Category: 70057-67-9

Calas, Michele; Ouattara, Mahama; Piquet, Gilles; Ziora, Zyta; Bordat, Y.; Ancelin, Marie L.; Escale, Roger; Vial, Henri published the artcile< Potent Antimalarial Activity of 2-Aminopyridinium Salts, Amidines, and Guanidines>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is aminopyridinium salt amidine guanidine derivative preparation antimalarial malaria Plasmodium.

The authors describe the design, synthesis, and antimalarial activity of 60 bis-tertiary amine, bis-2(1H)-imino-heterocycle, bis-amidine, and bis-guanidine series. Bis-tertiary amines with a linker from 12 to 16 methylene groups were active against the in vitro growth of Plasmodium falciparum within the 10-6-10-7 M concentration range. IC50 decreased by 2 orders of magnitude for bis-2-aminopyridinium salts, bis-amidines, and bis-guanidines (27 compounds with IC50 < 10 nM). Increasing the alkyl chain length from 6 to 12 methylene groups led to increased activity, while beyond this antimalarial activity decreased. Antimalarial activities appear to be strictly related to the basicity of the cationic head with an optimal pKa over 12.5. Maximal activity occurs for bis-2-aminopyridinium, two C-duplicated bis-amidines, and three bis-guanidines, with IC50 values lower than 1 nM. In comparison to similar quaternary ammonium salts, amidinium compounds have distinct structural requirements for antimalarial activity and likely addnl. binding opportunities on account of their hydrogen-bond-forming properties. Journal of Medicinal Chemistry published new progress about Antimalarials. 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

Liu, Zheng; Bian, Ming; Ma, Qian-Qian; Zhang, Zhuo; Du, Huan-Huan; Wei, Cheng-Xi published the artcile< Design and synthesis of new benzo[d]oxazole-based derivatives and their neuroprotective effects on β-amyloid-induced PC12 cells>, HPLC of Formula: 70057-67-9, the main research area is benzoxazolylthio aryl thiadiazolyl acetamide preparation Alzheimer neuroprotective amyloid; Akt/GSK-3β/NF-κB signaling pathway; Alzheimer’s disease; benzo[d]oxazol; synthesis; thiadiazoles; β-amyloid.

A series of novel synthetic substituted benzo[d]oxazole-based derivatives I (R = H, 3,4,5-(OMe)3, 2-Cl-5-F, etc.) exerted neuroprotective effects on β-amyloid (Aβ)-induced PC12 cells as a potential approach for the treatment of Alzheimer’s disease (AD). In vitro studies show that most of the synthesized compounds I were potent in reducing the neurotoxicity of Aβ25-35-induced PC12 cells at 5μg/mL. The compound I (R = 3-Cl) (II) was non-neurotoxic at 30μg/mL and significantly increased the viability of Aβ25-35-induced PC12 cells at 1.25, 2.5 and 5μg/mL. Western blot anal. showed that compound II promoted the phosphorylation of Akt and glycogen synthase kinase (GSK-3β) and decreased the expression of nuclear factor-κB (NF-κB) in Aβ25-35-induced PC12 cells. In addition, the findings demonstrated that compound II protected PC12 cells from Aβ25-35-induced apoptosis, reduced the hyperphosphorylation of tau protein, and decreased the expression of receptor for AGE (RAGE), β-site amyloid precursor protein (APP)-cleaving enzyme 1 (BACE1), inducible nitric oxide synthase (iNOS) and Bcl-2-associated X protein/B-cell lymphoma 2 (Bax/Bcl-2) via Akt/GSK-3β/NF-κB signaling pathway. In vivo studies suggest that compound II shows less toxicity than donepezil in the heart and nervous system of zebrafish.

Molecules published new progress about Alzheimer disease. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, HPLC of Formula: 70057-67-9.

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

Alam, Faruk; Dey, Biplab Kr. published the artcile< Synthesis, characterization and in-vitro anti-oxidant activity of some novel 1,3,4-thiadiazole derivatives>, Product Details of C8H6ClN3S, the main research area is aryl thiadiazolyl thioureido piperidinyl hydrazinyl acetamide preparation antioxidant SAR; acetamide aromatic amino thiadiazolyl aryl preparation antioxidant SAR.

Synthesis of 1,3,4-thiadiazole derivatives I [R1 = 2-OH, 3-Cl, 4-O2N; R2 = hydrazinyl, thioureido, piperidin-1-yl] and II [R3 = PhNH, PhNHNH, Ph2N] was reported. All the synthesized compounds I and II were studied for their antioxidant activity. SAR studies revealed that the tested compounds having hydroxy and halogen substituents on the aromatic ring showed higher activity compared to those with other substituents, for e.g., II [R1 = 2-OH, R3 = PhNHNH] showed good scavenging activity.

Pharma Chemica published new progress about Amides Role: PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Product Details of C8H6ClN3S.

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

Spillane, William J.; Coyle, Catherine M.; Feeney, Brendan G.; Thompson, Emer F. published the artcile< Development of Structure-Taste Relationships for Thiazolyl-, Benzothiazolyl-, and Thiadiazolylsulfamates>, Electric Literature of 70057-67-9, the main research area is heterocyclic sulfamate taste MSBAR.

A total of 28 new five-membered aromatic ring thiazolyl-, benzothiazolyl-, and thiadiazolylsulfamates, as their sodium salts, have been synthesized and combined with 30 known similar heterocyclic sulfamates to create a database for the study of structure-activity (taste) relationships (SARs) in this heterocyclic subgroup, which is known to contain a somewhat disproportionate number of sweet compounds compared to other groups of tastants. A series of nine parameters (descriptors) to describe the properties of the sulfamate anions were calculated in Spartan Pro and HyperChem programs. These are the HOMO, LUMO, length of the mol., dipole moment, area, volume, Esolv, σ (from the literature), and log P. The taste data for all 58 compounds were categorized into three classes, namely, sweet (S), nonsweet (N), and nonsweet/sweet (N/S). Discriminant anal. only classified 44 of the 58 compounds correctly. Classification and regression tree anal. (CART) using the S_ Plus program proved highly effective, in that the derived tree correctly classified 46 compounds from a training set of 48 and, from a computer randomly selected test set of 10 compounds, 7 had their taste correctly predicted. A second tree was grown using the addnl. taste category N/S, and this tree also performed extremely well, with 8 of the 10 compounds in the test set correctly classified. These trees should be very reliable for predicting the tastes of other heterocyclic sulfamates, which belong to the subset used here.

Journal of Agricultural and Food Chemistry published new progress about Discriminant analysis. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Electric Literature of 70057-67-9.

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

Jatav, Varsha; Kashaw, Sushil; Mishra, Pradeep published the artcile< Synthesis, antibacterial and antifungal activity of some novel 3-[5-(4-substituted phenyl) 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones>, Application of C8H6ClN3S, the main research area is aryl thiadiazolyl styryl quinazolinone preparation antibacterial antifungal activity.

A series of novel 3-[5-substituted phenyl-1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones, e.g., I, were synthesized and evaluated for antibacterial activity against pathogenic strains of Staphylococcus aureus (MTCC number 96), Bacillus subtilis (MTCC number 619), Pseudomonas aeruginosa (MTCC number 424) and Escherichia coli (MTCC number 40) and antifungal activity against Aspergillus niger, Candida albicans and Fusarium oxysporum. The cup-plate method was employed to determine the min. inhibitory concentration (MIC) value of the compounds Some of the compounds exhibited activity comparable to Norfloxacin. The present report reveals that synthesized 2-styryl-quinazoline-4(3H)-one exhibited better antibacterial than antifungal activity.

Medicinal Chemistry Research published new progress about Antibacterial agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Application of C8H6ClN3S.

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

Pandit, Neelanjana; Shah, Kamal; Agrawal, Neetu; Upmanyu, Neeraj; Shrivastava, Sushant K.; Mishra, Pradeep published the artcile< Synthesis, characterization and biological evaluation of some novel fluoroquinolones>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is fluoroquinolone thiadiazole derivative preparation bactericide fungicide.

Different derivatives of fluoroquinolones were synthesized by combining them with different thiadiazoles. The synthesized compounds were characterized by IR spectroscopy, proton NMR and mass spectral data. The compounds were screened for their antibacterial and antifungal activity. Ciprofloxacin thiadiazole 7c (I) showed good antibacterial as well as antifungal activities, whereas 13c and 13e (II; R1 = Cl, R2 = H and R1 = R2 = OMe, resp.) showed antibacterial and antifungal activity resp. Sparfloxacin derivative 8c (III) showed both antibacterial and antifungal activity. Sparfloxacin derivatives 14b and 14e (IV; R1 = H, R2 = Cl and R1 = R2 OMe) showed antibacterial and antifungal activity resp.

Medicinal Chemistry Research published new progress about Antibacterial agents. 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

Joseph, Alex; Pai, Aravinda; Srinivasan, K. K.; Kedar, Tukaram; Thomas, Angel Treasa; Jessy, E. M.; Singla, Rajeev K. published the artcile< Synthesis and anticancer activity of some novel 3-(1,3,4-thiadiazol-2-yl)-quinazolin-4(3H)-ones>, Synthetic Route of 70057-67-9, the main research area is thiadiazolylquinazolinone preparation anticancer; quinazolinone thiadiazolyl preparation anticancer.

The synthesis of various thiadiazole-substituted quinazolin-4(3H)-ones was reported. Novel 3-(1,3,4-thiadiazol-2-yl)quinazolin-4(3H)-ones were synthesized by reaction of 5-alkyl/aryl-1,3,4-thiadiazol-2-amines with 2-methyl/phenyl-4H-1,3-benzoxazin-4-ones in the presence of pyridine. All the synthesized compounds were characterized by spectra and phys. data. In vitro anticancer activity of all the synthesized compounds was determined by MTT assay on HeLa cells. Most active compounds from in vitro studies were further evaluated for in vivo activity on Liquid tumor (Ehrlich’s Ascites Carcinoma; EAC)-induced mice. The anticancer activity of one of the compounds was comparable to that of cisplatin against HeLa cells, and this compound was also effective in preventing the growth of tumor in mice as indicated by decrease in progressive gain in body weight as well as increase in life span.

Orbital: The Electronic Journal of Chemistry published new progress about Antitumor agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Synthetic Route of 70057-67-9.

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

Kerru, Nagaraju; Gummidi, Lalitha; Bhaskaruni, Sandeep V. H. S.; Maddila, Surya Narayana; Jonnalagadda, Sreekantha B. published the artcile< Ultrasound-assisted synthesis and antibacterial activity of novel 1,3,4-thiadiazole-1H-pyrazol-4-yl-thiazolidin-4-one derivatives>, Related Products of 70057-67-9, the main research area is diphenylpyrazolyl phenylthiadiazolyl thiazolidinone preparation ultrasonication green chem antibacterial SAR.

An efficient multicomponent method was reported for the synthesis of biol. active 1,3,4-thiadiazole-1H-pyrazol-4-yl-thiazolidin-4-one hybrids I [R = H, 3-Cl, 3,4,5-tri-MeO, etc.] from the reaction of pyrazole-4-carbaldehyde, 5-(substituted phenyl)-1,3,4-thiadiazol-2-amines and 2-mercaptoacetic acid in ethanol under ultrasound irradiation Reactions gave excellent yields (91-97%) of desired products in short times (55-65 min) at 50°C. All the twelve new thiazolidin-4-one derivatives I were fully characterized by spectroscopic techniques and were screened for their antibacterial activity. Among the screened hybrids, derivatives I [R = 3-O2N, 4-O2N] showed fourfold (MBC = 156.3μg/cm3) and twofold (MBC = 312.5μg/cm3) stronger potency against Pseudomonas aeruginosa strain as compared to the standard ciprofloxacin. SAR studies revealed the importance of the functional groups on the Ph ring of 1,3,4-thiadiazol-2-amine moiety for varying bacterial activity. The electron-withdrawing (NO2) group at para- and meta-position played a significant role in enhancing the antibacterial activity. The prominent features of the described protocol are excellent yields, green protocol, catalyst-free, high atom economy (94%) and excellent carbon efficiency (98%).

Monatshefte fuer Chemie published new progress about Antibacterial agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Related Products of 70057-67-9.

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

Gummidi, Lalitha; Kerru, Nagaraju; Awolade, Paul; Raza, Asif; Sharma, Arun K.; Singh, Parvesh published the artcile< Synthesis of indole-tethered [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids as anti-pancreatic cancer agents>, Synthetic Route of 70057-67-9, the main research area is indole tethered thiadiazolo oxadiazolopyrimidinone hydrid preparation antitumor agent; Indole; Molecular hybridization; Pancreatic cancer; Pyrimidinone; [4+2] Cycloaddition reaction.

New indole-tethered [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one (e.g. I) and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids (e.g. II) were synthesized using [4+2] cycloaddition reactions of functionalized 1,3-diazabuta-1,3-dienes with indole-ketenes. All mol. hybrids were structurally characterized by spectroscopic techniques (IR, NMR, and HRMS) and screened for their anti-pancreatic cancer activity in vitro. The [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids showed stronger anti-pancreatic cancer activity than the [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one hybrids against the PANC-1 cell line. II bearing an ortho-chlorophenyl moiety emerged as the most potent anti-pancreatic cancer agent with an IC50 value of 7.7 ± 0.4μM, much superior to the standard drug Gemcitabine (IC50 > 500μM). The discovery of these [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids elicits their potentials as pursuable candidates for pancreatic cancer chemotherapy.

Bioorganic & Medicinal Chemistry Letters published new progress about [4+2] Cycloaddition reaction. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Synthetic Route of 70057-67-9.

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

Yu, Yuye published the artcile< Microwave-assisted synthesis and biological activity of 2,5-disubstituted-1,3,4-thiadiazole>, SDS of cas: 70057-67-9, the main research area is carboxylic acid thiosemicarbazide cyclocondensation phosphoryl chloride dehydrating agent; thiadiazole preparation antifungal activity.

The reaction of substitute aryl and alkyl acid with thiosemicarbazide in the presence of dehydrating agent POCl3, affords a series of 2-amino-5-aryl-1,3,4-thiadiazoles under microwave irradiation 2,5-Disubstituted-1,3,4-thiadiazoles have attracted much attention due to their diverse biol. activities, such as antimicrobial, antibacterial, anesthetic, anticonvulsant and antiinflammatory activities. Compared with classical methods, this method has the advantages of high yields, short reaction time, easy preparation and mild reaction conditions. The preliminary biol. test showed that the synthesized compound has weak antifungal activity to G. zeae Petch, B. cinerea Pers, Phytophthora infestans (Mont.) de Bary, Botryosphaeria berengeriana f. sp. piricola (Nose) koganezawa et Sakuma, Fusarium oxysporum f.sp. cucumerinum and Cercospora arachidicola. The structures of compounds were characterized by m.ps., 1H NMR and IR.

Asian Journal of Chemistry published new progress about Carboxylic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 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