30748-47-1Relevant articles and documents
Synthesis and application of 2-N-(thiazol-2-yl)benzo/naphtho [1,2-d]-1,2,3-triazoles
Rangnekar, Dinesh W.,Kazemi, Gadhir J.,Malanker, Jayesh V.,Ramamurthy, Rajesh
, p. 185 - 190 (1998)
The synthesis of a series of bright, intensely fluorescent brighteners bused on 2-N-(thiazol-2-yl)benzo/naphtho [1,2-d]-1,2,3-triazoles is described. The absorption - emission spectra of the fluorescent brighteners were recorded and their dyeing properties were studied.
N-(5-acetyl-4-methylthiazol-2-yl)arylamide derivatives as multi-target-directed ligands: design, synthesis, biochemical evaluation and computational analysis
Channar, Kashif Ali,Channar, Pervaiz Ali,Ejaz, Syeda Abida,Indher, Hafiz Abdul Bari,Ismail, Hammad,Mahmood, Hafiz Mohammad Kashif,Rafiq, Mamoona,Saeed, Aamer,Saeed, Amna,Saeed, Shomaila,Ujan, Rabail
, (2022/01/19)
In the present study, we are reporting the synthesis of a total eight derivatives of N-(5-acetyl-4-methylthiazol-2-yl) Arylamide derivatives (3a-h). The products obtained in good to excellent yield represents drug-like molecules with a well-developed structure-activity relationship. All the synthesized compounds were further subjected to chemical characterization (NMR, FTIR and elemental analysis) and further tested for biological activities (antioxidant, antibacterial, antifungal and α-glucosidase). The anti-oxidant properties of compound 3h (IC50 ± SEM = 141.9 ± 1.12?μg/mL) were found maximum in comparison to the rest of the derivatives. The antibacterial results showed the compounds 3d and 3h as a significant bacterial inhibitor. The significant fungicidal activity was observed by compound 3a with the zone of inhibition up to 24 mm which in comparison with the results of positive control (Terbinafine). When the effect was observed on α-glucosidase activity, the highest enzyme inhibition activity was observed by 3h (IC50 ± SEM 134.4 ± 1.01?μg/mL) followed by 3c (IC50 ± SEM = 157.3 ± 1.11?μg/mL). The results were further supported by molecular docking studies and the chemical stability of the derivatives was also performed by density functional theory (DFTs) calculations. The data revealed that most of the derivatives are multi-target ligands and can be used as lead molecules for the synthesis of derivatives for their further evaluation at molecular targets for the treatment of specific diseases. Graphical abstract: [Figure not available: see fulltext.] Synopsis This article reports the synthesis of a total of eight derivatives of N-(5-acetyl-4-methylthiazol-2-yl) Arylamide derivatives. The products obtained in good to excellent yield represents drug-like molecules with a well-developed structure-activity relationship.
Synthesis, Characterization, Crystal Structure and Biological Study of Carboxamides Obtained from 2-Aminothiazole Derivatives
Wazalwar, Sachin S.,Banpurkar, Anita R.,Perdih, Franc
, p. 319 - 329 (2019/07/29)
Abstract: Two series of novel thiazolylcarboxamide derivatives were synthesized by the reaction of ethyl 2-amino-4-methylthiazole-5-carboxylate or 1-(2-amino-4-methylthiazol-5-yl)ethan-1-one with four substituted carbonyl chlorides at 0?°C in excellent yi
Design, synthesis, antitumor activity and theoretical calculation of novel PI3Ka inhibitors
Guo, Hui,Jin, Ru-Yi,Li, Zhi,Long, Xu,Tang, Tian,Tang, Yu-Ping,Xie, Hong-Lei,Yan, Hao,Zhou, Jing,Zhou, Sha,Zuo, Zheng-Yu
, (2020/03/18)
PI3Kα has been identified as an ideal target to treat with PIK3CA gene mutation disease, including drugs such as Alpelisib and Copanlisib. Five purine analogues and four thiazole analogues were designed and synthesized. Their enzymatic activity against PI3Ka/β/γ/δ were tested, respectively. All compounds showed excellent selectivity in modulating PI3Ka activity, and parts of the compounds showed good inhibition. Meanwhile, we used Autodock 4.2 to explore the binding mode of the most potential compound Tg with the target protein. In addition, DFT was used to calculate the HOMO-LUMO maps of the compounds Tf, Tg and positive control. This paper will provide some useful information for further drug design of PI3Kα inhibitors.
