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1.
J Educ Health Promot ; 13: 20, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38532921

RESUMO

BACKGROUND: Diabetic patients are at higher risk of cardiovascular morbidity and mortality. NT-proBNP levels measurements are useful for the assessment of risk in heart failure patients in emergency condition and give the faster result. Further, it also offers lower cost and unnecessary hospitalization and follow-up cost. The studies have shown that NT-proBNP levels are a direct predictor of outcome risk in diabetic patients with heart failure. The objective of this research was to study the role of NT-proBNP levels to determine the severity of heart failure in diabetic patients. MATERIALS AND METHODS: In this study 150 patients diagnosed with symptomatic heart failure admitted to the emergency department of a tertiary care center from January 2021 to January 2022 have been included in Saraswati Institute Of Medical Sciences, Hapur, India. N-terminal pro-B-type natriuretic peptide (NT-Pro-BNP) levels were measured using an automated analyzer ranging between 60 and 3000 pg/ml. According to the European society of cardiology (ESC) guidelines, it has been defined as NT-Pro-BNP level above 125 pg/ml indicates a high possibility of heart failure and NT-Pro-BNP level below 125 pg/ml excludes the high possibility of heart failure. All the patients underwent an echocardiographic study and ejection fraction was calculated and recorded. RESULTS: In diabetic patients ejection fraction was significantly lower in diabetic patients: 47.15 ± 8.75% vs. 43.24 ± 9.54%, P = 0.002). We have observed statistically significant lower HDL values (40.10 ± vs. 35.94 mg/dL, P = 0.0004), however, significant higher triglycerides values were found (101.43 ± 41.7 mg/dL vs. 151.37 ± 78.85, P = 0.001). No significant difference was observed in LDL level (97.8 ± 31.23 vs. 92.35 ± 314.2, P ≥ 0.05) and total cholesterol level (161.49 ± 41.38 vs. 159.97 ± 41.12, P ≥ 0.05). CONCLUSION: We concluded that the measurement of NT-proBNP in heart failure and diabetic patients could be an economic marker for the evaluation of morbidity and mortality, facilitating better management and follow-up.

2.
Top Curr Chem (Cham) ; 382(1): 8, 2024 Feb 25.
Artigo em Inglês | MEDLINE | ID: mdl-38403746

RESUMO

From a synthetic perspective, bis(indolyl)methanes have undergone extensive investigation over the past two to three decades owing to their remarkable pharmacological activities, encompassing anticancer, antimicrobial, antioxidant, and antiinflammatory properties. These highly desirable attributes have spurred significant interest within the scientific community, leading to the development of various synthetic strategies that are not only more efficient but also ecofriendly. This synthesis-based literature review delves into the advancements made in the past 5 years, focusing on the synthesis of symmetrical as well as unsymmetrical bis(indolyl)methanes. The review encompasses a wide array of methods, ranging from well-established techniques to more unconventional and innovative approaches. Furthermore, it highlights the exploration of various substrates, encompassing readily available chemicals such as indole, aldehydes/ketones, indolyl methanols, etc. as well as the use of some specific compounds as starting materials to achieve the synthesis of this invaluable molecule. By encapsulating the latest developments in this field, this review provides insights into the expanding horizons of bis(indolyl)methane synthesis.


Assuntos
Anti-Infecciosos , Metano , Metano/química , Metanol , Antioxidantes , Aldeídos
3.
Chem Biodivers ; : e202301159, 2023 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-37718514

RESUMO

An [Et3 NH][HSO4 ] ionic-liquid catalyzed, intermolecular C-N bond formation for 1,2-disubstituted benzimidazole synthesis was achieved by the reaction of OPD and substituted aldehydes at ambient reaction conditions. Operational simplicity, use of easily available substrate and reagents, good yields (74-95 %) in short reaction time (4-18 min), simple work-up, and column chromatographic free synthesis are the remarkable features of this new protocol. The applicability of [Et3 NH][HSO4 ] ionic-liquid as a green and inexpensive catalyst with good recyclability and compatibility with a broad range of functional group having heteroatom, electron-withdrawing, and electron-releasing groups manifested the sustainability, eco-friendliness, and efficiency of the present methodology. Moreover, the antioxidant studies of the synthesized compounds using DPPH and ABTS assays were appealing and several synthesized compounds showed significant antioxidant activity.

