ChemInform Abstract: Design and Synthesis of Anticonvulsive Agents as γ-Vinyl GABA-Based Potential Dual Acting Prodrugs and Their Biological Activities.

ChemInform ◽  
2010 ◽  
Vol 31 (28) ◽  
pp. no-no
Author(s):  
Eung-Seok Lee ◽  
et al. et al.
Keyword(s):  
Biological Activities ◽  
Design And Synthesis ◽  
Anticonvulsive Agents

Design and synthesis of anticonvulsive agents as γ-vinyl GABA-based potential dual acting prodrugs and their biological activities

2000 ◽  
Vol 10 (7) ◽  
pp. 609-613 ◽  
Author(s):  
Yong-chul Kim ◽  
Long-Xuan Zhao ◽  
Tae-Hyung Kim ◽  
Sun-mi Je ◽  
Eun-kyung Kim ◽  
...  
Keyword(s):  
Biological Activities ◽  
Design And Synthesis ◽  
Anticonvulsive Agents

scholarly journals Design and synthesis of multi-target directed 1,2,3-triazole-dimethylaminoacryloyl-chromenone derivatives with potential use in Alzheimer's disease

BMC Chemistry ◽  
2020 ◽  
Vol 14 (1) ◽  
Author(s):  
Hajar Karimi Askarani ◽  
Aida Iraji ◽  
Arezoo Rastegari ◽  
Syed Nasir Abbas Bukhari ◽  
Omidreza Firuzi ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Biological Activities ◽  
Neuroprotective Effects ◽  
Design And Synthesis ◽  
Catalytic Active Site ◽  
Aβ Aggregation ◽  
Multifunctional Agents ◽  
Potential Use

Abstract To discover multifunctional agents for the treatment of Alzheimer's disease (AD), a new series of 1,2,3-triazole-chromenone derivatives were designed and synthesized based on the multi target-directed ligands approach. The in vitro biological activities included acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition as well as anti-Aβ aggregation, neuroprotective effects, and metal-chelating properties. The results indicated a highly selective BuChE inhibitory activity with an IC50 value of 21.71 μM for compound 10h as the most potent compound. Besides, compound 10h could inhibit self-induced Aβ1–42 aggregation and AChE-induced Aβ aggregation with 32.6% and 29.4% inhibition values, respectively. The Lineweaver–Burk plot and molecular modeling study showed that compound 10h targeted both the catalytic active site (CAS) and peripheral anionic site (PAS) of BuChE. It should be noted that compound 10h was able to chelate biometals. Thus, the designed scaffold could be considered as multifunctional agents in AD drug discovery developments.

scholarly journals DESIGN AND SYNTHESIS OF NOVEL 1-((DIMETHYLAMINO)METHYL)-3-(4-(3-(SUBSTITUTE DPHENYL)-4-OXOTHIAZOLIDIN-2-YL)PHENYLIMINO)-5-NITROINDOLIN-2-ONES AS POTENT ANTITUBERCULAR AGENTS

2019 ◽  
pp. 200-207
Author(s):  
KOSARAJU LAHARI ◽  
RAJA SUNDARARAJAN
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
Proton Nuclear Magnetic Resonance ◽  
Design And Synthesis ◽  
Group Variation

Objective: Isatins have emerged as antimicrobial agents due to their broad spectrum of in vitro and in vivo antimicrobial activities. In addition, thiazolidinone also reported to possess various biological activities particularly antimicrobial activity. Due to the importance, we planned to synthesize compounds with isatin functionality coupled with thiazolidinone as possible antitubercular and antimicrobial agents which could furnish better therapeutic results. Methods: In vitro Mycobacterium tuberculosis method and agar streak dilution test are used to estimate antitubercular and antimicrobial potency of title analogs, respectively. Minimum inhibitory concentration of entire title compounds was determined against all tested microorganism such as M. tuberculosis, four Gram-positive, three Gram-negative bacteria, and two fungi. Results: A series of new thiazolidinone substituted Schiff and Mannich bases of 5-nitroisatins were designed and synthesized by a multistep synthesis from isatin. Structures of synthesized compounds are characterized using Fourier-transform infrared, proton nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. Mild to good antitubercular and antimicrobial activity was showed by synthesized 5-nitroisatin analogs. The relationship between the biological activity and the functional group variation of the tested compounds was discussed. Conclusion: 3-(4-(3-(4-Aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethyl amino)methyl)-5-nitroindolin-2-one 6 and 3-(4-(3- (2-aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethylamino)methyl)-5-nitroindolin-2-one 13 were found to be the most potent compounds of this series which might be extended as a novel class of antimicrobial agents.

