scholarly journals Review on Synthesis of Thiazole Derivatives from α-Halo- ketones and Thiourea or N-Substituted Thiourea

Author(s):  
Sagar Ramdas Shrimandilkar

Thiazole represents important class of heterocyclic compounds. Thiazole and its derivatives have been reported to possess antitubercular, antibacterial, anti-inflammatory, anticancer, antifungal activity. Several methods of synthesis of thiazole derivatives have been reported, but most widely used synthetic approach to obtained thiazole derivatives is Hantzsch process. It involved synthesis of thiazole derivative from ?-halo-carbonyl compounds and thiourea or thiourea derivatives. This review mainly focuses on the research work reported in the scientific literature on the different procedures of synthesis of 2-amino thiazole and their derivatives.

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Ruhi Ali ◽  
Nadeem Siddiqui

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Benzothiazole is among the usually occurring heterocyclic nuclei in many marine as well as natural plant products. Benzothiazole is a privileged bicyclic ring system with multiple applications. It is known to exhibit a wide range of biological properties including anticancer, antimicrobial, and antidiabetic, anticonvulsant, anti-inflammatory, antiviral, antitubercular activities. A large number of therapeutic agents are synthesized with the help of benzothiazole nucleus. During recent years there have been some interesting developments in the biological activities of benzothiazole derivatives. These compounds have special significance in the field of medicinal chemistry due to their remarkable pharmacological potentialities. This review is mainly an attempt to present the research work reported in the recent scientific literature on different biological activities of benzothiazole compounds.


2020 ◽  
Vol 16 ◽  
Author(s):  
Meghshyam K. Patil ◽  
Vijay H. Masand ◽  
Atish K. Maldhure

: Schiff bases and their complexes are versatile compounds, which have been synthesized from the condensation of carbonyl compounds with amino compounds and exhibit a broad range of applications in biological, medicinal, catalysis, and industrial purposes. Furthermore, Schiff base-metal complexes have been used as a precursor for the synthesis of different metal oxides, which includes oxides of iron, cobalt, copper, nickel, manganese, vanadium, cadmium, zinc, mercury, etc. and ferrites such as Fe3O4, ZnFe2O4, and ZnCo2O4. These metal oxides have been utilized for several applications, which includes as a catalyst for several organic transformations and for biological activity. This review encompasses different methods of synthesis of metal oxides using Schiff base metal complexes precursor, their characterization, and various applications in detail.


Author(s):  
Anna Biernasiuk ◽  
Anna Berecka-Rycerz ◽  
Anna Gumieniczek ◽  
Maria Malm ◽  
Krzysztof Z. Łączkowski ◽  
...  

Abstract Recently, the occurrence of candidiasis has increased dramatically, especially in immunocompromised patients. Additionally, their treatment is often ineffective due to the resistance of yeasts to antimycotics. Therefore, there is a need to search for new antifungals. A series of nine newly synthesized thiazole derivatives containing the cyclopropane system, showing promising activity against Candida spp., has been further investigated. We decided to verify their antifungal activity towards clinical Candida albicans isolated from the oral cavity of patients with hematological malignancies and investigate the mode of action on fungal cell, the effect of combination with the selected antimycotics, toxicity to erythrocytes, and lipophilicity. These studies were performed by the broth microdilution method, test with sorbitol and ergosterol, checkerboard technique, erythrocyte lysis assay, and reversed phase thin-layer chromatography, respectively. All derivatives showed very strong activity (similar and even higher than nystatin) against all C. albicans isolates with minimal inhibitory concentration (MIC) = 0.008–7.81 µg/mL Their mechanism of action may be related to action within the fungal cell wall structure and/or within the cell membrane. The interactions between the derivatives and the selected antimycotics (nystatin, chlorhexidine, and thymol) showed additive effect only in the case of combination some of them and thymol. The erythrocyte lysis assay confirmed the low cytotoxicity of these compounds as compared to nystatin. The high lipophilicity of the derivatives was related with their high antifungal activity. The present studies confirm that the studied thiazole derivatives containing the cyclopropane system appear to be a very promising group of compounds in treatment of infections caused by C. albicans. However, this requires further studies in vivo. Key points • The newly thiazoles showed high antifungal activity and some of them — additive effect in combination with thymol. • Their mode of action may be related with the influence on the structure of the fungal cell wall and/or the cell membrane. • The low cytotoxicity against erythrocytes and high lipophilicity of these derivatives are their additional good properties. Graphical abstract


Life ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 16
Author(s):  
Andreza C. Santana ◽  
Ronaldo C. Silva Filho ◽  
José C. J. M. D. S. Menezes ◽  
Diego Allonso ◽  
Vinícius R. Campos

