scholarly journals Synthesis and Biological Evaluation of 2-Hydroxy-3-[(2-aryloxyethyl)amino]propyl 4-[(Alkoxycarbonyl)amino]benzoates

2013 ◽  
Vol 2013 ◽  
pp. 1-13 ◽  
Author(s):  
Jan Tengler ◽  
Iva Kapustíková ◽  
Matúš Peško ◽  
Rodney Govender ◽  
Stanislava Keltošová ◽  
...  
Keyword(s):  
Electron Transport ◽  
Conformational Changes ◽  
Spinacia Oleracea ◽  
Photosynthetic Electron Transport ◽  
Thylakoid Membranes ◽  
Biological Evaluation ◽  
Mycobacterial Species ◽  
Monocytic Leukaemia ◽  
Synthesis And Biological Evaluation

A series of twenty substituted 2-hydroxy-3-[(2-aryloxyethyl)amino]propyl 4-[(alkoxycarbonyl)amino]benzoates were prepared and characterized. As similar compounds have been described as potential antimycobacterials, primaryin vitroscreening of the synthesized carbamates was also performed against two mycobacterial species. 2-Hydroxy-3-[2-(2,6-dimethoxyphenoxy)ethylamino]-propyl 4-(butoxycarbonylamino)benzoate hydrochloride, 2-hydroxy-3-[2-(4-methoxyphenoxy)ethylamino]-propyl 4-(butoxycarbonylamino)benzoate hydrochloride, and 2-hydroxy-3-[2-(2-methoxyphenoxy)ethylamino]-propyl 4-(butoxycarbonylamino)benzoate hydrochloride showed higher activity againstM. aviumsubsp.paratuberculosisandM. intracellularethan the standards ciprofloxacin, isoniazid, or pyrazinamide. Cytotoxicity assay of effective compounds was performed using the human monocytic leukaemia THP-1 cell line. Compounds with predicted amphiphilic properties were also tested for their effects on the rate of photosynthetic electron transport (PET) in spinach (Spinacia oleraceaL.) chloroplasts. All butyl derivatives significantly stimulated the rate of PET, indicating that the compounds can induce conformational changes in thylakoid membranes resulting in an increase of their permeability and so causing uncoupling of phosphorylation from electron transport.

Regulation of photosystem II by metabolic and environmental factors

1989 ◽  
Vol 323 (1216) ◽  
pp. 269-279 ◽  
Keyword(s):  
Electron Transport ◽  
Higher Plants ◽  
Photosynthetic Electron Transport ◽  
Thylakoid Membranes ◽  
Internal Factors ◽  
Regulatory Processes ◽  
Quenching Analysis ◽  
Intact Chloroplasts ◽  
Rate Of Dissipation

The thylakoid membranes of higher plants possess several mechanisms that control both the distribution and rate of dissipation of absorbed light. These mechanisms, which allow regulation of photosynthetic electron transport in response to alteration in external and internal factors, can be observed as the various processes that quench chlorophyll fluorescence. By using the 'light-doubling techniques’, together with analysis of quenching relaxation, it is possible to assess quantitatively the extents of these regulatory processes and to allow their interrelations to be studied. These techniques can be applied to in vitro systems or to leaves, and can be particularly useful when applied with electron-transport measurements and when models are used to aid interpretation. Results of quenching analysis at different light intensities in isolated thylakoids, intact chloroplasts, protoplasts, algae and leaves of a variety of species are presented.

