Synthesis, Characterization and Biological Evaluation of some Novel 2-Substituted Aminothiazoles

Author(s):  
Suresh Kumar ◽  
Renu Saharan ◽  
Randhir Singh

The synthesis of biologically active molecules carried out by using Aminothiazole nuclei and their various derivatives as precursors. In present work, Schiff's bases (27-36) were prepared by reacting amino group of thiazole moiety (26) with various aromatic aldehydes. The titled, novel 2-substituted aminothiazoles (37-46) were obtained by reaction of these Schiff's bases with benzil by providing excess amount of ammonium acetate (NH4OAc). Structure elucidation of all the newly synthesized compounds was carried out by employing elemental analysis, FT-IR, 1H NMR and Mass spectrometry. The newly synthesized novel 2-substituted-aminothiazoles were screened for their anti-bacterial activity against two gram +ve bacterial strains viz. Staphylococcus aureus and Bacillus subtilis and against a gram –ve bacterial strain viz. Escherichia coli and for anti-fungal activity against two fungal strains viz. Candida albicans and Aspergillus niger using cup plate method by using Norfloxacin and Fluconazole as standard drugs respectively. Cyto-toxic activity of the synthesized compounds was evaluated by determining the percentage growth inhibition of Daltonꞌs Lymphoma Ascites (DLA) cells and Erlichꞌs Ascites Carcinoma (EAC) cells by Tryphan Blue Dye Exclusion technique. Results of biological activity studies indicated that the newly synthesized 2-substituted aminothiazoles displayed good anti-bacterial activity against gram –ve bacterial strain Escherichia coli and anti-fungal activity against Candida albicans. Further, these compounds were found to show significant percent growth inhibition against DLA and EAC, cell-lines.

2005 ◽  
Vol 125 (1) ◽  
pp. 108-115 ◽  
Author(s):  
Belén López-García ◽  
Phillip H.A. Lee ◽  
Kenshi Yamasaki ◽  
Richard L. Gallo

2019 ◽  
Vol 6 (2) ◽  
pp. 107-114
Author(s):  
Rustam Musta ◽  
Laily Nurliana

Kinetic studies effectiveness clove leaf (Syzigium aromaticum) oil as antifungal Candida albicans have been done. The study have purpose to determine the reaction order, reaction constants (k) and relationship the concentration of clove leaf (Syzigium aromaticum) oil every time (At) with the initial concentration of of clove (Syzigium aromaticum) oil (Ao) and time (t) and equipped determination of the minimum concentration of clove leaf (Syzigium aromaticum)oil effective anti-fungus Candida albicans. The results shows the anti-fungal activity clove leaf (Syzigium aromaticum) oil on Candida albicans for each variation of the concentration 100%, 75%, 50% and 25% are 14.2 mm, 12.2 mm, 10.8 mm and 10.4 mm respectively. Reaction order as antifungal of the clove leaf (Syzigium aromaticum) oil on Candida albicans is 0.2112 with k = 5.0594. The minimum concentration of clove leaf (Syzigium aromaticum) oil as anti-fungal Candida albicans is 17.86%.


2021 ◽  
Vol 37 (2) ◽  
pp. 508-512
Author(s):  
Jaganmohana Rao Saketi ◽  
S N Murthy Boddapati ◽  
Raghuram M ◽  
Geetha Bhavani Koduru ◽  
Haribabu Bollikolla

The in vitroantimicrobial properties of a series of N-methyl-3-aryl indazoles (5a-5j) were screened. In this present work, we describe our efforts towards the development of potent antimicrobial activity of synthesized indazole derivatives. The antimicrobial activities of the prepared compounds were investigated against four bacterial strains: Xanthomonas campestris, Escherichia coli, Bacillus cereus, Bacillus megaterium, and a fungal strain Candida albicans. The biological evaluation studies of these indazole derivatives revealed that some of these tested compounds have shown moderate to goodin vitroantimicrobial activities.


2020 ◽  
Vol 18 ◽  
Author(s):  
Faheem Hadi ◽  
Tahir Maqbool ◽  
Sameera Khurshid ◽  
Aisha Nawaz ◽  
Saira Aftab ◽  
...  

