Category: 70057-67-9

Jatav, Varsha; Mishra, Pradeep; Kashaw, Sushil; Stables, J. P. published the artcile< Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is thiadiazolylstyryl quinazolinone preparation anticonvulsant sedative hypnotic CNS depressant agent.

A series of novel 3-[5-substituted phenyl-1,3,4-thiadiazol-2-yl]-2-styryl quinazoline-4(3H)-ones were synthesized and evaluated for anticonvulsant, sedative-hypnotic and CNS depressant activities. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight 2-styrylquinazolin-4(3H)-one derivatives were examined in the maximal electroshock induced seizures (MES) and s.c. pentylenetetrazole (scPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. Out of eighteen compounds only five, e.g., I (R = H or Cl), showed anticonvulsant activity in one or more test models. All except two compounds exhibited significant sedative-hypnotic activity via actophotometer screen. CNS depressant activity screened with the help of the forced swim pool method resulted into some potent compounds From the exptl. observation it can be concluded that synthesized compounds exhibited relatively better sedative-hypnotic and CNS depressant activities.

European Journal of Medicinal Chemistry published new progress about Anticonvulsants. 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

Zhao, Zhigang; Li, Lin; Liu, Min; Mei, Qinggang published the artcile< An efficient synthesis of novel bis-1,3,4-thiadiazolyl-carbamate derivatives based on deoxycholic acid under microwave irradiation>, Category: chlorides-buliding-blocks, the main research area is carboxylate thiosemicarbazide cyclocondensation; thiadiazole amine preparation carbamation deoxycholate; thiadiazolyl carbamate cholanoate preparation microwave.

An easy and efficient method for the synthesis of novel deoxycholic acid bis-1,3,4-thiadiazol-carbamate derivatives under microwave irradiation was developed. Twelve new Me 3α,12α-bis-[(5-aryl-1,3,4-thiadiazol-2-yl)carbamoyloxy]-cholan-24-oates were obtained in better yield (78-91%) and shorter time (15-22 min). Their structures were identified by 1H NMR, IR, MS spectra and elemental analyses.

Journal of Chemical Research published new progress about Aromatic carboxylic acids 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

Martins, Solange C.; Desoti, Vania C.; Lazarin-Bidoia, Danielle; Vandresen, Fabio; da Silva, Cleuza C.; Ueda-Nakamura, Tania; Silva, Sueli de O.; Nakamura, Celso V. published the artcile< Synthesis and evaluation of the trypanocidal activity of a series of 1,3,4-thiadiazole derivatives of R-(+)-limonene benzaldehyde-thiosemicarbazones>, Related Products of 70057-67-9, the main research area is thiadiazole preparation trypanocidal cytotoxicity.

A series of 1,3,4-thiadiazole derivatives of R-(+)-limonene benzaldehyde-thiosemicarbazones I has been synthesized. The synthesized compounds and a series of 1,3,4-thiadiazole without the monoterpene R-(+)-limonene II were tested in in-vitro assays against epimastigote and trypomastigote forms of T. cruzi, and the cytotoxicity was also determined in LLCMK2 cells. The 1,3,4-thiadiazole compounds showed significant trypanocidal activity and a high selectivity indexes. The vast majority of the monoterpene derivatives, substituted by R-(+)-limonene, presented better anti-T. cruzi activity than the non-substituted compounds Regarding the cytotoxic profile, the compounds without the monoterpene R-(+)-limonene were, in general, less toxic. The present findings indicate that the 1,3,4-thiadiazoles derivatives of R-limonene have potential trypanocidal activity that justify further studies to better understand the mechanism of action of these substances on T. cruzi.

Medicinal Chemistry Research published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Li, Xin-yang; Wang, De-pu; Li, Shuai; Xue, Wen-han; Qian, Xin-hua; Liu, Kai-li; Li, Yu-heng; Lin, Qi-qi; Dong, Gang; Meng, Fan-hao; Jian, Ling-yan published the artcile< Discovery of N-(1,3,4-thiadiazol-2-yl)benzamide derivatives containing a 6,7-methoxyquinoline structure as novel EGFR/HER-2 dual-target inhibitors against cancer growth and angiogenesis>, Category: chlorides-buliding-blocks, the main research area is dimethoxy quinolinyloxymethyl thiazolyl benzamide preparation EGFR HER2 inhibition antitumor; Angiogenesis; Dual-target inhibitor; EGFR; HER-2.

