3028-02-2Relevant academic research and scientific papers
(Z)-2-(Benzo[d]thiazol-2-ylamino)-5-(substituted benzylidene) thiazol-4(5H)-one derivatives as novel tyrosinase inhibitors
Kang, Kyeong Ha,Lee, Bonggi,Son, Sujin,Yun, Hwi Young,Moon, Kyoung Mi,Jeong, Hyoung Oh,Kim, Dae Hyun,Lee, Eun Kyeong,Choi, Yeon Ja,Kim, Do Hyun,Chun, Pusoon,Moon, Hyung Ryong,Chung, Hae Young
, p. 1227 - 1233 (2015)
Inhibiting tyrosinase is an important goal to prevent melanin accumulation in skin and thereby to inhibit pigmentation disorders. Therefore, tyrosinase inhibitors are an attractive target in cosmetics and treatments for pigmentation disorders. However, on
Thiazole and benzothiazole derivatives of cytisine
Saprykina,Vinogradova,Ambartsumova,Ibragimov,Shakhidoyatov
, p. 470 - 472 (2006)
Several new derivatives were prepared by reacting N-1(5-R-thiazol-2-yl)-2- chloroacetamides and N-1(6-R-benzothiazol-2-yl)chloroacetamides with cytisine.
Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents
Sever, Belgin,Altlntop, Mehlika Dilek,?zdemir, Ahmet,Tabanca, Nurhayat,Estep, Alden S.,Becnel, James J.,Bloomquist, Jeffrey R.
, p. 288 - 294 (2019)
Aedes aegypti is associated with the transmission of numerous human and animal diseases, such as yellow fever, dengue fever, chikungunya, and more recently Zika virus. Emerging insecticide resistance has created a need to develop new mosquitocidal agents for effective control operations. A series of benzothiazole-piperidine derivatives (1-24) were investigated for their larvicidal and adulticidal effects on Ae. aegypti It was observed that compounds 2, 4, 6, 7, 8, 11 and 13 showed notable larvicidal activity. Furthermore, compounds 6 and 10 showed promising adulticidal activity. Based on the mosquitocidal properties of these compounds, docking studies were also carried out in the active site of the AeSCP2 enzyme to explore any insights into further in vitro enzyme studies. Docking results indicated that all these active compounds showed reasonable interactions with critical residues in the active site of this enzyme. This outcome suggested that these compounds might show their larvicidal and adulticidal effects via the inhibition of AeSCP2. According to in vitro and in silico studies, compounds 2, 4, 6, 7, 8, 10, 11 and 13 stand out as candidates for further studies.
Biological evaluation of some antimicrobial nano-materials
Mokhtari, Bahram,Pourabdollah, Kobra
, p. 663 - 670 (2013)
N-(benzothiazol-2-yl)-2-(piperidin-1-yl)acetamide derivatives (1-24) were obtained by the reaction of 2-chloro-N-(benzothiazole-2-yl)acetamides with piperidine derivatives. The structures of the compounds were elucidated by 1H-NMR and mass spectral data and elemental analysis. The compounds were screened for their antimicrobial activities against pathogenic bacteria and Candida species. The compounds were also investigated for their cytotoxic properties usingMTT assay. The microbiological results revealed that the compounds were more effective against fungi than bacteria. Among Candida species C. utilis was the most susceptible fungus to compounds 7 and 11. It is apparent that 2,6-dimethylpiperidine group and chloro and methyl substituents on benzothiazole ring have an important impact on anticandidal activity. MTT assay indicated that the effective doses of these derivatives were lower than their cytotoxic doses.
2-Heteroarylimino-5-benzylidene-4-thiazolidinones analogues of 2-thiazolylimino-5-benzylidene-4-thiazolidinones with antimicrobial activity: Synthesis and structure-activity relationship
Vicini, Paola,Geronikaki, Athina,Incerti, Matteo,Zani, Franca,Dearden, John,Hewitt, Mark
, p. 3714 - 3724 (2008)
2-Heteroarylimino-5-benzylidene-4-thiazolidinones, unsubstituted or carrying hydroxy, methoxy, nitro and chloro groups on the benzene ring, were synthesised and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria, yeasts and mould. The antimicrobial activity of the 2-benzo[d]thiazolyl- and of the 2-benzo[d]isothiazolyl-imino-5-benzylidene-4-thiazolidinones is, on the whole, lower in comparison with the high activity detected for the derivatives of the 2-thiazolylimino-5-benzylidene-4-thiazolidinone class. Nevertheless most of the benzo[d]thiazole analogues display good inhibition of the growth of Gram positive bacilli and staphylococci, including methicillin-resistant Staphylococcus strains. Among the 2-benzo[d]isothiazole analogues a few derivatives show a strong and selective activity against bacilli. Moreover, it is worth noting that the replacement of the thiazole nucleus for the benzo[d]thiazole bicyclic system in the parent 2-(benzo[d]thiazol-2-ylimino)thiazolidin-4-one leads to significant antifungal properties against both yeasts and moulds, properties not shown by the analogous 2-thiazolyl- and 2-benzo[d]isothiazolyl-imino)thiazolidin-4-ones. The structure-activity relationship of 33 analogues possessing the 2-heteroarylimino-4-thiazolidinone structure is analysed through QSAR models.