Background: Fungal infections have always remain a problem and they are getting worse with passage of each year due to their resistance against available antibiotics. Natural ways of treatment with homoeopathic medicines made of mother tinctures of plants have no reported side effects and have been proved effective against many bacterial and fungal infections. Materials & Methods: Preparation of mother tinctures of plants Cressa cretica, Leptadenia pyrotechnica and Pulicaria crispa was done and used to evaluate the anti-fungal potential of these plants against potentially pathogenic fungal species like Aspergillus niger, Aspergillus flavus, Aspergillus ustus and Candida albicans by agar disc diffusion method. Each tincture was evaluated at 0.25 ml, 0.5 ml and 1 ml volume per disc and zone of inhibition was measured in millimetres and compared with commercial drug Fluconazole (2 mg/ml) which was used as standard. Results: The results showed that satisfactory anti-fungal activity of these plants in comparison to standard drug Fluconazole. The ratio of antifungal activity of Cressa cretica measured as the zone of growth inhibition of these cultures against Aspergillus niger, Aspergillus flavus, Aspergillus ustus and Candida albicans was 24 mm / 27 mm, 30mm / 28 mm, 23 mm/ 30 mm and 32 mm/ 30 mm respectively. In the case of Leptadenia pyrotechnica, the mother tincture’s antifungal activity was 32 mm / 27 mm, 30 mm / 28 mm, 17 mm/ 30 mm and 24 mm/ 30 mm. In case of our third plant Pulicaria crispa, antifungal activity came out to be 23 mm/ 27 mm, 26 mm/ 28 mm, 26 mm / 30 mm and 24 mm/ 30 mm. Conclusion: Our study proved that mother tincture of these plants can be a potential new therapy to treat fungal infections and has the potential to rule out fungal problems. Further research using mother tincture of these plants against other fungal species has the potential to prove them a safer and widespread anti-fungal homoeopathic medicine.


Author(s):  
Ravi Kumar Konda ◽  
Anish Kumar K ◽  
Phani Lakshman M ◽  
Mohammed Asif ◽  
Anusha Reddy D

Heterocyclic compounds are cyclic compounds containing carbon and other heteroatoms. The most common heteroatoms are oxygen, nitrogen, and Sulphur. A heterocyclic compound is a cyclic compound that has atoms at least two different elements as members of its ring. A Schiff base (azomethine) is named after its inventor, Hugo Schiff and it is a functional group that contains a carbon-nitrogen double bond with the nitrogen atom connected to an aryl or alkyl group but not hydrogen. Schiff bases of Pyridin-3 yl-carbohydrazide derivatives from ethyl nicotinate and different aromatic aldehydes. Schiff’s bases are aromatic substituted imine compounds. These compounds are very important in the medicinal and pharmaceutical fields because of their wide spectrum of biological activity. Schiff’s bases show antibacterial activity, antifungal activity, and also antitumor activity. Aromatic aldehydes were refluxed with ethyl nicotinate using ethanol as a solvent to form Schiff's bases. All chemicals are taken in equimolar concentrations. The synthesized compounds were characterized by melting point, solubility, percentage yield, TLC, and IR spectral analysis. All derivatives are evaluated for anti-bacterial activity by the cup plate method. The antibacterial activity of test compounds was compared against standard Streptomycin. The 5 synthesized compounds show moderate antimicrobial activity. The experimental work summarizes the synthesis and in-vitro antibacterial activity of Schiff base derivatives.


2020 ◽  
Vol 1 (2) ◽  
pp. 7
Author(s):  
Dyah Widiastuti ◽  
Ihda Zuyina Zuyina Ratna Sari ◽  
Isya Fikria Kalimah ◽  
Endang Setiani

Hand hygiene is one of the important factors that determine a person's health status. Hands are easily contaminated by microbes from the environment such as bacteria, viruses, and fungi through direct contact. Hand sanitizer is a type of media that can be used to clean hands from disease-causing microbes other than soap. Hand sanitizers are widely used by the community because they are considered more practical to use. This study aims to determine the anti-fungal activity of the hand sanitizer recommended by the World Health Organization (WHO) against Candida albicans. Anti-fungal activity was tested using the well diffusion method. The results showed that the higher the concentration of the hand sanitizer, the bigger the inhibition zone formed. The statistical test results obtained a significance value of p <0.05 at the variation of the concentration of hand sanitizer 50%, 75%, 100%, and treatment control. These results indicate that there is a significant difference between the hand sanitizer treatment and control of the inhibition zone formation in C. albicans. The WHO recommended hand sanitizer has medium inhibitory power against C. albicans bacteria.


