Design and synthesis of novel isatin derivatives as potent analgesic, anti-inflammatory and antimicrobial agents

Lahari, Kosaraju; Sundararajan, Raja

doi:10.1007/s12039-020-01795-0

Cited by 19 publications

(12 citation statements)

References 25 publications

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“…In 2020, Lahari et al [ 75 ] designed a new set of indole-2,3-dione analogues (53a – m) for their analgesic, anti-inflammatory, and antimicrobial potential. The antimicrobial potential of furnished analogues was examined against a panel of bacterial and fungal strains.…”

Section: Development Of Isatin Derivatives As Promising Therapeutic A...mentioning

confidence: 99%

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Cheke¹,

Patil²,

Firke

et al. 2022

Pharmaceuticals

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Isatin (1H indole 2, 3-dione) is a heterocyclic, endogenous lead molecule recognized in humans and different plants. The isatin nucleus and its derivatives are owed the attention of researchers due to their diverse pharmacological activities such as anticancer, anti-TB, antifungal, antimicrobial, antioxidant, anti-inflammatory, anticonvulsant, anti-HIV, and so on. Many research chemists take advantage of the gentle structure of isatins, such as NH at position 1 and carbonyl functions at positions 2 and 3, for designing biologically active analogues via different approaches. Literature surveys based on reported preclinical, clinical, and patented details confirm the multitarget profile of isatin analogues and thus their importance in the field of medicinal chemistry as a potent chemotherapeutic agent. This review represents the recent development of isatin analogues possessing potential pharmacological action in the years 2016–2020. The structure–activity relationship is also discussed to provide a pharmacophoric pattern that may contribute in the future to the design and synthesis of potent and less toxic therapeutics.

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Section: Development Of Isatin Derivatives As Promising Therapeutic A...mentioning

confidence: 99%

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Cheke¹,

Patil²,

Firke

et al. 2022

Pharmaceuticals

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show abstract

“…Địa chỉ email: nguyendinthanh@hus.edu.vn https://doi.org/10.25073/2588-1140/vnunst.5174 methylbuten-2'-yl)isatin được tìm thấy trong Streptomyces albus [2]. Các tài liệu tham khảo [3] chỉ ra rằng isatin và các dẫn xuất của nó thể hiện nhiều hoạt tính sinh học đáng chú ý, như hoạt tính chống ung thư [4,5], kháng khuẩn [6], kháng nấm [7], chống co giật [8], chống lao [9], kháng HIV [10], chống oxy hoá [11,12], chống viêm [13,14], gây tê [14], chống trầm cảm [15],… Các dẫn xuất của dị vòng 1,2,3-triazole được sử dụng rộng rãi trong chữa bệnh, và hiện nay, việc nghiên cứu tổng hợp và thăm dò hoạt tính sinh học của chúng là một trong những lĩnh vực quan trọng nhất trong nghiên cứu và phát triển thuốc [16,17]. Việc kết nối (hóa học click) giữa vòng isatin có nhóm thế azido và hợp phần đường có mang nửa 1-alkyne thông qua vòng 1,2,3-triazole có thể mang lại các hoạt tính sinh học đáng chú ý cho các phân tử đích [18].…”

Section: Mở đầU *unclassified

Góp phần nghiên cứu tổng hợp một số N-(ω-azidoalkyl)isatin thế từ các isatin thế và không thế

Thành

Trí²,

Toán³

et al. 2022

NST

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Tóm tắt: Các dẫn xuất azide của isatin là các chất đầu cần thiết cho phản ứng click để tạo ra dị vòng 1,2,3-triazole. Các dẫn xuất N-(ω-bromoalkyl)isatin cần cho chuyển hoá được tổng hợp từ phản ứng thế nucleophile của các isatin tương ứng với các dibromoalkane thích hợp. Một số N-(ω-azidoalkyl)isatin có chứa nhóm thế hoặc không thế ở vòng benzene đã được tổng hợp bằng phản ứng của các N-(ω-bromoalkyl)isatin tương ứng đã tổng hợp được với natri azide. Phản ứng được thực hiện trong DMF khan với sự có mặt của KI với vai trò chất xúc tiến. Hiệu suất sản phẩm đạt được 30−85%. Abstract: Azide derivatives of isatins were the needed initial materials for click chemistry in order to form 1,2,3-triazoles. N-(ω-Bromoalkyl)isatins were prepared by nucleophilic reaction of (un)substituted isatins with appropriate dibromoalkanes. Some ω-azidoalkylisatins were synthesized by reaction of corresponding ω-bromoalkylisatins with sodium azide. The reactions were performed in dry DMF as solvent in the presence of KI as promotive agent. Product yields achived 30−85%.

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“…In the continuous effort of our research group to develop potential drug candidates for cancer, [20,21] we utilized the isatin scaffold to synthesize various Schiff bases. Isatin-based Schiff bases are reported for diverse pharmacological properties such as analgesic, [22,23] anti-inflammatory, [24][25][26] antimicrobial, [27][28][29] antioxidant, [30][31][32][33] anticonvulsant, [34][35][36] and most predominantly, anticancer [37][38][39][40] properties. In addition, reported studies of isatin Schiff bases as VEGFR-2 inhibitors are encouraging.…”

Section: Introductionmentioning

confidence: 99%

Development of Isatin‐Based Schiff Bases Targeting VEGFR‐2 Inhibition: Synthesis, Characterization, Antiproliferative Properties, and QSAR Studies

Seliem

Panda

Girgis³

et al. 2022

ChemMedChem

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Three sets of isatin-based Schiff bases were synthesized utilizing the molecular hybridization approach. Some of the synthesized Schiff bases show significant to moderate antiproliferative properties against MCF7 (breast), HCT116 (colon), and PaCa2 (pancreatic) cancer cell lines with potency compared to reference drugs 5-fluorouracil (5-FU) and Sunitinib. Among all, compound 17 f-5-methylindolin-2-one) exhibits promising antiproliferative properties against the MCF7 cancer cell line with 2.1-fold more potency than Sunitinib. However, among all the synthesized compounds, three (5-methylisatin derivatives) were the most effective against HCT116 in comparison to 5-FU. Compound 17 f exhibited the highest anti-angiogenic effect on the vasculature as it significantly reduced BV from 43 mm to 2 mm in comparison to 5.7 mm for Sunitinib and flow cytometry supports the arrest of the cell cycle at G1/S phases. In addition, compound 17 f also showed high VEGFR-2 inhibition properties against breast cancer cell lines. Robust 2D-QSAR studies supported the biological data.

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Design and synthesis of novel isatin derivatives as potent analgesic, anti-inflammatory and antimicrobial agents

Cited by 19 publications

References 25 publications

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Therapeutic Outcomes of Isatin and Its Derivatives against Multiple Diseases: Recent Developments in Drug Discovery

Góp phần nghiên cứu tổng hợp một số N-(ω-azidoalkyl)isatin thế từ các isatin thế và không thế

Development of Isatin‐Based Schiff Bases Targeting VEGFR‐2 Inhibition: Synthesis, Characterization, Antiproliferative Properties, and QSAR Studies

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