Tag: M.W=200-250

Mohan, Jag; Anjaneyulu, G. S. R.; Kiran published the artcile< Heterocyclic systems containing a bridge-head nitrogen atom: reactions of 2-aminothiadiazoles with α-haloketones and ketones in the presence of NBS>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is antimicrobial diarylimidazothiadiazole bromo; imidazothiadiazole diaryl bromo preparation antimicrobial.

Diarylimidazo[2,1-b]-1,3,4-thiadiazoles I (R = Cl, R1 = H, Br, Me, Ph, Cl; R = Me, R1 = Cl, Ph) are prepared by the reaction of α-haloketones with 2-aminothiadiazoles II, or more conveniently, by treating II directly with ketones in the presence of NBS. Bromination of I (R = R1 = Cl) furnishes a 5-bromo-2,6-diarylimidazo[2,1-b]thiadiazole derivative The antimicrobial activity of I (R = R1 = Cl) and a derivative has been evaluated; they were found to be inactive.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about 70057-67-9. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine.

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

Plashkina, N. A.; Troitskaya, V. I.; Pushkareva, Z. V.; Ryapasova, T. P. published the artcile< Studies on riboflavine analogs. VIII. 7-(Trifluoromethyl)-8-chloroisoalloxazines>, Synthetic Route of 35375-74-7, the main research area is isoalloxazine chlorotrifluoromethyl; cyclocondensation alloxan ribityltoluidine; galactyltoluidine cyclocondensation; sorbityltoluidine cyclocondensation; rhamnityltoluidine cyclocondensation.

Chlorotoluidines I (R = H, Me, CH2CH2OH, ribityl, galactyl, sorbityl, rhamnityl), prepared in 72-95% yields by amination of the corresponding dichlorotoluene with RNH2, were reduced by Raney Ni and cyclized with alloxan to give 63-85% isoalloxazines II.

Khimiya Geterotsiklicheskikh Soedinenii published new progress about Condensation reaction. 35375-74-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3N2O2, Synthetic Route of 35375-74-7.

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

Luzina, Elena L.; Popov, Anatoliy V. published the artcile< Synthesis of 1-aroyl(1-arylsulfonyl)-4-bis(trifluoromethyl)alkyl semicarbazides as potential physiologically active compounds>, Name: 4-(Difluoromethoxy)benzene-1-sulfonyl chloride, the main research area is preparation semicarbazide physiol active compound Lipinski Gelovani parameter.

1,1-Bis(trifluoromethyl)alkyl isocyanates obtained from perfluoroisobutene (PFIB) react with aroyl(arylsulfonyl)hydrazines. Twenty eight prospective biol. active polyfluorinated 1,4-substituted semicarbazides, e.g. I, were synthesized. The structure of each new product was confirmed by anal. and spectroscopic methods. The Lipinski’s and Gelovani’s parameters were then calculated Two adjustments to the Lipinski rules of five are suggested for fluorinated drug candidates.

Journal of Fluorine Chemistry published new progress about Semicarbazides Role: SPN (Synthetic Preparation), PREP (Preparation). 351003-34-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H5ClF2O3S, Name: 4-(Difluoromethoxy)benzene-1-sulfonyl chloride.

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

Yu, Yu; Ran, Dongzhi; Jiang, Junhao; Pan, Tao; Dan, Yanrong; Tang, Qiang; Li, Wei; Zhang, Lin; Gan, LinLing; Gan, Zongjie published the artcile< Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2>, Electric Literature of 2382-10-7, the main research area is purin derivative preparation anticancer HDAC CDK dual inhibitor; Antitumor; CDKs; Dual inhibitors; HDACs; Purin.

HDAC and CDK inhibitors have been demonstrated to be synergistically in suppressing cancer cell proliferation and inducing apoptosis. In this work, we incorporated the pharmacophore groups of HDACs and CDKs inhibitors into one mol. to design and synthesize a series of purin derivatives as HDAC/CDK dual inhibitors. The lead compound I, showing good HDAC1 and CDK2 inhibitory activity with IC50 values of 5.8 and 56 nM, resp., exhibited attractive potency against several cancer cell lines in vitro. This work may lead to the discovery of a novel scaffold and potential dual HDAC/CDK inhibitors.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Electric Literature of 2382-10-7.

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

El Abbouchi, Abdelmoula; El Brahmi, Nabil; Hiebel, Marie-Aude; Bignon, Jerome; Guillaumet, Gerald; Suzenet, Franck; El Kazzouli, Said published the artcile< Synthesis and biological evaluation of ethacrynic acid derivatives bearing sulfonamides as potent anti-cancer agents>, Application In Synthesis of 22952-32-5, the main research area is ethacrynic acid sulfonamide preparation anticancer human safety; Anti-cancer; Anti-proliferative; Cancer cells; Ethacrynic acid; Safety ratios; Sulfonamides.