2021 ◽  
Vol 3 (1) ◽  
pp. 32-41
Author(s):  
Puji Astutik ◽  
Richa Yuswantina ◽  
Rissa Laila Vifta

Parijoto fruit (Medinilla speciosa) contains active compounds of flavonoids, tannins, saponins, glycosides. Parijoto fruit (Medinilla speciosa) has many benefits for human health, one of which is as an anti-fungal. In this study, the antifungal activity test of 70% ethanol extract and 96% ethanol extract of parijoto fruit (Medinilla speciosa) was tested against Candida albicans. This research was conducted by maceration using 70% ethanol and 96% ethanol as solvents. While the anti-fungal activity used the disc diffusion method using a concentration variation of 2.5% w / v; 5% w / v and 10% w / v using the ratio of ketoconazole antibiotics. Parijoto fruit extract (Medinilla speciosa) obtained 70% (%) ethanol and 96% (%) ethanol. Ethanol 70% with a concentration of 2.5% w / v of 25.83 mm; 5% w / v was 27.03 mm and 10% w / v was 28.03 mm, while the ethanol extract of 96% parijoto fruit (Medinilla speciosa) at a concentration of 2.5% w / v was 31.59 mm; 5% w / v of 33.24 mm and 10% w / v of 36.11 mm. The statistical results of 70% ethanol and 96% ethanol, both of which have anti-fungal activity, are not much different, as evidenced by the T-Test statistical test with a P-Value of 0.00 <0.05, because the effect of the 96% parijoto fruit compound is more effective. . The 70% ethanol extract and 96% ethanol extract of parijoto fruit (Medinilla speciosa) can inhibit the growth of Candda albicans with a concentration of 10%. ABSTRAK Buah Parijoto (Medinilla speciosa) mengandung senyawa aktif flavonoid, tanin, saponin, glikosida. Buah parijoto (Medinilla speciosa) merupakan yang memiliki banyak manfaat bagi kesehatan manusia, salah satunya adalah sebagai antifungi. Dalam penelitian ini, uji aktivitas antifungi dari ekstrak etanol 70% dan ekstrak etanol 96% buah parijoto (Medinilla speciosa) akan diuji terhadap Candida albicans. Penelitian ini dilakukan dengan maserasi menggunakan pelarut etanol 70% dan etanol 96%. Sedangkan aktivitas antifungi menggunakan metode difusi cakram menggunakan variasi kosentrasi 2,5% b/v; 5% b/v dan 10% b/v dengan menggunakan perbandingan antibiotik ketokonazole. Ekstrak buah parijoto (Medinilla speciosa) diperoleh hasil etanol 70% (%) dan etanol 96% (%). Etanol 70% dengan konsentrasi 2,5% b/v sebesar 25,83 mm; 5% b/v sebesar 27,03 mm dan 10% b/v sebesar 28,03 mm sedangkan ekstrak etanol 96% buah parijoto (Medinilla speciosa) pada konsentrasi 2,5% b/v sebesar 31,59 mm; 5% b/v sebesar 33,24 mm dan 10% b/v sebesar 36,11 mm. Hasil statistik etanol 70% dan etanol 96% aktivitas antifungi keduanya memiliki aktivitas antifungi yang tidak jauh berbeda sebagaimana dibuktikan dari uji statistik T-Test dengan nilai P-Value 0,00 <0,05, karena pengaruh dari senyawa buah parijoto 96% lebih efektif. Ekstrak etanol 70% dan etanol 96% buah parijoto (Medinilla speciosa) dapat menghambat pertumbuhan Candda albicans dengan kosentrasi 10%.


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