Tag: M.W=200-250

Alam, Faruk published the artcile< A study on the antimicrobial and antioxidant activities of some new 1, 3, 4-thiadiazole derivatives>, Application In Synthesis of 70057-67-9, the main research area is thiadiazole derivative antioxidant antimicrobial agent.

The various derivatives of thiadiazole were prepared by the reaction of m-chlorophenyl isocyanate and p-chlorophenyl isocyanate with 5-(substituted phenyl) -2-amino-1, 3, 4-thiadiazole in dry acetonitrile. Elemental anal., IR, 1H NMR, mass spectral data confirmed the structure of the newly synthesized compounds All the derivatives of these moieties were evaluated for invitro antimicrobial and invitro antioxidant activity. Most of the synthesized compounds showed potent antimicrobial activity at 100 and 50 μg/mL and antioxidant scavenging activity. Compounds showed most significant antibacterial activity against gram pos. test organism S.aureus and most significant antifungal activity against test organisms Aspergillus niger and Candida albicans. All the compounds were screened for in vitro antioxidant activity by various methods as Scavenging of DPPH, Scavenging of nitric oxide radical inhibitory activity.

International Journal of ChemTech Research published new progress about Antimicrobial agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Application In Synthesis of 70057-67-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Rojas-Prats, Elisa; Martinez-Gonzalez, Loreto; Gonzalo-Consuegra, Claudia; Liachko, Nicole F.; Perez, Concepcion; Ramirez, David; Kraemer, Brian C.; Martin-Requero, Angeles; Perez, Daniel I.; Gil, Carmen; de Lago, Eva; Martinez, Ana published the artcile< Targeting nuclear protein TDP-43 by cell division cycle kinase 7 inhibitors: A new therapeutic approach for amyotrophic lateral sclerosis>, Synthetic Route of 16799-05-6, the main research area is cdc7 inhibitor TDP43 ALS FTLD drug discovery; ALS; CDC7 inhibitors; Drug discovery; FTLD; TDP-43.

Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease with no known cure. Aggregates of the nuclear protein TDP-43 have been recognized as a hallmark of proteinopathy in both familial and sporadic cases of ALS. Post-translational modifications of this protein, include hyperphosphorylation, cause disruption of TDP-43 homeostasis and as a consequence, promotion of its neurotoxicity. Among the kinases involved in these changes, cell division cycle kinase 7 (CDC7) plays an important role by directly phosphorylating TDP-43. In the present manuscript the discovery, synthesis, and optimization of a new family of selective and ATP-competitive CDC7 inhibitors based on 6-mercaptopurine scaffold are described. Moreover, we demonstrate the ability of these inhibitors to reduce TDP-43 phosphorylation in both cell cultures and transgenic animal models such as C. elegans and Prp-hTDP43 (A315T) mice. Altogether, the compounds described here may be useful as versatile tools to explore the role of CDC7 in TDP-43 phosphorylation and also as new drug candidates for the future development of ALS therapies.

European Journal of Medicinal Chemistry published new progress about Amyotrophic lateral sclerosis. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Synthetic Route of 16799-05-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Oxoby, Mayalen; Moreau, Francois; Durant, Lionel; Denis, Alexis; Genevard, Jean-Marie; Vongsouthi, Vanida; Escaich, Sonia; Gerusz, Vincent published the artcile< Towards Gram-positive antivirulence drugs: New inhibitors of Streptococcus agalactiae Stk1>, Recommanded Product: 2,6-Dichloro-9-methyl-9H-purine, the main research area is preparation structure antibacterial antivirulence inhibitor Streptococcus agalactiae Stk1.

A structure-activity relationship study from a screening hit and structure-based design strategy has led to the identification of bisarylureas as potent inhibitors of Streptococcus agalactiae Stk1. As this target has been directly linked to bacterial virulence, these inhibitors can be considered as a promising step towards antivirulence drugs.

Bioorganic & Medicinal Chemistry Letters published new progress about Antibacterial agents. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Recommanded Product: 2,6-Dichloro-9-methyl-9H-purine.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Wang, Qian; Mgimpatsang, Kumchok C.; Konstantinidou, Markella; Shishkina, Svitlana V.; Doemling, Alexander published the artcile< 1,3,4-Oxadiazoles by Ugi-Tetrazole and Huisgen Reaction>, Product Details of C8H4ClF3O2, the main research area is oxadiazole aminoalkyl metal free multicomponent preparation; Ugi reaction amine aldehyde azidotrimethylsilane isonitrile; Huisgen reaction aminoalkyl tetrazole acyl chloride pyridine solvent.

