequently prescribed DMTs included fingolimod (33.4%), di-Me fumarate (25.0%), ocrelizumab (23.6%), natalizumab (10.6%) and teriflunomide (7.5%). The frequency of self-reported relapses ranged from 9.7% to 13.6%. Notable differences were found in the number of self-reported side-effects, ranging from 9.1% with natalizumab to 56.7% with di-Me fumarate. This cross-sectional anal. suggested that the majority of individuals with RRMS in Switzerland continuously receive tolerable DMT. However, groups not receiving DMT or struggling with side-effects or continued disease worsening while on DMT still persist. It is conceivable that the number of self-reported symptoms indicates the need for more detailed clarification of the DMT characteristics and expectations of treatment outcomes. Injectable DMTs no longer play a major role in the treatment of RRMS in Switzerland and a trend toward an early use of potent drugs is emerging.

Multiple Sclerosis and Related Disorders 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 C6H8O4, Quality Control of 624-49-7.

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

Xu, Wengang published the artcileVisible-Light-Induced Selective Defluoroborylation of Polyfluoroarenes, gem-Difluoroalkenes, and Trifluoromethylalkenes, Formula: C5H10O2S, the publication is Angewandte Chemie, International Edition (2020), 59(10), 4009-4016, database is CAplus and MEDLINE.

Fluorinated organoboranes serve as versatile synthetic precursors for the preparation of value-added fluorinated organic compounds Recent progress has been mainly focused on the transition-metal catalyzed defluoroborylation. Herein, we report a photocatalytic defluoroborylation platform through direct B-H activation of N-heterocyclic carbene boranes, through the synergistic merger of a photoredox catalyst and a hydrogen atom transfer catalyst. This atom-economic and operationally simple protocol has enabled defluoroborylation of an extremely broad scope of multifluorinated substrates including polyfluoroarenes, gem-difluoroalkenes, and trifluoromethylalkenes in a highly selective fashion. Intriguingly, the defluoroborylation protocol can be transition-metal free, and the regioselectivity obtained is complementary to the reported transition-metal-catalysis in many cases.

Angewandte Chemie, International Edition 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 C4H10OS, Formula: C5H10O2S.

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