A series of ethacrynic acid (2-[2,3-dichloro-4-(2-methylidenebutanoyl)phenoxy]acetic acid) (EA, Edecrin) containing sulfonamides linked via three types of linkers namely 1,2-ethylenediamine, piperazine and 4-aminopiperidine was synthesized and subsequently evaluated in vitro against HL60 and HCT116 cancer cell lines. All the EA analogs, excluding two derivs, showed anti-proliferative activity with IC50s in the micromolar range (less than 4 uM). Three derivatives I-III were selected for their interesting dual activity on HL60 cell line in order to be further evaluated against a panel of cancer cell lines (HCT116, A549, MCF7, PC3, U87-MG and SKOV3) as well as on MRC5 as a normal cell line. These compounds displayed IC50 values in nanomolar range against A549, MCF7, PC3 and HCT116 cell lines, deducing the discovery that piperazine or 4-aminopiperidine is the linker’s best choice to develop EA analogs with highly potent anti-proliferative activities own up to 24 nM. Besides, in terms of selectivity, those linkers are more suitable offering safety ratios of up to 63.8.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Application In Synthesis of 22952-32-5.

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

Tian, Maoqun; Abdelrahman, Aliaa; Baqi, Younis; Fuentes, Eduardo; Azazna, Djamil; Spanier, Claudia; Densborn, Sabrina; Hinz, Sonja; Schmid, Ralf; Mueller, Christa E. published the artcile< Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists>, Name: 5-Chloro-2-methoxybenzenesulfonyl chloride, the main research area is inflammation P2X1 receptor calcium influx allosteric modulators antagonists.

Antagonists for the ATP-gated ion channel receptor P2X1 have potential as antithrombotics and for treating hyperactive bladder and inflammation. In this study, salicylanilide derivatives were synthesized based on a screening hit. P2X1 antagonistic potency was assessed in 1321N1 astrocytoma cells stably transfected with the human P2X1 receptor by measuring inhibition of the ATP-induced calcium influx. Structure-activity relationships were analyzed, and selectivity vs. other P2X receptor subtypes was assessed. The most potent compounds, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide (1, IC50 0.0192 μM)(I) and N-[3,5-bis(trifluoromethyl)phenyl]-4-chloro-2-hydroxybenzamide (14, IC50 0.0231 μM)(II), displayed >500-fold selectivity vs. P2X2 and P2X3, and 10-fold selectivity vs. P2X4 and P2X7 receptors, and inhibited collagen-induced platelet aggregation. They behaved as neg. allosteric modulators, and mol. modeling studies suggested an extracellular binding site. Besides selective P2X1 antagonists, compounds with ancillary P2X4 and/or P2X7 receptor inhibition were discovered. These compounds represent the first potent, non-acidic, allosteric P2X1 receptor antagonists reported to date.

Journal of Medicinal Chemistry published new progress about Asthma. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Name: 5-Chloro-2-methoxybenzenesulfonyl chloride.

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

Ajenjo, Javier; Klepetarova, Blanka; Greenhall, Martin; Bim, Daniel; Culka, Martin; Rulisek, Lubomir; Beier, Petr published the artcile< Preparation of (Pentafluorosulfanyl)benzenes by Direct Fluorination of Diaryldisulfides: Synthetic Approach and Mechanistic Aspects>, Recommanded Product: 5-Chloro-2-methoxybenzenesulfonyl chloride, the main research area is pentafluorosulfanyl benzene preparation reaction mechanism radical; fluorine; pentafluorosulfanyl; radical reactions; reaction mechanisms; synthetic methods.

Direct fluorination of ortho-, meta- and para-substituted aromatic thiols and disulfides using elemental fluorine afforded substituted (pentafluorosulfanyl)benzenes ArSF5 [Ar = 4-FC6H4, 2-NCC6H4, 4-HOOCC6H4, etc.]. This work thus represented the first study of the scope and limitation of direct fluorination for the synthesis of new SF5-containing building blocks. Fluorinations in batch and flow modes were compared. A comprehensive computational study was carried out employing d. functional and wave function methods to elucidate the reaction mechanism of the transformation of ArSF3 into ArSF5. Eliminating various nonradical pathways, it was shown that the reaction proceeded by a radical mechanism, initiated by the attack of the F. on the ArSF3 moiety, propagated via an almost barrierless F2+ArSF4.→ArSF5+F. step and terminated by the ArSF4.+F.→ArSF5. Most of the calculated data were in very good agreement with exptl. observations concerning the ortho-substituent effect on the reaction rates and yields.

Chemistry – A European Journal published new progress about Aromatic compounds Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation) ((pentafluorosulfanyl)benzenes). 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Recommanded Product: 5-Chloro-2-methoxybenzenesulfonyl chloride.