Arboviruses, in general, are a global threat due to their morbidity and mortality, which results in an important social and economic impact. Chikungunya virus (CHIKV), one of the most relevant arbovirus currently known, is a re-emergent virus that causes a disease named chikungunya fever, characterized by a severe arthralgia (joint pains) that can persist for several months or years in some individuals. Until now, no vaccine or specific antiviral drug is commercially available. Nitrogen heterocyclic scaffolds are found in medications, such as aristeromycin, favipiravir, fluorouracil, 6-azauridine, thioguanine, pyrimethamine, among others. New families of natural and synthetic nitrogen analogous compounds are reported to have significant anti-CHIKV effects. In the present work, we focus on these nitrogen-based heterocyclic compounds as an important class with CHIKV antiviral activity. We summarize the present understanding on this class of compounds against CHIKV and also present their possible mechanism of action.


2015 ◽  
Vol 35 (1Sup) ◽  
pp. 89-97 ◽  
Author(s):  
Gabriel Alexis Malagon ◽  
Jeisson Bello Peña ◽  
Gabriel Ordóñez Plata ◽  
Cesar Duarte Gualdrón

<p class="MsoNormal" style="text-align: justify;"><span style="font-family: 'Century Gothic', sans-serif; font-size: 8pt; letter-spacing: -0.1pt;"><span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">This article presents an analysis and discussion on the performance of a circuit-based model for Compact Fluorescent Lamps (CFL) <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">in a 120V 60Hz power grid. This model is proposed and validated in previous scientific literature for CFLs in 230V 50Hz systems. <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">Nevertheless, the derivation of this model is not straightforward to follow and its performance in 120V 60Hz systems is a matter of <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">research work. In this paper, the analytical derivation of this CFL model is presented in detail and its performance is discussed when <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">predicting the current of a CFL designed to operate in a 120V 60Hz electrical system. The derived model is separately implemented <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">in both MATLAB<span style="font-family: OptimaLTStd; font-size: 5pt; color: #231f20; font-style: normal; font-variant: normal;">® <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">and ATP-EMTP<span style="font-family: OptimaLTStd; font-size: 5pt; color: #231f20; font-style: normal; font-variant: normal;">® <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">software using two different sets of parameters previously proposed for 230V 50Hz CFLs. These <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">simulation results are compared against laboratory measurements using a programmable AC voltage source. The measurements <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">and simulations considered seven CFLs 110/127V 60Hz with different power ratings supplied by a sinusoidal (not distorted) voltage <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">source. The simulations under these conditions do not properly predict the current measurements and therefore the set of parameters <span style="font-family: OptimaLTStd; font-size: 9pt; color: #231f20; font-style: normal; font-variant: normal;">and/or the model itself need to be adjusted for 120V 60Hz power grids.</span></span></span></span></span></span></span></span></span><br style="font-style: normal; font-variant: normal; font-weight: normal; letter-spacing: normal; line-height: normal; orphans: 2; text-align: -webkit-auto; text-indent: 0px; text-transform: none; white-space: normal; widows: 2; word-spacing: 0px; -webkit-text-size-adjust: auto; -webkit-text-stroke-width: 0px;" /></span></span></span></span></span></span></p>


2013 ◽  
Vol 25 (4) ◽  
pp. 1849-1852 ◽  
Author(s):  
Ya-Li Song ◽  
Xiao-Ming Liu ◽  
Ning Yang ◽  
Geng-Liang Yang

1977 ◽  
Vol 25 (5) ◽  
pp. 922-925 ◽  
Author(s):  
TETSUJI KAMETANI ◽  
YOSHINARI SATOH ◽  
KEIICHIRO FUKUMOTO

2013 ◽  
Vol 10 (3) ◽  
pp. 525-536
Author(s):  
Baghdad Science Journal

The 4-(?-bromo acetyl)-4?-toluene sulfonanilide (2) was used as key intermediate to synthesize new heterocyclic compounds. This bromo compound was synthesized via sulfonation of amino group of p-amino acetophenone using Hinsburg method with 4-toluene sulfonyl chloride to form 4-acetyl-4?-toluene sulfonanilide (1) which is used as a starting material in this work. This compound was brominated to yield compound (2) which is used as a precursor to synthesize new five and seven membered heterocyclic compounds such as substituted 1,3-oxazoles (3,4), 1,3-thiazole derivatives (5-7), thiourea compounds (8a,b), 1,3-Thiazoline-2-thione compounds (9a-f) and 1,2,5-triazepine compounds (11a-d). The synthesized compounds were identified depending upon physical, FT-IR and UV spectroscopic data.


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