Design, synthesis and biological evaluation of 6-aryl-1,6-dihydro-1,3,5-triazine-2,4-diamines as antiplasmodial antifolates

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

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Design, Synthesis and Biological Evaluation of (2′,5′ and 3′5′-Linked) cGAMP Analogs that Activate Stimulator of Interferon Genes (STING)

Molecules ◽

10.3390/molecules25225285 ◽

2020 ◽

Vol 25 (22) ◽

pp. 5285

Author(s):

Xin Xie ◽

Junyi Liu ◽

Xiaowei Wang

Keyword(s):

Transmembrane Protein ◽

Biological Evaluation ◽

Type I ◽

Vaccine Adjuvants ◽

One Pot ◽

Design Synthesis ◽

Cellular Assays ◽

Type I Ifns ◽

Sting Pathway

Stimulator of interferon genes (STING) is an endoplasmic reticulum adaptor transmembrane protein that plays a pivotal role in innate immune system. STING agonists, such as endogenous cyclic dinucleotide (CDN) cyclic GMP-AMP (cGAMP), have been used in diverse clinical research for immunogenic tumor clearance, antiviral treatments and vaccine adjuvants. CDNs containing noncanonical mixed 3′-5′ and 2′-5′ phosphodiester linkages show higher potency in the activation of the STING pathway. In this study, a series of 2′3′-CDNs were designed and synthesized through a modified one-pot strategy. We then established a surface plasmon resonance (SPR)-based binding assay to quantify the binding affinities of synthesized CDNs for human STING, which requested a minuscule amount of sample without any pretreatment. Using this assay, we identified compound 8d (KD = 0.038 μM), a novel CDN that showed higher binding affinity with hSTING than cGAMP (KD = 0.543 μM). Cellular assays confirmed that 8d could trigger the expression of type I IFNs and other proinflammatory cytokines more robust than cGAMP. 8d also exhibited more resistant than cGAMP to enzymatic cleavage in vitro, indicating the successful improvement in drug availability. These findings provide guidelines for the design and structural optimization of CDNs as STING agonists.

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Design, synthesis, and biological evaluation of new series of 2-amido-1,3,4-thiadiazole derivatives as cytotoxic agents

Zeitschrift für Naturforschung B ◽

10.1515/znb-2015-0138 ◽

2016 ◽

Vol 71 (3) ◽

pp. 205-210 ◽

Cited By ~ 3

Author(s):

Ali Almasirad ◽

Loghman Firoozpour ◽

Maliheh Nejati ◽

Najmeh Edraki ◽

Omidreza Firuzi ◽

...

Keyword(s):

Human Tumor ◽

Inhibitory Effect ◽

Biological Evaluation ◽

Cytotoxic Agents ◽

Antitumor Activities ◽

Design Synthesis ◽

Ethidium Bromide Staining ◽

Thiadiazole Derivatives ◽

Synthesis And Biological Evaluation

AbstractA series of novel 1,3,4-thiadiazole derivatives bearing an amide moiety were designed, synthesized, and evaluated for their in vitro antitumor activities against HL-60, SKOV-3 and MOLT-4 human tumor cell lines by MTT assay. Ethyl 2-((5-(4-methoxybenzamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5f) showed the best inhibitory effect against SKOV-3 cells, with an IC50 value of 19.5 μm. In addition, the acridine orange/ethidium bromide staining assay in SKOV-3 cells suggested that the cytotoxic activity of 5f occurs via apoptosis.

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Design, synthesis and biological evaluation of N-oxide derivatives with potent in vivo antileishmanial activity

PLoS ONE ◽

10.1371/journal.pone.0259008 ◽

2021 ◽

Vol 16 (11) ◽

pp. e0259008

Author(s):

Leandro da Costa Clementino ◽

Guilherme Felipe Santos Fernandes ◽

Igor Muccilo Prokopczyk ◽

Wilquer Castro Laurindo ◽

Danyelle Toyama ◽

...

Keyword(s):

Parasite Burden ◽

Peritoneal Macrophages ◽

Biological Evaluation ◽

Antileishmanial Activity ◽

Dual Effect ◽

Design Synthesis ◽

Murine Peritoneal Macrophages ◽

Synthesis And Biological Evaluation

Leishmaniasis is a neglected disease that affects 12 million people living mainly in developing countries. Herein, 24 new N-oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antileishmanial activity. Compound 4f, a furoxan derivative, was particularly remarkable in this regard, with EC50 value of 3.6 μM against L. infantum amastigote forms and CC50 value superior to 500 μM against murine peritoneal macrophages. In vitro studies suggested that 4f may act by a dual effect, by releasing nitric oxide after biotransformation and by inhibiting cysteine protease CPB (IC50: 4.5 μM). In vivo studies using an acute model of infection showed that compound 4f at 7.7 mg/Kg reduced ~90% of parasite burden in the liver and spleen of L. infantum-infected BALB/c mice. Altogether, these outcomes highlight furoxan 4f as a promising compound for further evaluation as an antileishmanial agent.

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Design, synthesis, and biological evaluation of glycine-based molecular tongs as inhibitors of Aβ1–40 aggregation in vitro

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2008.03.052 ◽

2008 ◽

Vol 16 (9) ◽

pp. 4810-4822 ◽

Cited By ~ 18

Author(s):

Saverio Cellamare ◽

Angela Stefanachi ◽

Diana A. Stolfa ◽

Teodora Basile ◽

Marco Catto ◽

...

Keyword(s):

Biological Evaluation ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of (1,3-diphenyl-1H-pyrazol-4-yl) methyl benzoate derivatives as potential BRAFV600E inhibitors

RSC Advances ◽

10.1039/c4ra08708a ◽

2014 ◽

Vol 4 (95) ◽

pp. 52702-52711 ◽

Cited By ~ 4

Author(s):

Ya-Juan Qin ◽

Man Xing ◽

Ya-Liang Zhang ◽

Jigar A. Makawana ◽

Ai-Qin Jiang ◽

...

Keyword(s):

Inhibitory Activity ◽

Biological Evaluation ◽

Methyl Benzoate ◽

Design Synthesis ◽

Synthesis And Biological Evaluation ◽

Potent Inhibitory Activity ◽

Benzoate Derivatives

A series of (1,3-diphenyl-1H-pyrazol-4-yl) methyl benzoate derivatives (6a–10d) were designed and synthesized and evaluated as BRAFV600 inhibitors. Among them, compound 10a showed the most potent inhibitory activity against A375, WM266.4 and BRAFV600Ein vitro with IC50 values of 1.36 μM, 0.94 μM and 0.11 μM, respectively.

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Design, synthesis and biological evaluation of novel unsymmetrical azines as quorum sensing inhibitors

RSC Advances ◽

10.1039/c5ra12925g ◽

2015 ◽

Vol 5 (97) ◽

pp. 80027-80038 ◽

Cited By ~ 14

Author(s):

Sumit S. Chourasiya ◽

Deepika Kathuria ◽

Shaminder Singh ◽

Vijay C. Sonawane ◽

Asit K. Chakraborti ◽

...

Keyword(s):

Quorum Sensing ◽

Biological Evaluation ◽

One Pot ◽

Design Synthesis ◽

Quorum Sensing Inhibitors ◽

Synthesis And Biological Evaluation

In this report, novel unsymmetrical azines have been designed and synthesised by using one pot approach. Further, they were evaluated as quorum sensing inhibitors.

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