Amines, aldehydes, Me3SiN3, and tert-octyl isonitrile t-BuCH2CMe2N+C- underwent Ugi reactions to yield aminoalkyltetrazoles such as I; acid cleavage of the tert-octyl group followed by Huisgen reactions with acyl chlorides in pyridine yielded oxadiazoles such as II.

Organic Letters published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Product Details of C8H4ClF3O2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jakovljevic, Katarina; Joksovic, Milan D.; Botta, Bruno; Jovanovic, Ljiljana S.; Avdovic, Edina; Markovic, Zoran; Mihailovic, Vladimir; Andric, Marijana; Trifunovic, Snezana; Markovic, Violeta published the artcile< Novel 1,3,4-thiadiazole conjugates derived from protocatechuic acid: synthesis, antioxidant activity, and computational and electrochemical studies>, SDS of cas: 70057-67-9, the main research area is thiadiazole amide preparation antioxidant DFT electrochem.

A series of novel 1,3,4-thiadiazole amide derivatives I [R = cyclohexyl, Ph, Bn, etc.] containing a protocatechuic acid moiety were synthesized and structurally characterized. In addition, the corresponding imino and amino analogs of a 1,3,4-thiadiazole amide derivative I [R = Ph] were prepared to compare the effects of the structural changes on the radical-scavenging activity. The obtained compounds I were examined for their antioxidative potential by DPPH and ABTS assays. In addition, selected compounds were studied by d. functional theory (DFT) and cyclic voltammetry experiments The tested compounds showed high potential to scavenging DPPH radical and ABTS radical cation compared with the referent antioxidants ascorbic acid and nordihydroguaiaretic acid (NDGA). On the basis of the calculated thermodn. parameters, it can be concluded that the sequential proton loss electron transfer (SPLET) mechanism represented the most probable reaction path in a polar solvent for DPPH radical-scavenging activity. On the other hand, the single electron transfer followed by proton transfer (SET-PT) could be a likely mechanistic pathway in the case of an ABTS radical cation.

Comptes Rendus Chimie published new progress about Amides Role: PAC (Pharmacological Activity), PRP (Properties), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, SDS of cas: 70057-67-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Canale, Vittorio; Kotanska, Magdalena; Dziubina, Anna; Stefaniak, Matylda; Siwek, Agata; Starowicz, Gabriela; Marciniec, Krzysztof; Kasza, Patryk; Satala, Grzegorz; Duszynska, Beata; Bantreil, Xavier; Lamaty, Frederic; Bednarski, Marek; Sapa, Jacek; Zajdel, Pawel published the artcile< Design, Sustainable Synthesis and Biological Evaluation of a Novel Dual α2A/5-HT7 Receptor Antagonist with Antidepressant-Like Properties>, Synthetic Route of 22952-32-5, the main research area is dihydrobenzofuranoxy ethyl piperidine preparation antidepressant activity green chem SAR; 5-HT7 receptor antagonist; depression; forced swim test; medicinal mechanochemistry; α2 adrenoceptor antagonist.

The complex pathophysiol. of depression, together with the limits of currently available antidepressants, has resulted in the continuous quest for alternative therapeutic strategies. Numerous findings suggest that pharmacol. blockade ofα2-adrenoceptor might be beneficial for the treatment of depressive symptoms by increasing both norepinephrine and serotonin levels in certain brain areas. The antidepressant properties of 5-HT7 receptor antagonists have been widely demonstrated in a large set of animal models. Considering the potential therapeutic advantages in targeting both α2-adrenoceptors and 5-HT7 receptors, a small series of arylsulfonamide derivatives of (dihydrobenzofuranoxy)ethyl piperidines I (Ar = 4-fluorophenyl, naphthalen-1-yl, isoquinolin-4-yl, etc.; m = 0,1) as dually active ligands were designed. Following green chem. principles, the designed compounds were synthesized entirely using a sustainable mechanochem. approach. The identified compound I (Ar = 5-chloro-2-fluorophenyl (II)) behaved as a potent α2A/5-HT7 receptor antagonist and displayed moderate-to-high selectivity over α1-adrenoceptor subtypes and selected serotonin and dopaminergic receptors. Finally, (II) improved performance of mice in the forced swim test, displaying similar potency to the reference drug mirtazapine.

