Tag: M.W=200-250

Hilfiker, Mark A. published the artcileDiscovery of novel aminothiadiazole amides as selective EP3 receptor antagonists, Application In Synthesis of 89978-31-4, the main research area is aminothiadiazole amide preparation antagonist EP3 receptor.

This Letter discloses a series of 2-aminothiadiazole amides as selective EP3 receptor antagonists. Structure-activity relationship (SAR) optimization resulted in compounds with excellent functional activity in vitro. In addition, efforts to optimize DMPK properties in the rat are discussed. These efforts have resulted in the identification of potent, selective EP3 receptor antagonists with excellent DMPK properties suitable for in vivo studies.

Bioorganic & Medicinal Chemistry Letters published new progress about Drug bioavailability. 89978-31-4 belongs to class chlorides-buliding-blocks, name is 5-(2,6-Dichlorophenyl)-1,3,4-thiadiazol-2-amine, and the molecular formula is C8H5Cl2N3S, Application In Synthesis of 89978-31-4.

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

Alp, Mehmet published the artcileSynthesis and antiparasitic and antifungal evaluation of 2′-arylsubstituted-1H,1’H-[2,5′]bisbenzimidazolyl-5-carboxamidines, Name: 4-(4-Chlorophenoxy)benzaldehyde, the main research area is phenylenediamine benzimidazolyl condensation aldehyde aryl; benzimidazole bis aryl amidino preparation antiparasitic antifungal activity.

A series of 2′-aryl-1H,1’H-[2,5′]-bisbenzimidazolyl-5-carboxamidines I (e.g., R1R2 = benzo, R3 = R4 = H) were prepared in a six-step process starting from 4-amino-3-nitrobenzonitrile. The antiparasitic activity against Trypanosoma brucei rhodesiense (T.b.r.), Plasmodium falciparum (P.f.), Leishmania donovani (L.d.) and Trypanosoma cruzi (T.c.) and antifungal activity against Candida albicans and Candida krusei were evaluated in vitro. Several compounds showed promising in vitro activity against T.b.r., P.f. and C. albicans and had superior activity against P.f. as compared to chloroquine.

European Journal of Medicinal Chemistry published new progress about Aromatic diamines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Name: 4-(4-Chlorophenoxy)benzaldehyde.

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

Senkardes, Sevil published the artcileSynthesis, antimicrobial properties and in silico studies of aryloxyacetic acid derivatives with hydrazone or thiazolidine-4-one scaffold, Application In Synthesis of 93118-03-7, the main research area is arylideneamino phenoxyacetamide preparation antibacterial antifungal SAR docking; arylthiazolidinyl phenoxyacetamide preparation antibacterial antifungal SAR docking; 4-thiazolidinone; Cresol; antimicrobial activity; hydrazone; molecular docking.

In this work, twenty hydrazide-hydrazones I [Ar = 3,5-dimethylphenyl, 2-chloro-3-methoxyphenyl, 4-phenylthiophen-2-yl, etc.] and 4-thiazolidinone derivatives II were synthesized starting from m-cresol. Antimicrobial evaluation was carried out by microdilution method against Enterococcus faecalis and Staphylococcus aureus as Gram-pos. bacteria and Escherichia coli and Pseudomonas aeruginosa as Gram-neg. bacteria, and three pathogenic fungi Candida albicans, Candida parapsilosis and Candida krusei. Some compounds possessed considerable antimicrobial properties against the tested microorganisms, particularly against E. coli. Compounds II [Ar = 3-methoxyphenyl, 3,5-dichlorophenyl] were found to be the most active derivatives with MICs of 2 μg/mL against E. coli and compounds I [Ar = 3,5-dichlorophenyl] also displayed antifungal activity against Candida krusei that was comparable to fluconazole. Calculated drug-likeness and ADMET parameters of the most active compounds confirmed their potential as antimicrobial drug candidates. Mol. docking investigations were carried out in the thiamine diphosphate-binding site of pyruvate dehydrogenase multienzyme complex E1 component (PDHc-E1) to clarify the potential antibacterial mechanism against E. coli. The results showed the potential and importance of developing new hydrazones and 4-thiazolidinones that would be effective against microbial strains.

Journal of Biomolecular Structure and Dynamics published new progress about Antibacterial agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Application In Synthesis of 93118-03-7.

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

Yang, Peng-Yu published the artcileSolid-Phase Synthesis of Azidomethylene Inhibitors Targeting Cysteine Proteases, COA of Formula: C7H6ClFO2S, the main research area is azidomethylene library solid phase preparation inhibitor cysteine protease caspase.

An efficient strategy for the solid-phase synthesis of azidomethylene inhibitors targeting cysteine proteases is described. The method is highlighted by its compatibility with readily available building blocks, as well as its ability to accommodate different functional groups. A 249-member library has thus far been successfully synthesized, characterized, and screened against caspase-1, -3 and -7.

Organic Letters published new progress about Enzyme inhibitors. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, COA of Formula: C7H6ClFO2S.

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

Keith, John M. published the artcileHeteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase, Computed Properties of 61343-99-5, the main research area is heteroaryl urea fused bicyclic diamine core preparation; fatty acid amide hydrolase inhibitory activity; Anandamide; Aryl urea; Covalent inhibitor; Endocannabinoid; Enzyme; FAAH; Inhibitors; Serine hydrolase.

A series of mechanism-based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Several compounds I and II equipotent against both species were identified and profiled in vivo.

Bioorganic & Medicinal Chemistry Letters published new progress about Enzyme inhibitors (fatty acid amide hydrolase). 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Computed Properties of 61343-99-5.

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

Gajera, Nilesh N. published the artcileSynthesis, characterization and biological screening of new spirochromanones, Safety of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is spirochromanone leucine benzenesulfonamide preparation antibacterial antifungal.

New spirochromanones I (R = substituted phenyl) based on N-[1-(6-bromo-4-oxo-3,4-dihydro-1’H-spiro[chromene-2,4′-piperidin]-1′-yl)-3-methyl-1-oxobutan-2-yl]benzenesulfonamides were synthesized by series of reactions, such as cyclization, deprotection, coupling, and condensation. The compounds were tested for their activity against fungi and pathogenic strains of bacteria. The compounds bearing F, cyano, and OCF3 groups at para position showed competitive antifungal activity, while the compounds carrying either a halo or Me substituent at ortho position showed significant antibacterial activity.

Journal of Chemical and Pharmaceutical Research published new progress about Antibacterial agents. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Safety of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

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

Nie, Li Fei published the artcileDesign, synthesis, and toward a side-ring optimization of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones and their effect on melanin synthesis in murine B16 cells, Product Details of C7H6ClFO2S, the main research area is oxo tetrahydro pyrrolothienopyrimidinyl benzenesulfonamide preparation melanin synthesis activity; methyl oxo hexahydro thienopyrimidoazepinyl benzenesulfonamide preparation melanin synthesis activity.

The synthesis of 48 novel 3-sulfonylamides containing a tricyclic thieno[2,3-d]pyrimidin-4(3H)-one moiety, I [R1 = H, 3-F, 3-NO2, etc.; R2 = H, 4-Me, 5-Cl, etc.; n = 1,3], and their influence on melanin synthesis in murine B16 cells. All target sulfonylamides I were synthesized through key intermediate 3-nitro-thieno[2,3-d]pyrimidin-4(3H)-ones using three types of ipso-nitration reactions. In this case, the pyrido[1,2-a]- fragment of the thieno[2,3-d]pyrimidine moiety was converted to pyrrolo[1,2-a]- and azepino[1,2-a]- side-rings in order to evaluate the bioactivities of the synthesized derivatives for a structure activity-relationships point of view. The obtained results suggested that some of the selected compounds revealed a promising influence on melanin synthesis in murine B16 cells and may serve as lead compounds for further drug discovery and development.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Arenesulfonyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Product Details of C7H6ClFO2S.

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

Nie, Li Fei published the artcileSynthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells, Quality Control of 7079-48-3, the main research area is thienopyrimidinone benzenesulfonamide preparation melanin synthesis activity.

A series of novel sulfonamide derivatives containing tricyclic thieno[2,3-d]pyrimidinones I (R = Ph, 4-FC6H4, 2-F3CC6H4, 3,5-Cl2C6H3, etc.) was synthesized and evaluated for melanin synthesis in murine B16 cells. All new compounds were characterized by 1H NMR, 13C NMR, IR and HRMS. Among them, 6 compounds demonstrated excellent activity than pos. control (8-methoxylpsoralen, 8-MOP) with more than 1.5-fold potency. Compound I (R = 3,5-Cl2C6H3) was the most potent one (658.3 ± 8.7%), exhibiting 5.0-fold stronger activity than 8-MOP (130.9 ± 8.6%). The compound I (R = 3,5-F2C6H3) increased melanin synthesis in murine B16 cells with a 4.35-fold potency as compared to 8-MOP. These compounds may serve as lead compounds for further drug discoveries for the treatment of vitiligo.

Research on Chemical Intermediates published new progress about Arenesulfonyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Quality Control of 7079-48-3.

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

Liu, Zong-ying published the artcileSynthesis and evaluation of 1-(benzo[b]thiophen-2-yl)ethanone analogues as novel anti-osteoporosis agents acting on BMP-2 promotor, Quality Control of 93118-03-7, the main research area is benzothiophenyl ethanone derivative preparation BMP2 promotor antiosteoporosis agent.

A novel series of 1-(benzo[b]thiophen-2-yl)ethanone analogs were prepared and evaluated for enhancing BMP-2 expression. Some compounds exhibited potent effect for enhancing BMP-2 expression. Compounds I and II produced a dose-dependent increase on bone histol. and histomorphometry, and effectively reduced bone defects induced by ovariectomy in an ovariectomized rat model (OVX).

Bioorganic & Medicinal Chemistry Letters published new progress about Antiosteoporotic agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Quality Control of 93118-03-7.

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

Andres, Miriam published the artcile2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists, Application of Ethyl 2,5-dichlorobenzoate, the main research area is pyrazolylacetate preparation chemoattractant receptor antagonist; CRTh2 antagonists; Pyrazole; Structure–activity relationship (SAR).

In this manuscript, the synthesis and biol. activity of a series of pyrazole acetic acids, e.g. I [R1 = H, 4-MeO, 5-F, etc.; R2 = Ph, 2-FC6H4, 3-ClC6H4; X= SO2, S] as CRTh2 antagonists is presented. Biol. evaluation in vitro revealed that the pyrazole core showed in several cases a different structure-activity relationship to that of related indole acetic acid. A potent series of ortho-sulfonyl benzyl substituents was found, from which two compounds I [R1 = H; R2 = Ph; X = SO2] and I [R1 = H; R2 = 4-FC6H4; X = SO2] were advanced to in vivo profiling.

European Journal of Medicinal Chemistry published new progress about Structure-activity relationship, receptor-binding. 35112-27-7 belongs to class chlorides-buliding-blocks, name is Ethyl 2,5-dichlorobenzoate, and the molecular formula is C9H8Cl2O2, Application of Ethyl 2,5-dichlorobenzoate.

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