Targeting EGFR and HER-2 is an essential direction for cancer treatment. Here, a series of N-(1,3,4-thiadiazol-2-yl)benzamide derivatives containing a 6,7-methoxyquinoline structure was designed and synthesized to serve as EGFR/HER-2 dual-target inhibitors. The kinase assays verified that target compounds could inhibit the kinase activity of EGFR and HER-2 selectively. The results of CCK-8 and 3D cell viability assays confirmed that target compounds had excellent anti-proliferation ability against breast cancer cells (MCF-7 and SK-BR-3) and lung cancer cells (A549 and H1975), particularly against SK-BR-3 cells, while the inhibitory effect on healthy breast cells (MCF-10A) and lung cells (Beas-2B) was weak. Among them, the hit compound YH-9 binded to EGFR and HER-2 stably in mol. dynamics studies. Further studies found that YH-9 could induce the release of cytochrome c and inhibit proliferation by promoting ROS expression in SK-BR-3 cells. Moreover, YH-9 could diminish the secretion of VEGF and bFGF factors in SK-BR-3 cells, then inhibited tube formation and angiogenesis. Notably, YH-9 could effectively inhibit breast cancer growth and angiogenesis with little toxicity in the SK-BR-3 cell xenograft model. Taken together, in vitro and in vivo results revealed that YH-9 had high drug potential as a dual-target inhibitor of EGFR/HER-2 to inhibit breast cancer growth and angiogenesis.

Bioorganic Chemistry published new progress about Angiogenesis. 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

Amperayani, Karteek Rao; Parimi, Uma Devi published the artcile< Effect of silk strength by dietary supplementation of silk worm with 1,3,4-thiadiazoles, in silico and in vitro Bombyx mori DNA binding studies>, Product Details of C8H6ClN3S, the main research area is Bombyx silk strength feeding thiadiazole DNA binding.

In silico and in vitro DNA binding studies were carried out on silk worm DNA to determine the efficiency of 1,3,4-thiadiazoles (Th1-9) on Bombyx mori larvae during their 5th instar larval stage to increase the tensile strength, quality and quantity of biopolymer silk. These compounds were synthesized using ultrasonication method and supplied in ultra-dose as food supplement along with mulberry leaves to Bombyx mori and recorded the growth and other parameters of silkworm, cocoon parameters and mech. testing of silk filament. Tensile Strength, elongation and quantity of the silk was higher in larvae fed with synthesized compound in comparison with control larvae. This increase in strength and quality was due to the strong binding interactions of thiadiazoles moiety with silk worm DNA which was confirmed by higher binding energy values showed in In silco studies and DNA binding assay results.

Pharma Chemica published new progress about Binding energy. 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

Nam, Nguyen-Hai; Huong, Tran Lan; Dung, Do Thi Mai; Dung, Phan Thi Phuong; Oanh, Dao Thi Kim; Park, Sang Ho; Kim, Kyungrok; Han, Byung Woo; Yun, Jieun; Kang, Jong Soon; Kim, Youngsoo; Han, Sang-Bae published the artcile< Synthesis, bioevaluation and docking study of 5-substituted phenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents>, Application of C8H6ClN3S, the main research area is thiadiazole hydroxamic acid preparation histone deacetylase inhibitor antitumor; 5-phenyl-1,3,4-thiadiazole; cytotoxicity; heterocycle; histone deacetylase (HDAC) inhibitors.

Since the first histone deacetylase (HDAC) inhibitor (Zolinza, widely known as suberoylanilide hydroxamic acid; SAHA) was approved by the Food and Drug Administration for the treatment of T-cell lymphoma in 2006, the search for newer HDAC inhibitors has attracted a great deal of interest of medicinal chemists worldwide. As a continuity of the ongoing research in this area, the authors designed and synthesized a series of thiadiazole-based hydroxamic acids I [R = H, 2-Cl, 4-Me, etc.] as analogs of SAHA and evaluated their biol. activities. A number of compounds in this series, e.g. I [R = H], I [R = 2-Cl], I [R = 4-MeO], were found to possess potent anticancer cytotoxicity and HDAC inhibition effects. These compounds were generally two- to five-fold more potent in terms of cytotoxicity compared to SAHA against five cancer cell lines tested. Docking studies revealed that these hydroxamic acid displayed higher affinities than SAHA toward HDAC8.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antitumor 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

Bi, Qing-wei; Shi, Zhi-chuan; Zhao, Zhi-gang; Xia, Zhen-yang published the artcile< Synthesis of novel thiadiazoles type molecular tweezers based on hyodeoxycholic acid promoted by microwave irradiation>, Electric Literature of 70057-67-9, the main research area is thiadiazole mol tweezer hyodeoxycholic acid microwave preparation.

Ten novel steroidal mol. tweezers are efficiently synthesized via microwave irradiation by using hyodeoxycholic acid as spacer and 1, 3, 4-thiadiazoles unit as arm. Compared with a conventional method, the yields are increased from 38%∼48% to 80%∼91% and the reaction time is reduced from 1800-2400 min to 40-50 min. The structures of these novel mol. tweezers are characterized by 1H NMR, IR, ESI-MS spectra and elemental anal. The recognition properties of these mol. tweezers for D/L-Leu-OMe and D/L-Phe-OMe are investigated by UV-vis spectra. The result indicates that this type of mol. tweezers has good binding properties for D-amino acid Me esters.

Xinan Minzu Daxue Xuebao, Ziran Kexueban published new progress about Complexing agents. 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

Katane, Masumi; Osaka, Naoko; Matsuda, Satsuki; Maeda, Kazuhiro; Kawata, Tomonori; Saitoh, Yasuaki; Sekine, Masae; Furuchi, Takemitsu; Doi, Issei; Hirono, Shuichi; Homma, Hiroshi published the artcile< Identification of Novel d-Amino Acid Oxidase Inhibitors by in Silico Screening and Their Functional Characterization in Vitro>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is Amino acid oxidase inhibitor screening.

D-Amino acid oxidase (DAO) is a degradative enzyme that is stereospecific for d-amino acids, including d-serine and d-alanine, which are potential coagonists of the N-methyl-d-aspartate (NMDA) receptor. Dysfunction of NMDA receptor-mediated neurotransmission has been implicated in the onset of various mental disorders such as schizophrenia. Hence, a DAO inhibitor that augments the brain levels of d-serine and/or d-alanine and thereby activates NMDA receptor function is expected to be an antipsychotic drug, for instance, in the treatment of schizophrenia. In the search for potent DAO inhibitor(s), a large number of compounds were screened in silico, and several compounds were estimated as candidates. These compounds were then characterized and evaluated as novel DAO inhibitors in vitro. The results reported in this study indicate that some of these compounds are possible lead compounds for the development of a clin. useful DAO inhibitor and have the potential to serve as active site probes to elucidate the structure-function relationships of DAO.

Journal of Medicinal Chemistry published new progress about Antipsychotics. 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

Qu, Tengfei; Qu, Lailiang; Wang, Xiaoguang; Xu, Ting; Xiao, Xiao; Ding, Min; Deng, Li; Guo, Yong published the artcile< Design, synthesis, and antibacterial activity of novel 8-methoxyquinoline-2-carboxamide compounds containing 1,3,4-thiadiazole moiety>, Related Products of 70057-67-9, the main research area is arylthiadiazolyl methoxyquinoline carboxamide preparation antibacterial activity SAR; 1,3,4-thiadiazole; 2-methyl-8-hydroxyquinoline; antibacterial activity; structure-activity relationships.

A series of novel 8-methoxyquinoline-2-carboxamide compounds containing 1,3,4-thiadiazole moiety was designed and synthesized by using an active substructure combination method. Then, the antibacterial activities of all the target compounds were evaluated in-vitro against three Gram-pos. bacteria and three Gram-neg. bacteria. The antibacterial assay showed that some target compounds displayed moderate to good antibacterial efficacy in comparison with the reference drug chloromycin. Some interesting results of structure-activity relationships were also discussed.

Zeitschrift fuer Naturforschung, C: Journal of Biosciences 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

Yang, Tianjiao; Wang, Jiayi; Song, Gonghua published the artcile< Synthesis and nematicidal activity of azabicyclo[3.3.1]nonane-thiadiazole derivatives>, SDS of cas: 70057-67-9, the main research area is nematicidal azabicyclo nonane thiadiazole preparation agrochem.

Nematodes are crop pests which can cause serious loss in crop production and food crisis. Traditional nematicides, such as Carbamate, isothiocyanate and organophosphates, have largely inhibited the damages of nematodes on agriculture, but they also generate neg. effects on both plants and human health, such as root harm and human poisoning. Hence developing novel nematicides with low toxicity and high nematicidal efficiency are extremely urgent. 5-HT(5-hydroxytryptamine) is an important monoamine neurotransmitter which plays important role in mammalian endocrine function as well as in the central and peripheral nervous system. 5-HT was also found to be an important substance which can control the physiol. activities of nematodes including feeding, movement and reproduction So far, some studies have been reported on the development of 5-HT receptor as potential target for nematicides. Based on the previous achievements performed in our group and the principles of drug development, MDL 72222, a typical 5-HT3 receptor antagonist which can significantly inhibit the swallowing function of the pharyngeal pump in caenorhabditis elegans, has a lethal effect on nematicides at certain doses. Upon changing the configuration or number of carbon atoms of the bridged ring and introducing the bioactive group thiadiazole into the structure of compound MDL 72222, 23 new 3-azabicyclo[3.3.1]nonane-thiadiazoles derivatives were designed and synthesized. All the involved compounds were characterized by 1H-NMR, 13C-NMR and HRMS. The in vivo bioactivity test was performed using the root-knot nematodes, and the com. nematocidal agent Avermectin was used as the control product. The nematicidal activity against root-knot nematode was determined Ten target compounds exhibited certain inhibitory activity against root-knot nematodes at a concentration of 40 mg/L.

Huadong Ligong Daxue Xuebao, Ziran Kexueban published new progress about 5-HT antagonists. 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