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

Ghaffari, Samaneh; Esmaeili, Abbas Ali; Khojastehnezhad, Amir published the artcile< One-pot Three-component Synthesis of Novel 1,3,4-Thiadiazole-thiazolo[3,2-a]pyrimidine Derivatives Catalyzed by Molecular Iodine>, Category: chlorides-buliding-blocks, the main research area is thiadiazole thiazolopyrimidine preparation; amino phenyl thiadiazole dihydrothiazolopyrimidine aryl aldehyde three component reaction.

A new and efficient approach has been reported for the synthesis of novel [1,3,4]thiadiazol-thiazolo[3,2-a]pyrimidines, using the one-pot three-component reaction of 2-amino-5-phenyl[1,3,4]thiadiazoles with 2,3-dihydrothiazolo[3,2-a]pyrimidine and aromatic aldehydes. This was done in the presence of mol. iodine in refluxing acetonitrile.

Organic Preparations and Procedures International published new progress about Benzaldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Category: chlorides-buliding-blocks.

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

Gable, Jonathan E.; Lee, Gregory M.; Acker, Timothy M.; Hulce, Kaitlin R.; Gonzalez, Eric R.; Schweigler, Patrick; Melkko, Samu; Farady, Christopher J.; Craik, Charles S. published the artcile< Fragment-Based Protein-Protein Interaction Antagonists of a Viral Dimeric Protease>, HPLC of Formula: 35375-74-7, the main research area is fragment based screening inhibitor binding dimer interface KSHV protease; NMR spectroscopy; dimer disruption; fragment-based screening; human herpesviruses; proteases.

Fragment-based drug discovery has shown promise as an approach for challenging targets such as protein-protein interfaces. We developed and applied an activity-based fragment screen against dimeric Kaposi’s sarcoma-associated herpesvirus protease (KSHV Pr) using an optimized fluorogenic substrate. Dose-response determination was performed as a confirmation screen, and NMR spectroscopy was used to map fragment inhibitor binding to KSHV Pr. Kinetic assays demonstrated that several initial hits also inhibit human cytomegalovirus protease (HCMV Pr). Binding of these hits to HCMV Pr was also confirmed by NMR spectroscopy. Despite the use of a target-agnostic fragment library, more than 80 % of confirmed hits disrupted dimerization and bound to a previously reported pocket at the dimer interface of KSHV Pr, not to the active site. One class of fragments, an aminothiazole scaffold, was further explored using com. available analogs. These compounds demonstrated greater than 100-fold improvement of inhibition. This study illustrates the power of fragment-based screening for these challenging enzymic targets and provides an example of the potential druggability of pockets at protein-protein interfaces.

ChemMedChem published new progress about Enzyme functional sites, inhibitor-binding. 35375-74-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3N2O2, HPLC of Formula: 35375-74-7.

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

Rafique, Rafaila; Khan, Khalid Mohammed; Arshia; Chigurupati, Sridevi; Wadood, Abdul; Rehman, Ashfaq Ur; Salar, Uzma; Venugopal, Vijayan; Shamim, Shahbaz; Taha, Muhammad; Perveen, Shahnaz published the artcile< Synthesis, in-vitro α-amylase inhibitory, and radicals (DPPH & ABTS) scavenging potentials of new N-sulfonohydrazide substituted indazoles>, Application In Synthesis of 22952-32-5, the main research area is phenyl tetrahydroindazolone preparation; tetrahydroindazolylidene sulfonohydrazide diastereoselective preparation; amylase inhibition kinetics antioxidant activity SAR docking; ABTS and DPPH; In silico; In vitro; Indazole; Sulfonohydrazide; α-amylase enzyme.

A series of new N-sulfonohydrazide substituted indazoles I and II [R = Me, Ph, 1-naphthyl, etc.] were synthesized by multistep reaction scheme and assessed for in-vitro α-amylase inhibitory and radical (DPPH and ABTS) scavenging properties. All compounds I and II were fully characterized by different spectroscopic techniques including 1H, 13C NMR, EI-MS, HREI-MS, ESI-MS and HRESI-MS. Compounds I and II showed promising α-amylase inhibitory activities (IC50 = 1.23 ± 0.06-4.5 ± 0.03μM) as compared to the standard acarbose (IC50 1.20 ± 0.09μM). In addition to that all derivatives were found good to moderate scavengers of DPPH (IC50 = 2.01 ± 0.13-5.3 ± 0.11) and ABTS (IC50 = 2.34 ± 0.07-5.5 ± 0.07μM) radicals, in comparison with standard ascorbic acid having scavenging activities with IC50 = 1.99 ± 0.09μM and IC50 = 2.03 ± 0.11μM for DPPH and ABTS radicals. In-silico mol. docking study was conducted to rationalized the binding interaction of α-amylase enzyme with ligands. Compounds were observed as mixed type inhibitors in enzyme kinetic characterization.

Bioorganic Chemistry published new progress about Antioxidants. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Application In Synthesis of 22952-32-5.

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