Synthesis and Biological Evaluation of (E)-3-(Nitrophenyl)-1-(pyrazin-2-yl)prop-2-en-1-ones

2006 ◽  
Vol 71 (1) ◽  
pp. 44-58 ◽  
Author(s):  
Veronika Opletalová ◽  
Milan Pour ◽  
Jiří Kuneš ◽  
Vladimír Buchta ◽  
Luís Silva ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Photosynthetic Electron Transport ◽  
Trichophyton Mentagrophytes ◽  
Antimycobacterial Activity ◽  
Biological Evaluation ◽  
Inhibiting Activity ◽  
High Potency ◽  
Nitro Derivatives ◽  
Synthesis And Biological Evaluation

The title (E)-(3-nitrophenyl)-1-(pyrazin-2-yl)prop-2-en-1-ones were prepared by the Claisen- Schmidt condensation of acetylpyrazines and 2-nitro-, 3-nitro- and 4-nitrobenzaldehyde in pyridine using diethylamine as the catalyst. The compounds were bioassayed for in vitro antifungal, antimycobacterial and photosynthesis-inhibiting activity. The high potency of (E)-1-(5-tert-butylpyrazin-2-yl)-3-(4-nitrophenyl)prop-2-en-1-one againstMycobacterium tuberculosis(MIC 0.78 μg/ml) and moderate activities of several compounds againstTrichophyton mentagrophytesandCandidaspp. do not support the assumption that phenolic groups are essential for antimycobacterial and antifungal activity of chalcones and their analogues. In fact, the nitro-substituted compounds were superior to the previously described hydroxylated congeners with antimycobacterial activity (MIC ≥ 12.5 μg/ml). The compounds also reduced chlorophyll content in green algaChlorella vulgaris, and some of them inhibited photosynthetic electron transport in spinach chloroplasts as well. The photosynthesis-inhibiting activity of nitro derivatives was lower than that of the corresponding hydroxylated analogues.

Hybrid Design of Isonicotinic Acid Hydrazide Derivatives: Machine Learning Studies, Synthesis and Biological Evaluation of their Antituberculosis Activity

2020 ◽  
Vol 17 (3) ◽  
pp. 365-375
Author(s):  
Vasyl Kovalishyn ◽  
Diana Hodyna ◽  
Vitaliy O. Sinenko ◽  
Volodymyr Blagodatny ◽  
Ivan Semenyuta ◽  
...  
Keyword(s):  
Machine Learning ◽  
Isonicotinic Acid ◽  
Acid Hydrazide ◽  
Predictive Ability ◽  
Antitubercular Activity ◽  
Biological Evaluation ◽  
Starting Point ◽  
Binary Classifiers ◽  
Synthesis And Biological Evaluation

Background: Tuberculosis (TB) is an infection disease caused by Mycobacterium tuberculosis (Mtb) bacteria. One of the main causes of mortality from TB is the problem of Mtb resistance to known drugs. Objective: The goal of this work is to identify potent small molecule anti-TB agents by machine learning, synthesis and biological evaluation. Methods: The On-line Chemical Database and Modeling Environment (OCHEM) was used to build predictive machine learning models. Seven compounds were synthesized and tested in vitro for their antitubercular activity against H37Rv and resistant Mtb strains. Results: A set of predictive models was built with OCHEM based on a set of previously synthesized isoniazid (INH) derivatives containing a thiazole core and tested against Mtb. The predictive ability of the models was tested by a 5-fold cross-validation, and resulted in balanced accuracies (BA) of 61–78% for the binary classifiers. Test set validation showed that the models could be instrumental in predicting anti- TB activity with a reasonable accuracy (with BA = 67–79 %) within the applicability domain. Seven designed compounds were synthesized and demonstrated activity against both the H37Rv and multidrugresistant (MDR) Mtb strains resistant to rifampicin and isoniazid. According to the acute toxicity evaluation in Daphnia magna neonates, six compounds were classified as moderately toxic (LD50 in the range of 10−100 mg/L) and one as practically harmless (LD50 in the range of 100−1000 mg/L). Conclusion: The newly identified compounds may represent a starting point for further development of therapies against Mtb. The developed models are available online at OCHEM http://ochem.eu/article/11 1066 and can be used to virtually screen for potential compounds with anti-TB activity.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

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.

Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  
Keyword(s):  
Cell Lines ◽  
A549 Cells ◽  
Positive Control ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Pyrimidine Derivatives ◽  
Concentration Dependent Manner ◽  
Ic50 Value ◽  
Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

Glyphosate Does Not Inhibit Photosynthetic Electron Transport and Phosphorylation in Pea (Pisum sativum) Chloroplasts

Weed Science ◽  
1979 ◽  
Vol 27 (6) ◽  
pp. 684-688 ◽  
Author(s):  
E. P. Richard ◽  
J. R. Goss ◽  
C. J. Arntzen
Keyword(s):  
Electron Transport ◽  
Pisum Sativum ◽  
Photosynthetic Electron Transport ◽  
Photochemical Reactions ◽  
Transport Processes ◽  
Ps Ii ◽  
Dark Incubation ◽  
Fluorescence Studies ◽  
Mixture Prior

The activity of glyphosate [N-(phosphonomethyl)glycine], formulated as the isopropylamine salt, on in vitro photosynthesis was investigated. When pH 4.7 glyphosate solutions were titrated to a pH equal to that of the reaction media (pH 7.8), glyphosate additions had no effect on whole chain electron transport between coupled photosystem II (PS II) and photosystem I (PS I) in stroma-free chloroplast thylakoids from peas (Pisum sativumL. ‘Morse's Progress No. 9′). Inhibition did not occur even after a 2-h dark incubation of lamellae in a 5-mM solution of glyphosate. Fluorescence studies failed to detect an effect of glyphosate on PS-II mediated electron transport processes or upon light harvesting properties of PS II even after a 2-h glyphosate/chloroplast preincubation. Glyphosate had no effect on cyclic and noncyclic photophosphorylation even after a 100-min dark incubation of chloroplast membranes in a 5-mM solution of glyphosate. Based on these assays it is concluded that glyphosate has no direct effect on the photochemical reactions of photosynthesis when the pH of the active compound is adjusted to that of the reaction mixture prior to addition to a chloroplast suspension.

scholarly journals Synthesis and Biological Evaluation of O-[3-18F-fluoropropyl]-α-methyl Tyrosine in Mesothelioma-Bearing Rodents

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
I-Hong Shih ◽  
Fan-Lin Kong ◽  
Mohammad S. Ali ◽  
Yinhan Zhang ◽  
Dong-Fang Yu ◽  
...  
Keyword(s):  
Radiochemical Purity ◽  
Biological Evaluation ◽  
Synthesis Methods ◽  
Automated Synthesis ◽  
Imaging Studies ◽  
Biodistribution Studies ◽  
Synthesis And Biological Evaluation ◽  
Automated Methods

Radiolabeled tyrosine analogs enter cancer cells via upregulated amino acid transporter system and have been shown to be superior to18F-fluoro-2-deoxy-D-glucose (18F-FDG) in differential diagnosis in cancers. In this study, we synthesized O-[3-19F-fluoropropyl]-α-methyl tyrosine (19F-FPAMT) and used manual and automated methods to synthesize O-[3-18F-fluoropropyl]-α-methyl tyrosine (18F-FPAMT) in three steps: nucleophilic substitution, deprotection of butoxycarbonyl, and deesterification. Manual and automated synthesis methods produced18F-FPAMT with a radiochemical purity >96%. The decay-corrected yield of18F-FPAMT by manual synthesis was 34% at end-of-synthesis (88 min). The decay-corrected yield of18F-FPAMT by automated synthesis was 15% at end-of-synthesis (110 min).18F-FDG and18F-FPAMT were used forin vitroandin vivostudies to evaluate the feasibility of18F-FPAMT for imaging rat mesothelioma (IL-45).In vitrostudies comparing18F-FPAMT with18F-FDG revealed that18F-FDG had higher uptake than that of18F-FPAMT, and the uptake ratio of18F-FPAMT reached the plateau after being incubated for 60 min. Biodistribution studies revealed that the accumulation of18F-FPAMT in the heart, lungs, thyroid, spleen, and brain was significantly lower than that of18F-FDG. There was poor bone uptake in18F-FPAMT for up to 3 hrs suggesting itsin vivostability. The imaging studies showed good visualization of tumors with18F-FPAMT. Together, these results suggest that18F-FPAMT can be successfully synthesized and has great potential in mesothelioma imaging.

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