Design and Synthesis of Novel Thiosemicarbazones as Potent Anti-breast Cancer Agents

2019 ◽  
Vol 16 (4) ◽  
pp. 446-452 ◽  
Author(s):  
Mashooq Ahmad Bhat ◽  
M. Al-Tahhan ◽  
Mohamed A. Al-Omar ◽  
Ahmed M. Naglah ◽  
Abdullah Al-Dhfyan
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Side Population ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Inhibition Assay ◽  
Reference Drug ◽  
Design And Synthesis ◽  
Pure Compounds ◽  
Mcf 7

Background: Thiosemicarbazones and its derivatives received a great pharmaceutical importance due to their prominent biological activities. Methods: A series of disubstituted thiosemicarbazone derivatives (1-12) were designed and synthesized as pure compounds in good yield. All the synthesized compounds were analyzed by spectral data. The anticancer activity of all the compounds was performed against breast cancer MCF-7 and MDA-MB-231 cell lines. Results: Most of the compounds showed activity against breast cancer MCF-7 and MDA-MB-231 cell lines with (IC50 = 12.25 µM ‒ 185.35 µM) and (IC50 = 12.97 µM ‒ 107.33 µM), respectively. Compound 9 presented (IC50 = 12.76 µM and 12.97 µM) against MCF-7 and MDA-MB-231 cell lines, respectively. Conclusion: Compound 9, was found to exhibit significant anti-breast cancer activity. This compound was further evaluated for side population percent inhibition assay on the breast cancer cell line MCF-7 at 5 and 10 µM concentration. It showed superiority to block side population by more than 80% at 5 μM concentration compared to the reference drug verapamil.

scholarly journals Exploration of Newer Possibilities to the Synthesis of Diazepine and Quinoline Carboxylic Acid Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-8
Author(s):  
Vatsala Soni ◽  
Meenakshi Sharma ◽  
Anshu Agarwal ◽  
Dharma Kishore
Keyword(s):  
Carboxylic Acid ◽  
Drug Design ◽  
Spectral Data ◽  
Biological Activities ◽  
Design And Synthesis ◽  
Quinoline Carboxylic Acid ◽  
Quinoline Moiety ◽  
Molecular Framework

Heterocyclic systems containing benzothiazoles, carbazole (and azacarbazole) moieties have attracted the attention of chemists owing to these nuclei having been identified in the literature as most promising pharmacophores in drug design and synthesis. Based on these observations, it could be anticipated that incorporation of the bioactive azepine moiety and quinoline moiety into the molecular framework of benzothiazoles fused to carbazole (and azacarbazoles) could produce interesting series of compounds9–12with enhanced biological activities, whose structure was unequivocally established from its microanalyses and spectral data.

scholarly journals Synthesis and biological evaluation of heterocyclic 1,2,4-Triazole scaffolds as promising pharmacological agents

2020 ◽  
Author(s):  
Mukesh Kumari ◽  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Kalavathy Ramasamy ◽  
Siong Meng Lim ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pharmacological Agents ◽  
Drug Candidates ◽  
Design And Synthesis ◽  
Hct 116

Abstract Background: Triazole is an important heterocyclic moiety that occupied a unique position in heterocyclic chemistry, due to its large number of biological activities. It exists in two isomeric forms i.e. 1,2,4-triazole and 1,2,3-triazole and used as core molecule for the design and synthesis of many medicinal compounds. 1,2,4-Triazole possess broad spectrum of therapeutically interesting drug candidates such as analgesic, antiseptic, antimicrobial, antioxidant, antiurease , anti-inflammatory, diuretics, anticancer, anticonvulsant, antidiabetic, antimigrain agents.Methods: The structure of all synthesized compounds were characterized by physicochemical properties and spectral means (IR and NMR). The synthesized compounds were evaluated for their in vitro antimicrobial activity against Gram-positive (B. subtilis), Gram-negative (P. aeruginosa and E. coli) bacterial and fungal (C. albicans and A. niger) strains by tube dilution method using ciprofloxacin, amoxicillin and fluconazole as standards. In-vitro antioxidant and anti-urease screening was done by DPPH assay and indophenol method, respectively. The in-vitro anticancer evaluation was carried out against MCF-7 and HCT116 cancer cell lines using 5-FU and cisplatin as standards.Results, discussion and conclusion: The biological screening results reveal that the compounds T5 (MICBS, EC = 24.7µM, MICPA, CA = 12.3 µM) and T17 (MICAN = 27.1µM) exhibited potent antimicrobial activity as comparable to standards ciprofloxacin, amoxicillin (MICCipro = 18.1µM, MICAmo = 17.1µM) and fluconazole (MICFlu = 20.4µM), respectively. The antioxidant evaluation showed that compounds T2 (IC50 = 34.83 µg/ml) and T3 (IC50 = 34.38 µg/ml) showed significant antioxidant activity and comparable to ascorbic acid (IC50 = 35.44 µg/ml). Compounds T3 (IC50 = 54.01µg/ml) was the most potent urease inhibitor amongst the synthesized compounds and compared to standard thiourea (IC50 = 54.25 µg/ml). The most potent anticancer activity showed by compounds T2 (IC50 = 3.84 μM) and T7 (IC50 = 3.25 μM) against HCT 116 cell lines as compared to standard 5-FU (IC50 = 25.36 μM).

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