4.
RSC Adv ; 13(34): 24093-24111, 2023 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-37577091

RESUMO

Benzoxazole is a resourceful and important member of the heteroarenes that connects synthetic organic chemistry to medicinal, pharmaceutical, and industrial areas. It is a bicyclic planar molecule and is the most favorable moiety for researchers because it has been extensively used as a starting material for different mechanistic approaches in drug discovery. The motif exhibits a high possibility of broad substrate scope and functionalization to offer several biological activities like anti-microbial, anti-fungal, anti-cancer, anti-oxidant, anti-inflammatory effects, and so on. There has been a large upsurge in the synthesis of benzoxazole via different pathways. The present article presents recent advances in synthetic strategies for benzoxazole derivatives since 2018. A variety of well-organized synthetic methodologies for benzoxazole using 2-aminophenol with aldehydes, ketones, acids, alcohols, isothiocyanates, ortho-esters, and alkynones under different reaction conditions and catalysts, viz. nanocatalysts, metal catalysts, and ionic liquid catalysts, with other miscellaneous techniques has been summarized.

5.
Diagn Cytopathol ; 51(10): 639-645, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37435632

RESUMO

BACKGROUND: Scrape cytology technique is useful for rapid intraoperative diagnosis of ovarian mass lesions that acts as an adjunct to frozen section examination. Though ovaries can be accessed by laparoscopy and USG guided FNAC, there are controversial reports regarding the safety of these procedures. The present study has been designed to evaluate the role of scrape cytology in a variety of ovarian mass lesions. OBJECTIVES: To study the cyto-morphology of ovarian mass lesions and to evaluate the role of scrape cytology technique in correctly diagnosing the ovarian lesions taking histopathological diagnosis as gold standard. MATERIAL AND METHODS: This is a prospective observational study done on 61 ovarian mass lesions as received from the Obstetrics and Gynecology department of our Institution. RESULT: Out of 61 cases, 58 (95.08%) cases were correctly diagnosed with respect to categorization and typing. The age ranged from 14 to 65 years with the mean age being 38.1 years. On histopathology, out of 61 cases, 39 (63.93%) were epithelial along with sub categorization of benign, borderline, and malignant, 13 (22.9%) were germ cell tumors, 5(8.19%) were sex cord stromal tumors, 3 (4.91%) were hemorrhagic cysts and the remaining 1 (1.63%) was massive ovarian edema. Thus, on comparing with histopathology, the sensitivity and specificity of scrape cytology technique were 93.55% and 96.67%, and the diagnostic accuracy was 95.08%. CONCLUSION: Scrape cytology of ovarian lesions can give quick and reliable results. Also, proper training of cytopathologists chiefly regarding the sampling technique, gross presentation of ovarian lesions and interpretation of scrape cytology smears is needed. Further studies to provide standard guidelines and reporting criteria will prove to be helpful.


Assuntos
Cistos Ovarianos , Neoplasias Ovarianas , Feminino , Humanos , Adolescente , Adulto Jovem , Adulto , Pessoa de Meia-Idade , Idoso , Neoplasias Ovarianas/patologia , Cistos Ovarianos/patologia , Técnicas Citológicas , Citodiagnóstico/métodos
6.
RSC Adv ; 13(19): 13337-13353, 2023 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-37143699

RESUMO

A highly promising approach for the synthesis of functionalized 1,1-dihomoarylmethane scaffolds (bis-dimedones, bis-cyclohexanediones, bis-pyrazoles, and bis-coumarins) using g-C3N4·SO3H ionic liquid via Knoevenagel-Michael reaction has been developed and the synthesized derivatives were well characterized using spectral studies. The method involved the reaction of C-H activated acids with a range of aromatic aldehydes, in a 2 : 1 ratio catalyzed by a g-C3N4·SO3H ionic liquid catalyst. The use of g-C3N4·SO3H as a catalyst has several benefits, such as low cost, easy preparation, and high stability. It was synthesized from urea powder and chloro-sulfonic acid and was thoroughly characterized using FT-IR, XRD, SEM, and HRTEM. The present work unveils a promising and environmentally friendly method for synthesizing 1,1-dihomoarylmethane scaffolds with high yield, selectivity, and efficiency, using mild reaction conditions, no need for chromatographic separation, and short reaction times. The approach adheres to green chemistry principles and offers a viable alternative to the previously reported methods.

7.
Heliyon ; 9(2): e13226, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36785822

RESUMO

The present pathway involves synthesis of isonicotinohydrazide derivatives using isoniazid and diversely substituted aldehydes in the presence of EtOH and catalytic amount of glycerol based carbon sulfonic acid catalyst. The developed pathway has so many merits like excellent yields (91-98%), short reaction time (4-10 min), easy reaction set up, no need of column chromatography, large substrate scope, easily recyclable and reusable catalyst. The synthesized compounds were screened for antimicrobial and anti-tubercular activity and it was observed that compounds possessed high biological potency against the Gram positive and Gram negative bacterial and fungal strains. Regarding anti-tubercular activity, compound 3m exhibited high % inhibition against Mycobacterium tuberculosis H37RV strain. Based on the outcome of in vitro studies, all the synthesized compounds were docked against E. coli (1KZN), C. albicans (1IYL), and M. tuberculosis H 37 Rv strain (2NSD). The synthesized derivatives were docked within the binding site of 1KZN, and 1IYL. However, with 2NSD, apart from 3h, all the derivatives displayed interaction within the binding cavity of the protein. All the crucial interactions with Asn46, Asp73, and Arg136 in 1KZN, His227, Leu451 in 1IYL, and Tyr158 in 2NSD were witnessed in the top-scored docked candidates. Molecular docking studies revealed the importance of the substitution at R position on isonicotinohydrazide scaffold. The nitrogen atoms of hydrazide moiety were involved in forming hydrogen bonding with the active site amino acids, and the substitution at the R position occupy the hydrophobic position in the binding pocket. Also, the functional groups present on the substituted R position were involved in forming hydrogen bonding with the crucial active site residues.

8.
RSC Adv ; 13(6): 3694-3714, 2023 Jan 24.
Artigo em Inglês | MEDLINE | ID: mdl-36756601

RESUMO

Benzodiazepines, seven-membered heterocyclic compounds having two nitrogen atoms at different positions, are ruling scaffolds in the area of pharmaceutical industry. They act as cardinal moieties in organic synthesis as well as in medicinal chemistry. Among the different benzodiazepines, 1,4- and 1,5-benzodiazepines play a far-reaching role in the field of biological activities such as anticonvulsion, anti-anxiety, sedation, and hypnotics. In the past few decades, researchers have conducted a lot of work on these moieties and developed broad, valuable, and significant approaches for their synthesis. In this review article, we recapitulate the systematic synthetic strategies of 1,4- and 1,5-benzodiazepines using o-phenylenediamine as a precursor over the past five years (2018-2022). This article will be helpful for scientists and researchers to examine and explore novel and efficient methods for the synthesis of these biologically active moieties.

9.
ACS Omega ; 8(6): 5877-5884, 2023 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-36816668

RESUMO

Green, eco-benign, and sustainable synthesis is paramount in present chemistry. Here, a facile, efficient, and [H2-DABCO][HSO4]2 ionic-liquid-catalyzed one-pot multicomponent synthesis of hexahydroquinolines was reported under ambient reaction conditions. The reaction of 1,3-dicarbonyls, malononitrile, and ammonium acetate with various aldehydes in the presence of an ionic liquid catalyst and EtOH solvent at room temperature afforded excellent yields (76-100%) of hexahydroquinolines under a short reaction time (5-15 min). Mild reaction conditions, broad substrate scope (28 derivatives), and column-chromatography-free synthesis with excellent catalytic efficiency and good recyclability rendered this protocol superior and practical. The greenness of the present method was assessed through eco-score and E-factor. The significant results in gram-scale synthetic conditions validate its applicability in industries as well as academia in the near future.

10.
ACS Omega ; 8(2): 2315-2327, 2023 Jan 17.
Artigo em Inglês | MEDLINE | ID: mdl-36687113

RESUMO

A demand for functional materials that are capable of tailoring light-emissive properties has apparently been rising nowadays substantially for their utilization in organic optoelectronic devices. Motivated by such promising characteristics, we present highly emissive as well as aggregation-induced emission (AIE) electroluminescent composite systems composed of a nematic liquid crystals (NLC) blended with polyethylene-functionalized gold nanospheres (GNSs). The major findings of this study include superior electro-optical properties such as threshold voltage reduction by around 24%. The fall time is reduced by 11.50, 30.33, 49.33, and 63.17% respectively, and rotational viscosity is reduced by 13.86, 32.77, 36.97, and 49.58% for 5.0 × 1011, 5.0 × 1012, 2.5 × 1013, and 5.0 × 1013 number of GNS-blended liquid crystal (LC) cells. The increased UV absorbance and greatly enhanced luminescence properties have been attributed to surface plasmon resonance near the surface of GNSs and AIE effect risen due to agglomeration of the capping agent with the NLC molecules respectively, and these characteristics make them suitable for new-age display applications.

11.
Comb Chem High Throughput Screen ; 26(7): 1251-1284, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-35770415

RESUMO

The present COVID-19 pandemic is terrible for the respiratory system and is caused by severe acute respiratory syndrome Coronavirus 2 (SARS-CoV-2). It has affected millions of people globally and over 511.9 million cases and 6.2 million deaths have been reported across the world. Various drugs have been repurposed, however, no specific medicine has been approved by the FDA to combat this disease till date. In this condition, researchers have been attracted to natural and safe products to improve immunity to viral infections through inhibiting viral cell entry, replication, and modulation. Various natural products, probiotics, and nutrients have antimicrobial, antiviral, analgesic, anti-inflammatory, and antiproliferative activities, and some of the compounds are also utilized in traditional medicine in Ayurveda, Siddha, and other cultures. This review provides a clinical perspective on the application of herbs for the prevention of viral infections.


Assuntos
COVID-19 , SARS-CoV-2 , Humanos , Pandemias , Antivirais/farmacologia , Antivirais/uso terapêutico , Anti-Inflamatórios
12.
J Mol Model ; 28(4): 77, 2022 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-35244782

RESUMO

Phalaris minor is a major weed of wheat crop which has evolved resistance against herbicides. Isoproturon is the most accepted herbicide developed resistance in 1992. Later, introduced herbicides also developed resistance and cross-resistance to their respective binding sites. Isoproturon binds at the QB binding site of the D1 protein of photosystem-II (PS-II), which blocks the electron transfer in photosynthesis. In this work, we have carried out a series of computational studies to prioritize the promising herbicides against D1 protein of P. minor. Through the computational studies, twenty-four lead molecules are prioritized which have shown a higher binding affinity and inhibition constant than the reference ligand molecule. The binding and conformational stability of docked complexes was evaluated by molecular dynamics simulations and binding free energy calculations i.e., MM/PBSA. A list of amino acids such as Ala225, Ser226, Phe227, and Asn229 present in the binding site of protein is obtained to be playing an important role in the stability of the protein-lead complex via hydrogen bond and π-π interactions. Binding free energy calculation revealed that the selected lead molecule binding is energetically favorable and driven by electrostatic interactions. Among 24 leads, computational results have uncovered eight promising compounds as potential herbicides which have shown comparable physiochemical profile, better docking scores, system stability, H-bond occupancy, and binding free energy than terbutryn, a reference molecule. These prioritized molecules were custom synthesized and evaluated for their herbicidal activity and specificity through whole plant assay under laboratory-controlled conditions. The lead molecule ELC5 (6-ethoxy-4-N-(2-morpholin-4-ylethyl)-2-N-propan-2-yl-1,3,5-triazine-2,4-diamine) has shown comparable activity to the reference herbicide(isoproturon) against P. minor.


Assuntos
Herbicidas , Phalaris , Diaminas , Herbicidas/química , Herbicidas/metabolismo , Herbicidas/farmacologia , Phalaris/metabolismo , Triazinas/farmacologia , Triticum/metabolismo
13.
Mol Divers ; 26(1): 513-553, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33180241

RESUMO

Benzothiazole is a privileged scaffold in the field of synthetic and medicinal chemistry. Its derivatives and metal complexes possess a gamut of pharmacological properties and high degree of structural diversity that has proven it vital for the investigation for novel therapeutics. The 2nd position of benzothiazole is the most active site that makes 2-arylbenzothiazole as felicitous scaffolds in pharmaceutical chemistry. The extensive significance of benzo-fused heterocyclic moieties formation has led to broad and valuable different approaches for their synthesis. This review deals with the synthetic approaches developed so far for the synthesis of 2-arylbenzothiazoles. Moreover, this article abridges the publications devoted to the synthesis of this moiety over the last 6 years. This study gives a current precis of research on the fabrication of 2-arylbenzothiazoles through different synthetic pathways and shall be helpful for researchers and scientists who are working in this field to make more potent biologically active benzothiazole-based drugs.


Assuntos
Química Farmacêutica
14.
Mini Rev Med Chem ; 21(20): 3219-3248, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33663363

RESUMO

Dementia is a chronic neurodegenerative disease, and a maximum number of the cases are directly related to Alzheimer's disease. More than 4 million people are living with Alzheimer's disease-related dementia in India, making it a national crisis. Alzheimer's disease deteriorates cognitive functions with the passage of time and consists of multi-faceted factors, such as the decline of acetylcholine level, amyloid ß-aggregation, tau hyperphosphorylation, oxidative stress, etc. The classical drugs used to date, are focused on only one target and are not serving the cause properly. Hence, the community of scientists is rigorously working on multi-target-directed agents that incorporate two or more active scaffolds in one compound or hybrid of active moieties. This article aims to evaluate novel potential compounds and moieties, such as quinolines, chalcones, coumarins, chromenes, piperazine, carbazoles, cinnamic acids, tacrine hybrids, donepezil hybrids, etc., that have been introduced as multi-target-directed agents in the recent five years.


Assuntos
Doença de Alzheimer , Doenças Neurodegenerativas , Fármacos Neuroprotetores , Doença de Alzheimer/tratamento farmacológico , Peptídeos beta-Amiloides , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/uso terapêutico , Humanos , Ligantes , Doenças Neurodegenerativas/tratamento farmacológico , Fármacos Neuroprotetores/uso terapêutico
15.
Curr Org Synth ; 18(4): 388-398, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33441076

RESUMO

AIM AND OBJECTIVE: To explore the impact of synthesis conditions (temperature and time) on the properties of developed Graphene Oxide (GO). BACKGROUND: A highly promising approach has been used for the synthesis of graphene oxide (GO) from graphite flakes using the modified Hummers method. Concentrated sulfuric acid was used as an intercalating agent and the oxidation was done with the help of potassium permanganate and hydrogen peroxide. METHODS: The present method does not need expensive membranes for the filtration of Carbon and metalcontaining residues. The pre-cooling method is used to eradicate the explosive behavior of intermediate steps. The high quality of synthesized graphene oxides was confirmed by a series of characterization techniques, including Fourier transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, thermogravimetric analysis, energy-dispersive X-ray spectroscopy, and atomic force microscopy. RESULTS: The results indicated the presence of Oxygen-containing functional groups, and a rise in the Oxygen content confirmed the synthesis of high-quality graphene oxide. CONCLUSION: As per obtained experimental findings and subsequent analysis, the synthesized high-quality graphene oxide could be used in the design of membranes for water treatment applications.

16.
Top Curr Chem (Cham) ; 378(4-5): 44, 2020 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-32776212

RESUMO

Perimidines are versatile scaffolds and a fascinating class of N-heterocycles that have evolved significantly in recent years due to their immense applications in life sciences, medical sciences, and industrial chemistry. Their ability of molecular interaction with different proteins, complex formation with metals, and distinct behavior in various ranges of light makes them more appealing and challenging for future scientists. Various novel technologies have been developed for the selective synthesis of perimidines and their conjugated derivatives. These methods extend to the preparation of different bioactive and industrially applicable molecules. This review aims to present the most recent advancements in perimidine synthesis under varied conditions like MW radiation, ultrasound, and grinding using different catalysts such as ionic liquids, acid, metal, and nanocatalyst and also under green environments like catalyst and solvent-free synthesis. The applications of perimidine derivatives in drug discovery, polymer chemistry, photo sensors, dye industries, and catalytic activity in organic synthesis are discussed in this survey. This article is expected to be a systematic, authoritative, and critical review on the chemistry of perimidines that compiles most of the state-of-art innovation in this area.


Assuntos
Quinazolinas/síntese química , Descoberta de Drogas , Estrutura Molecular , Quinazolinas/química , Ondas Ultrassônicas
17.
Mini Rev Med Chem ; 20(13): 1190-1232, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32348221

RESUMO

Curcumin is a poly phenolic compound extracted from turmeric. Over the past years, it has acquired significant interest among researchers due to its numerous pharmacological activities like anti- cancer, anti-alzheimer, anti-diabetic, anti-bacterial, anti-inflammatory and so on. However, the clinical use of curcumin is still obstructed due to tremendously poor bioavailability, rapid metabolism, lower gastrointestinal absorption, and low permeability through cell that makes its pharmacology thrilling. These issues have led to enormous surge of investigation to develop curcumin nano formulations which can overcome these restrictive causes. The scientists all across the universe are working on designing several drug delivery systems viz. liposomes, micelles, magnetic nano carriers, etc. for curcumin and its composites which not only improve its physiochemical properties but also enhanced its therapeutic applications. The review aims to systematically examine the treasure of information about the medicinal use of curcumin. This article delivers a general idea of the current study piloted to overwhelm the complications with the bioavailability of curcumin which have exhibited an enhanced biological activity than curcumin. This article explains the latest and detailed study of curcumin and its conjugates, its phytochemistry and biological perspectives and also proved curcumin as an efficient drug candidate for the treatment of numerous diseases. Recent advancements and futuristic viewpoints are also deliberated, which shall help researchers and foster commercial translations of improved nanosized curcumin combination for the treatment of various diseases.


Assuntos
Curcumina/química , Portadores de Fármacos/química , Sobrevivência Celular/efeitos dos fármacos , Curcumina/farmacologia , Curcumina/uso terapêutico , Humanos , Hidrogéis/química , Lipossomos/química , Micelas , Nanoestruturas/química , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Cicatrização/efeitos dos fármacos
18.
Top Curr Chem (Cham) ; 378(2): 34, 2020 Mar 23.
Artigo em Inglês | MEDLINE | ID: mdl-32206929

RESUMO

In past decades, interdisciplinary research has been of great interest for scholars. Thiazolidine motifs behave as a bridge between organic synthesis and medicinal chemistry and compel researchers to explore new drug candidates. Thiazolidine motifs are very intriguing heterocyclic five-membered moieties present in diverse natural and bioactive compounds having sulfur at the first position and nitrogen at the third position. The presence of sulfur enhances their pharmacological properties, and, therefore, they are used as vehicles in the synthesis of valuable organic combinations. They show varied biological properties viz. anticancer, anticonvulsant, antimicrobial, anti-inflammatory, neuroprotective, antioxidant activity and so on. This diversity in the biological response makes it a highly prized moiety. Based on literature studies, various synthetic approaches like multicomponent reaction, click reaction, nano-catalysis and green chemistry have been employed to improve their selectivity, purity, product yield and pharmacokinetic activity. In this review article, we have summarized systematic approaches for the synthesis of thiazolidine and its derivatives, along with their pharmacological activity, including advantages of green synthesis, atom economy, cleaner reaction profile and catalyst recovery which will help scientists to probe and stimulate the study of these scaffolds.


Assuntos
Técnicas de Química Sintética/métodos , Tiazolidinas/química , Estrutura Molecular
19.
Curr Org Synth ; 16(8): 1078-1104, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31984918

RESUMO

Heterocyclic compounds are pervasive in many areas of life and one of the heterocycles, imidazole is a unique heterocyclic five-membered aromatic compound having two sp2 hybridized nitrogen atoms. Its integral name is 1, 3 diazole and previously, it was known as glyoxalin. This moiety has achieved a considerable place among scientists in recent years by reason of its divergent synthetic strategies and uncommon biological and pharmacological activities, for example, anti-convulsant, anti-microbial, anti-cancer, anti-inflammatory, anti-tumor, anti-viral, anti-ulcer, analgesic, etc. Due to distinct therapeutic actions, it is still an engrossed area of research. Researchers currently are inventing new greener methods to synthesize its derivatives and to improve its pharmacological activities. The purpose of this review is to study the literature that can help researchers to explore this area, its prevailing program for synthesis in environmentally friendly conditions and biological profile throughout past decades.


Assuntos
Imidazóis/síntese química , Imidazóis/farmacologia , Analgésicos/síntese química , Analgésicos/farmacologia , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/farmacologia , Antiulcerosos/síntese química , Antiulcerosos/farmacologia , