TLC data in QSAR assay of thiazole and benzothiazole derivatives with H1-antihistamine activity. Part 1

2003 ◽  
Vol 16 (6) ◽  
pp. 451-457 ◽  
Author(s):  
Elżbieta Brzezińska ◽  
Grażyna Kośka
2020 ◽  
Vol 11 (3) ◽  
pp. 3309-3315
Author(s):  
Manahil B Elamin ◽  
Amani Abd Elrazig Salman Abd Elaziz ◽  
Emad Mohamed Abdallah

Heterocyclic chemistry has provided an inexhaustible source of pharmaceutical molecules. Heterocyclic compounds such as benzothiazole moieties and its derivatives area substantial class of compounds in pharmaceutical chemistry and exhibited therapeutic capabilities, such as antitumor, anticancer, antioxidant, antidiabetic, antiviral, antimicrobial, antimalarial, anthelmintic and other activities. Besides, some antibiotics such as penicillin and cephalosporin have heterocyclic moiety. The growing prevalence of multi-drug resistant pathogens represents serious global concern,which requires the development of new antimicrobial drugs. Moreover, the emergence of pandemic SARSCoV-2 causing Covid-19 disease and all these health dilemmas urge the scientific community to examine the possible antimicrobial and antiviral capacities of some bioactive benzothiazole derivatives against these severe causative agents.This mini-review highlights some recent scientific literature on different benzothiazole molecules and their derivatives. It turns out that, there are numerous synthesized benzothiazole derivatives which exhibited different mode of actions against microorganisms or viruses and accordingly suggested them as an active candidate in the discovery of new antimicrobial or antiviral agents for clinical development. The recommended bioactive benzothiazole derivatives mentioned in the current study are mainly Schiff bases, azo dyes and metal complexes benzothiazole derivatives; the starting material for most of these derivatives are 2-aminobenzothiazole although careful pharmaceutical studies should be conducted to ensure the safety and efficacy of these bioactive synthesized molecules as an antimicrobial or antiviral drug in the future.


2017 ◽  
Vol 17 (8) ◽  
pp. 721-726 ◽  
Author(s):  
Abbas Ahmadi ◽  
Mohsen Khalili ◽  
Lida Sohrabi ◽  
Nazanin Delzendeh ◽  
Babak Nahri-Niknafs ◽  
...  

2015 ◽  
Vol 12 (3) ◽  
pp. 197-204 ◽  
Author(s):  
Prabhakar Rairala ◽  
Bandi Yadagiri ◽  
Rajashaker Bantu ◽  
Vijayacharan Guguloth ◽  
Lingaiah Nagarapu

2018 ◽  
Vol 16 (1) ◽  
pp. 34-39
Author(s):  
Yao-Wei Li ◽  
Pei-Ming Zhang ◽  
Rui Li ◽  
Yan Bai ◽  
Yu Yu ◽  
...  

CDI combined with CH3SO3H was found to be highly effective for the cyclization of 2-aminothiophenol derivatives with carboxylic acids under MW condition. Fourteen benzothiazole derivatives were synthesized in good yield and their structures were characterized by 1H-NMR, 13CNMR, IR and mass spectrometry. This simple, rapid synthetic method is believed to provide a useful process for the synthesis of 2-substituted benzothiazole compounds.


1988 ◽  
Vol 53 (8) ◽  
pp. 1806-1811 ◽  
Author(s):  
Zdeněk Polívka ◽  
Jan Metyš ◽  
Miroslav Protiva

Reactions of 11-chloro-6,11-dihydrodibenzo[b,e]thiepin and its 2-methyl derivative, and further of the methanesulfonates of 2-chloro- and 2-bromo-6,11-dihydrodibenzo[b,e]thiepin-11-ol with 3-quinuclidinol afforded the title ethers I-IV. The 2-methyl compound II (VÚFB-17 088) showed significant antihistamine activity and the 2-chloro compound III (VÚFB-17 089), having antireserpine and anticataleptic activity, proved a potential antidepressant agent.


Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 695
Author(s):  
Nur Zahirah Abd Rani ◽  
Kok Wai Lam ◽  
Juriyati Jalil ◽  
Hazni Falina Mohamad ◽  
Mohd Shukri Mat Ali ◽  
...  

Phyllanthus amarus Schum. & Thonn. (Phyllanthaceae) is a medicinal plant that is commonly used to treat diseases such as asthma, diabetes, and anemia. This study aimed to examine the antiallergic activity of P. amarus extract and its compounds. The antiallergic activity was determined by measuring the concentration of allergy markers release from rat basophilic leukemia (RBL-2H3) cells with ketotifen fumarate as the positive control. As a result, P. amarus did not stabilize mast cell degranulation but exhibited antihistamine activity. The antihistamine activity was evaluated by conducting a competition radioligand binding assay on the histamine 1 receptor (H1R). Four compounds were identified from the high performance liquid chromatography (HPLC) analysis which were phyllanthin (1), hypophyllanthin (2), niranthin (3), and corilagin (4). To gain insights into the binding interactions of the most active compound hypophyllanthin (2), molecular docking was conducted and found that hypophyllanthin (2) exhibited favorable binding in the H1R binding site. In conclusion, P. amarus and hypophyllanthin (2) could potentially exhibit antiallergic activity by preventing the activation of the H1 receptor.


Sign in / Sign up

Export Citation Format

Share Document