Benzylaminoethylureido‐Tailed Benzenesulfonamides Show Potent Inhibitory Activity against Bacterial Carbonic Anhydrases

ChemMedChem ◽  
2020 ◽  
Vol 15 (24) ◽  
pp. 2444-2447
Author(s):  
Majid Ali ◽  
Andrea Angeli ◽  
Murat Bozdag ◽  
Fabrizio Carta ◽  
Clemente Capasso ◽  
...  
2017 ◽  
Vol 75 ◽  
pp. 170-172 ◽  
Author(s):  
Andrea Angeli ◽  
Ghulam Abbas ◽  
Sonia Del Prete ◽  
Fabrizio Carta ◽  
Clemente Capasso ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3580 ◽  
Author(s):  
Kartsev ◽  
Geronikaki ◽  
Bua ◽  
Nocentini ◽  
Petrou ◽  
...  

Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the fundamental reaction of CO2 hydration in all living organisms and are actively involved in the regulation of a plethora of pathological and physiological conditions. A set of new coumarin/ dihydrocoumarin derivatives was here synthesized, characterized, and tested as human CA inhibitors. Their inhibitory activity was evaluated against the cytosolic human isoforms hCA I and II and the transmembrane hCA IX and hCA XII. Two compounds showed potent inhibitory activity against hCA IX, being more active or equipotent with the reference drug acetazolamide. Computational procedures were used to investigate the binding mode of this class of compounds within the active site of hCA IX and XII that are validated as anti-tumor targets.


2009 ◽  
Vol 19 (5) ◽  
pp. 1371-1375 ◽  
Author(s):  
Letizia Crocetti ◽  
Alfonso Maresca ◽  
Claudia Temperini ◽  
Rebecca A. Hall ◽  
Andrea Scozzafava ◽  
...  

Author(s):  
Andri Frediansyah ◽  
Jan Straetener ◽  
Heike Brötz-Oesterhelt ◽  
Harald Gross

AbstractA cyclic tetrapeptide, designated massiliamide, was isolated from the liquid culture of the Gram-negative bacterium Massilia albidiflava DSM 17472T. The structure was elucidated through extensive spectroscopic analysis, including HR-MS and 1D and 2D NMR experiments. The absolute configuration was determined using the Marfey´s method. Massiliamide showed potent inhibitory activity towards tyrosinase with an IC50 value of 1.15 µM and no cytotoxicity.


2021 ◽  
Vol 22 (11) ◽  
pp. 5482
Author(s):  
Zuo-Peng Zhang ◽  
Ye Zhong ◽  
Zhen-Bin Han ◽  
Lin Zhou ◽  
Hua-Sheng Su ◽  
...  

A series of saccharide-modified thiadiazole sulfonamide derivatives has been designed and synthesized by the “tail approach” and evaluated for inhibitory activity against carbonic anhydrases II, IX, and XII. Most of the compounds showed high topological polar surface area (TPSA) values and excellent enzyme inhibitory activity. The impacts of some compounds on the viability of HT-29, MDA-MB-231, and MG-63 human cancer cell lines were examined under both normoxic and hypoxic conditions, and they showed certain inhibitory effects on cell viability. Moreover, it was found that the series of compounds had the ability to raise the pH of the tumor cell microenvironment. All the results proved that saccharide-modified thiadiazole sulfonamides have important research prospects for the development of CA IX inhibitors.


RSC Advances ◽  
2014 ◽  
Vol 4 (97) ◽  
pp. 54217-54225 ◽  
Author(s):  
Xin Zhang ◽  
Chetan B. Sangani ◽  
Li-Xin Jia ◽  
Pi-Xian Gong ◽  
Fang Wang ◽  
...  

Series of novel Schiff's base derivatives have been synthesized. Compound 10q showed the most potent inhibitory activity (IC50 = 2.6883 μM).


INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 24-28
Author(s):  
A.A Rege ◽  
◽  
A. S Chowdhary

Aqueous extracts of Ocimum sanctum Linn., Tinospora cordifolia (Willd.) Miers ex Hook. f. & Thoms, Withania somnifera Dunal, Avicennia officinalis Linn. and Rhizophora mucronata Lam. were included for the present in vitro study. Pepsin was used as a substitute for HIV-protease to evaluate inhibitory activity of these extracts, as pepsin has close resemblance with HIV-protease in proteolytic activity. O. sanctum revealed the highest inhibitory activity followed by R. mucronata. In our earlier study, O. sanctum and R. mucronata exerted anti-HIV activity via multiple mechanisms of action; viz., interference with the gp120 / CD4 interaction and inhibition of HIV-reverse transcriptase. In the present study, they also showed potent inhibitory activity against pepsin enzyme (indirectly against HIV-protease) which may be due their flavonoids content.


2015 ◽  
Vol 10 (1) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Nilubon Sornkaew ◽  
Yuan Lin ◽  
Fei Wang ◽  
Guolin Zhang ◽  
Ratchanaporn Chokchaisiri ◽  
...  

Eight new diarylheptanoids, a 1.2:1 mixture of (3S)- and (3 R)-1-(4-hydroxyphenyl)-7-phenyl-(4 E,6 E)-4,6-heptadien-3-ol (1a and 1b), a racemic mixture of (3S)- and (3 R)-1-(4-hydroxyphenyl)-3-methoxy-7-phenyl-(4 E,6 E)-4,6-heptadiene (2a and 2b), a ca. 1:1 mixture of (3S)- and (3 R)-1-(4-hydroxy-3-methoxyphenyl)-3-methoxy-7-phenyl)-(4 E,6 E)-4,6-heptadiene (3a and 3b), 3-acetoxy-1-(3,4-dihydroxyphenyl)-7-phenylheptan-5-ol (4), (3 R)-1-(4,5-dihydroxyphenyl)-7-phenyl-(6 E)-6-hepten-3,2′-epoxide (5), and thirteen known diarylheptanoids, 6-12, a 3:1 mixture of 13a and 13b, and 14-17, were isolated from the rhizomes of Curcuma comosa from Sakon Nakhon, northeastern part of Thailand. The isolated compounds were evaluated for their antiinflammatory activities on the inhibition of lipopolysaccharide-induced nitric oxide production in macrophage RAW 264.7 cells and the diarylheptanoids 1a and 1b mixture and 14 exhibited potent inhibitory activity.


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