5 - (3 - Phenyl-acryloyl) thiazole derivative and its preparation method and application (by machine translation)
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, (2018/10/02)
The present invention is shown in formula I 5 - (3 - phenyl-acryloyl) thiazole derivatives and their pharmaceutically acceptable salt, pharmaceutical composition and thereof in the preparation of influenza virus neuraminidase inhibitors in the application. Wherein R is selected from: methyl, ethyl, C3 - C4 Straight-chain or C3 - C4 Branched alkyl; R1 Is selected from: hydrogen, 2 - nitro, 3 - nitro, 4 - nitro, 2 - amino, 3 - amino, 4 - amino, 2 - methylamino, 3 - methylamino, 4 - methylamino, 2 - dimethylamino, 3 - dimethylamino, 4 - dimethylamino, 2 - methoxy, 3 - methoxy, 4 - methoxy, 2 - ethoxy, 3 - ethoxy, 4 - ethoxy, 2 - hydroxy, 3 - hydroxy, 4 - hydroxy, 2, 3 - dihydroxy, 2, 4 - dihydroxy, 2, 5 - dihydroxy, 3, 4 - dihydroxy, 3, 5 - dihydroxy, 2 - hydroxy - 3 - methoxy, 3 - hydroxy - 4 - methoxy, 4 - hydroxy - 3 - methoxy, 4 - hydroxy - 3 - ethoxy, 3, 4, 5 - trimethoxy or 4 - hydroxy - 3, 5 - dimethoxy; R2 Is selected from: hydrogen, C1 - C2 Alkyl, C3 - C4 Straight-chain or C3 - C4 Branched alkyl, trifluoromethyl or chloro C1 - C4 Straight-chain alkyl. (by machine translation)
Novel indole-thiazolidinone conjugates: Design, synthesis and whole-cell phenotypic evaluation as a novel class of antimicrobial agents
Abo-Ashour, Mahmoud F.,Eldehna, Wagdy M.,George, Riham F.,Abdel-Aziz, Marwa M.,Elaasser, Mahmoud M.,Abdel Gawad, Nagwa M.,Gupta, Antima,Bhakta, Sanjib,Abou-Seri, Sahar M.
, p. 49 - 60 (2018/10/20)
In connection with our research program on the development of novel anti-tubercular candidates, herein we report the design and synthesis of two different sets of indole-thiazolidinone conjugates (8a,b; 11a-d) and (14a-k; 15a-h). The target compounds were evaluated for their in vitro antibacterial and antifungal activities against selected human pathogens viz. Staphylococcus aureus (Gram positiveve), Pseudomonas aeruginosa, Escherichia coli (Gram negative), Mycobacterium tuberculosis (Acid-fast bacteria), Aspergillus fumigates and Candida albicans (fungi). Moreover, eukaryotic cell-toxicity was tested via an integrated ex vivo drug screening model in order to evaluate the selective therapeutic index (SI) towards antimicrobial activity when microbes are growing inside primary immune cells. Also, the cytotoxicity towards a panel of cancer cell lines and human lung fibroblast normal cell line, WI-38 cells, was explored to assure their safety. Compound 15b emerged as a hit in this study with potent broad spectrum antibacterial (MIC: 0.39–0.98 μg/mL) and antifungal (MIC: 0.49–0.98 μg/mL) activities, in addition to its ability to kill mycobacteria M. aurum inside an infected macrophage model with good therapeutic window. Moreover, compound 15b displayed promising activity towards resistant bacteria strains MRSA and VRE with MIC values equal 3.90 and 7.81 μg/mL, respectively. These results suggest compound 15b as a new therapeutic lead with good selectivity for further optimization and development.
TBHP/AIBN-Mediated Synthesis of 2-Amino-thioazoles from Active Methylene Ketones and Thiourea under Metal-free Conditions
Sun, Jiyun,Ge, Huaibin,Zhen, Xiaohua,An, Xuechan,Zhang, Guangtao,Zhang-Negrerie, Daisy,Du, Yunfei,Zhao, Kang
, p. 2107 - 2114 (2018/03/26)
A new oxidative system of tert-butyl hydroperoxide (TBHP)/azodiisobutyronitrile (AIBN) has been used for the first time for a convenient, metal-free synthesis of substituted 2-aminothioazoles from active methylene ketone derivatives and thiourea. The reaction is postulated to proceed via an oxidative cyclization initiated by a radical process and followed by a condensation reaction.
Nitrogenous condensed heterocyclic compound as well as preparation method, intermediate, composition and application thereof
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Paragraph 0315; 0316; 0317; 0318, (2018/11/22)
The invention discloses a nitrogenous condensed heterocyclic compound as well as a preparation method, an intermediate, a composition and application thereof. The compound disclosed by the invention has high inhibition activity for different subtypes of CDK (Cyclin-Dependent Kinase) at a molecular level, has good inhibition activity on breast cancer cells at a cell level, has a remarkable proliferation inhibition function on tumor cells related to cyclin-dependent kinase activity at an animal level, is good in liver microsome stability upon human beings, mice, and the like, is good in in-vivoabsorption in mice and rats, is high in bioavailability and is good in druggability.
MANNOSE DERIVATIVES USEFUL FOR TREATING PATHOLOGIES ASSOCIATED WITH ADHERENT E. COLI
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Page/Page column 70, (2017/02/28)
The present invention relates to mannose derivatives of formula (I): wherein R1 represents H, CO-(C1-C6)-alkyl or CO-alkylaryl, Y represents a single bond, CH2, O, NR3, S, A represents O, NH or S, X represents H and X' represents OH or X and X' taken together with the carbon atom bearing them form a CO group, R2 represents H, a linear or branched (C1-C6 )-alkyl or CF3, R3 represents H, a C1-C6 alkyl, a CO-(C1-C6 )-alkyl, CF3 or COCF3, and R is as described in claim 1. The mannose derivatives of formulae (I) are useful for treating pathologies associated with the presence of adherent Escherichia coli (AEC), in particular inflammatory bowel diseases (IBD), such as Crohn's disease and ulcerative colitis; a urinary tract infection, in particular painful bladder syndrome and cystitis, more particularly interstitial cystitis; irritable bowel syndrome; metabolic diseases such as metabolic obesity, diabetes, hypercholesterolemia; autoimmune inflammatory diseases; and colorectal cancer, in particular colon cancer.
Microwave-assisted green synthesis of new imidazo[2,1-b]thiazole derivatives and their antimicrobial, antimalarial, and antitubercular activities
Vekariya, Rajesh H.,Patel, Kinjal D.,Vekariya, Mayur K.,Prajapati, Neelam P.,Rajani, Dhanji P.,Rajani, Smita D.,Patel, Hitesh D.
, p. 6207 - 6231 (2017/10/05)
Abstract: We have synthesized some imidazo[2,1-b]thiazole derivatives by reaction of 1-(2-amino-4-methylthiazol-5-yl)ethanone or ethyl 2-amino-4-methylthiazole-5-carboxylate with α-bromo aralkyl ketones (phenacyl bromides) in presence of polyethylene glycol-400 (PEG-400) as efficient, inexpensive, biodegradable, and green reaction medium and catalyst (dual nature) under Microwave Irradiation (MWI) at 300?W as well as under thermal heating at 90?°C. Moreover, we also synthesized 1-(2-amino-4-methylthiazol-5-yl)ethanone and ethyl 2-amino-4-methylthiazole-5-carboxylate by one-pot reaction of acetyl acetone/ethyl acetoacetate with N-bromosuccinimide (NBS) and thiourea in presence of PEG-400 under microwave irradiation at 180?W. All synthesized compounds were screened for antimicrobial and antimalarial activities. All compounds were found to show good to excellent antibacterial activity, and some analogs exhibited good antimalarial activity.