Synthesis, in silico pharmacokinetic analysis and anticancer activity evaluation of benzothiazole-triazole hybrids
Rawat, Srishti,Rawat, Diwan S.,Negi, Beena
, p. 409 - 417 (2021/09/28)
Over the past decade, a variety of benzothiazole derivatives have been reported with promising anticancer activity. Benzothiazole and its analogues are capable of acting on a number of molecular targets and thus exerting their anticancer activity. To further develop benzothiazole derivatives as anticancer agents, we attempted to design and synthesize a library of benzothiazole-triazole derivatives. The synthesized hybrid compounds have been selected by National Cancer Institute, USA for the in vitro activity evaluation against 60 human cancer cell lines in a one dose screening panel. Most of the synthesized compounds showed 60-80% growth rate against renal cancer cell line UO-31.
An extensive research on aldose reductase inhibitory effects of new 4H-1,2,4-triazole derivatives
Sever, Belgin,Alt?ntop, Mehlika Dilek,Demir, Yeliz,Pekdo?an, Muhammed,Akal?n ?ift?i, Gül?en,Beydemir, ?ükrü,?zdemir, Ahmet
, (2020/10/27)
Aldose reductase (AR) is a key enzyme, which triggers the excessive accumulation of sorbitol in insulin independent tissues leading to severe diabetes-induced microvascular complications. Substantial evidence has proven that AR inhibition is a well-establ
Synthesis and docking study of some bioactive n-(Benzo[d]thiazol-2-yl)-2-(4-((substituted)phenoxy)acetamide on cyclo-oxygenase-2 enzyme and in vivo analgesic activity evaluation
Kumar, Sumit,Kumar, Arvind,Verma, Amit,Mishra, Arun Kumar
, p. 396 - 405 (2021/06/17)
Background: The benzothiazole and its derivatives reported an extremely crucial duty in the progress of commercially important intermediary molecules, which are wanted for the manufac-turing of various pharmacologically active agents. Introduction: As a n
Thiazolidinedione "magic Bullets" Simultaneously Targeting PPARγand HDACs: Design, Synthesis, and Investigations of their in Vitro and in Vivo Antitumor Effects
Tilekar, Kalpana,Hess, Jessica D.,Upadhyay, Neha,Bianco, Alessandra Lo,Schweipert, Markus,Laghezza, Antonio,Loiodice, Fulvio,Meyer-Almes, Franz-Josef,Aguilera, Renato J.,Lavecchia, Antonio,Ramaa
, p. 6949 - 6971 (2021/06/25)
Monotargeting anticancer agents suffer from resistance and target nonspecificity concerns, which can be tackled with a multitargeting approach. The combined treatment with HDAC inhibitors and PPARγagonists has displayed potential antitumor effects. Based on these observations, this work involves design and synthesis of molecules that can simultaneously target PPARγand HDAC. Several out of 25 compounds inhibited HDAC4, and six compounds acted as dual-targeting agents. Compound 7i was the most potent, with activity toward PPARγEC50 = 0.245 μM and HDAC4 IC50 = 1.1 μM. Additionally, compounds 7c and 7i were cytotoxic to CCRF-CEM cells (CC50 = 2.8 and 9.6 μM, respectively), induced apoptosis, and caused DNA fragmentation. Furthermore, compound 7c modulated the expression of c-Myc, cleaved caspase-3, and caused in vivo tumor regression in CCRF-CEM tumor xenografts. Thus, this study provides a basis for the rational design of dual/multitargeting agents that could be developed further as anticancer therapeutics.
Targeting EGFR tyrosine kinase: Synthesis, in vitro antitumor evaluation, and molecular modeling studies of benzothiazole-based derivatives
Mokhtar, Amal M.,El-Messery, Shahenda M.,Ghaly, Mariam A.,Hassan, Ghada S.
, (2020/09/15)
New benzothiazole-based derivatives were synthesized in the present work with the aim of evaluating their antitumor activity. They were in vitro tested against hepatocellular carcinoma (HepG2), colorectal carcinoma (HCT-116), mammary gland cancer (MCF-7), prostate cancer (PC-3), and epithelioid carcinoma (HeLa). The results of the in vitro antitumor evaluation revealed that the most active compounds were 39, 40, 51, 56, and 61 exhibiting IC50 values comparable to the reference drug lapatinib. The most active compounds were further subjected to EGFR inhibitory activity assay to rationalize their potency mode. Notably, the most active antitumor compounds 39 and 40 represented the most potent inhibitors to EGFR with IC50 values of 24.58 and 30.42 nM respectively in comparison with 17.38 nM for lapatinib as a standard drug. Molecular modeling studies were also conducted for the synthesized compounds, including docking into EGFR active site and surface mapping. Results proved the superior binding of the hydrazone derivatives 39 and 40 with EGFR suggesting them as good candidates for targeted antitumor therapy through EGFR kinase inhibition.