Molecules published new progress about 5-HT antagonists. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Synthetic Route of 22952-32-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Peng, Long; Li, Yuqiang; Li, Yangyang; Wang, Wang; Pang, Hailiang; Yin, Guoyin published the artcile< Ligand-Controlled Nickel-Catalyzed Reductive Relay Cross-Coupling of Alkyl Bromides and Aryl Bromides>, Recommanded Product: 3-Chlorophenethyl Bromide, the main research area is regioselective synthesis arylalkane; ligand controlled nickel catalyzed reductive relay cross coupling; alkyl bromide reductive relay cross coupling aryl bromide.

1,1-Diarylalkanes are important structural frameworks which are widespread in biol. active mols. Herein, we report a reductive relay cross-coupling of alkyl bromides with aryl bromides by nickel catalysis with a simple nitrogen-containing ligand. This method selectively affords 1,1-diarylalkane derivatives with good to excellent yields and regioselectivity.

ACS Catalysis published new progress about Alkylarenes Role: SPN (Synthetic Preparation), PREP (Preparation) (1,1-diarylalkanes). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Recommanded Product: 3-Chlorophenethyl Bromide.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zhang, Yang-Ming; Gu, Min; Ma, Hui; Tang, Jie; Lu, Wei; Nan, Fa-Jun published the artcile< An efficient synthesis of 2-chloropyrimidines via Pd-catalyzed regioselective dechlorination of 2,4-dichloropyrimidines in the presence of NaHCO3>, Name: 2,6-Dichloro-9-methyl-9H-purine, the main research area is chloropyrimidine regioselective dechlorination palladium catalyst sodium hydrocarbonate; pyrimidine chloro preparation.

An efficient synthesis of 2-chloropyrimidines from readily accessible 2,4-dichloropyrimidines was achieved via Pd-catalyzed regioselective dechlorination in the presence NaHCO3.

Chinese Journal of Chemistry published new progress about Dechlorination (regioselective). 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Name: 2,6-Dichloro-9-methyl-9H-purine.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Blaser, Adrian; Palmer, Brian D.; Sutherland, Hamish S.; Kmentova, Iveta; Franzblau, Scott G.; Wan, Baojie; Wang, Yuehong; Ma, Zhenkun; Thompson, Andrew M.; Denny, William A. published the artcile< Structure-Activity Relationships for Amide-, Carbamate-, And Urea-Linked Analogues of the Tuberculosis Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)>, Name: 2-(Trifluoromethoxy)benzoyl chloride, the main research area is structure activity relationship Mycobacterium tuberculosis infection drug imidazooxazine preparation; PA 824 analog preparation SAR tuberculosis infection drug.

Analogs of clin. tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824, I), in which the OCH2 linkage was replaced with amide, carbamate, and urea functionality, were investigated as an alternative approach to address oxidative metabolism, reduce lipophilicity, and improve aqueous solubility Several soluble monoaryl examples displayed moderately improved (∼2- to 4-fold) potencies against replicating Mycobacterium tuberculosis but were generally inferior inhibitors under anaerobic (nonreplicating) conditions. More lipophilic biaryl derivatives mostly displayed similar or reduced potencies to these in contrast to the parent biaryl series. The leading biaryl carbamate demonstrated exceptional metabolic stability and a 5-fold better efficacy than the parent drug in a mouse model of acute M. tuberculosis infection but was poorly soluble Bioisosteric replacement of this biaryl moiety by arylpiperazine resulted in a soluble, orally bioavailable carbamate analog providing identical activity in the acute model, comparable efficacy to OPC-67683 in a chronic infection model, favorable pharmacokinetic profiles across several species, and enhanced safety.

Journal of Medicinal Chemistry published new progress about Homo sapiens. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Name: 2-(Trifluoromethoxy)benzoyl chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Mete, Antonio; Bowers, Keith; Chevalier, Eric; Donald, David K.; Edwards, Helen; Escott, Katherine J.; Ford, Rhonan; Grime, Ken; Millichip, Ian; Teobald, Barry; Russell, Vince published the artcile< The discovery of AZD9164, a novel muscarinic M3 antagonist>, Application of C8H8BrCl, the main research area is muscarinic M3 antagonist preparation AZD9164 COPD.

The optimization of a new series of muscarinic M3 antagonists is described, leading to the identification of AZD9164 which was progressed into the clinic for evaluation of its potential as a treatment for COPD.

Bioorganic & Medicinal Chemistry Letters published new progress about Chronic obstructive pulmonary disease. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Application of C8H8BrCl.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics