320741-36-4Relevant articles and documents
Design, Synthesis, and Antibacterial Evaluation of Propylene-tethered 8-Methoxyl Ciprofloxacin-isatin Hybrids
Guo, Hua
, p. 2434 - 2440 (2018)
A series of 8-methoxyl ciprofloxacin (8-OMe CPFX)-isatin hybrids 3a–f and 4a–f tethered through propylene were designed, synthesized, and examined for their in vitro antibacterial activities against a panel of Gram-positive and Gram-negative pathogens including drug-resistant bacteria. All the synthesized hybrids (minimum inhibitory concentration: ≤0.03–64?μg/mL) exhibited considerable activities against the tested strains, especially against the Gram-negative pathogens. Among them, hybrid 3b was no inferior to the parent 8-OMe CPFX that could act as a starting point for further optimization.
Synthesis and antiprotozoal activity of mono- and bis-uracil isatin conjugates against the human pathogen Trichomonas vaginalis
Kumar, Kewal,Liu, Nicole,Yang, Donald,Na, Daniel,Thompson, John,Wrischnik, Lisa A.,Land, Kirkwood M.,Kumar, Vipan
, p. 5190 - 5197 (2015)
A library of mono- and bis-uracil isatin conjugates were synthesized and subjected for the assessment of their in vitro activity against the protozoal pathogen Trichomonas vaginalis. The structure activity studies (SAR) revealed that the bis-uracil-isatin based conjugates were more effective than their corresponding mono conjugates in inhibiting the growth of T. vaginalis at approximately 10 μM with no visual effect on mammalian cells at the same concentration.
Benzofuran-isatin-imine hybrids tethered via different length alkyl linkers: Design, synthesis and in vitro evaluation of anti-tubercular and anti-bacterial activities as well as cytotoxicity
Gao, Feng,Wang, Tengfei,Gao, Meixiang,Zhang, Xia,Liu, Zhuqing,Zhao, ShiJia,Lv, ZaoSheng,Xiao, Jiaqi
, p. 323 - 331 (2019)
Herein we report the design and synthesis of twenty-two novel benzofuran-isatin-imine hybrids 7a-v tethered through propylene, butylene, pentylene and hexylene, and for the evaluation of their in vitro anti-tubercular and anti-bacterial activities as well
Benzofuran-isatin hybrids tethered via different length alkyl linkers and their in vitro anti-mycobacterial activities
Gao, Feng,Chen, Zijian,Ma, Long,Qiu, Lin,Lin, Jianguo,Lu, Guangming
, p. 2652 - 2656 (2019)
A series of novel benzofuran-isatin hybrids 6a–m tethered through different length alkyl linkers propylene, butylene, pentylene and hexylene were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against both drug-suscep
Diastereoselective approach to rationally design tetrahydro-β-carboline-isatin conjugates as potential SERMs against breast cancer
Sharma, Bharvi,Singh, Amandeep,Gu, Liang,Saha, Sourav Taru,Singh-Pillay, Ashona,Cele, Nosipho,Singh, Parvesh,Kaur, Mandeep,Kumar, Vipan
, p. 9809 - 9819 (2019)
A series of tetrahydro-β-carboline-isatin conjugates, with varying substituents as well as stereochemistry at C-1 and C-5 position of tetrahydro-β-carboline (THβC) and isatin ring, were prepared and assayed for anti-proliferative efficacy on Estrogen Responsive ER(+) (MCF-7) and ER(?ve) MDA-MB-231 cell-lines. The synthesized scaffolds displayed selective anti-proliferative efficacy against MCF-7 cell-line with the most active conjugate 8b exhibiting an IC50 value of 37.42 μM, comparable to that of peganumine A, a tetrahydro-β-carboline analogue, isolated from Peganum harmala. The synthesized compound 8b was also more potent than the standard drug tamoxifen (IC50 = 50 μM against MCF-7). The observed activities were further corroborated via docking studies in ER-α (PDB ID: 3ERT).
Benzofuran–isatin Hybrids: Design, Synthesis, and In Vitro Anti-cancer Activities
Diao, Quan-Ping,Guo, Hua,Wang, Gang-Qiang
, p. 1687 - 1693 (2019)
A series of novel benzofuran–isatin hybrids 6a–s tethered through propylene and butylene were designed, synthesized, and evaluated for their in vitro anti-cancer activities against HepG2 (liver carcinoma), Hela (cervical cancer), A549 (lung adenocarcinoma
Benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids: Design, synthesis and in vitro anti-mycobacterial activity evaluation
Zhang, Yaohuan,Wang, Ruo,Zhang, Tesen,Yan, Weitao,Chen, Yihong,Zhang, Yanping,Zhou, Muyang
, p. 653 - 655 (2019)
A series of novel benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids were designed, synthesized and evaluated for their in vitro anti-TB activities against drug-sensitive MTB H37Rv and MDR-TB isolates as well as cytotoxicity. All benzofu
Bioactive isatin (oxime)-triazole-thiazolidinedione ferrocene molecular conjugates: Design, synthesis and antimicrobial activities
Yagnam, Swetha,Trivedi, Rajiv,Krishna, Suman,Giribabu, Lingamallu,Praveena, Ganji,Prakasham, Reddy Shetty
, (2021)
Molecular conjugates often combine the inherent properties of the individual components and exhibit a different characteristic feature. Introduction of an organometallic moiety can indeed augment the overall effect. This article narrates the synthesis of ferrocene appended isatin?2,4-thiazolidinedione molecular hybrid linked via a triazole moiety. Isatin and 2,4-thiazolidinedione were linked via a triazole unit formed by a simple copper catalysed alkyne-azide 1,3-dipolar cycloaddition reaction. The UV–vis and electrochemical studies on all the new compounds are reported. Antimicrobial activity against some selected gram-positive and gram-negative strains was also examined for all the new derivatives and compounds 6(b), 6(c), 6(h) and 6(i) revealed similar antimicrobial activity for all tested microbes and similar pattern to that of standard antibiotics.
Synthesis and in vitro evaluation of novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids for their anti-mycobacterial activities
Yan, Xinjia,Lv, Zaosheng,Wen, Jing,Zhao, Shijia,Xu, Zhi
, p. 899 - 904 (2018)
Twelve novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids 5a-l were designed, synthesized and screened for their in vitro anti-mycobacterial activities against drug-sensitive and multidrug-resistant Mycobacterium tubercu
Synthesis and in vitro cytotoxic evaluation of N-alkylbromo and N-alkylphthalimido-isatins
Singh, Pardeep,Kaur, Sharanjeet,Kumar, Vipan,Bedi,Mahajan,Sehar, Irum,Pal, Harish Chandra,Saxena, Ajit Kumar
, p. 3017 - 3020 (2011)
The manuscript pertains to the synthesis and in vitro cytotoxic evaluation of a series of N-alkylbromo and N-alkylphthalimido-isatins against four different human cancer cell lines namely Colon: HCT-15; Liver: Hep-2; Lung: A-549 and Leukemia: THP-1 at 10 and 100 μM concentrations. The active compounds based on preliminary studies were evaluated for their IC50 value against six cell lines viz. Colo-205, HCT-15 (Colon), THP-1 (Leukemia), A-549 (Lung), PC-3 (Prostate) and HeLa (Cervix). The active analogue IS-4 exhibited IC50 values of 4.57, 10.90, 11.75, 12.40 and 54.20 μM against HeLa, PC-3, HCT-15, THP-1 and Colo-205, respectively.
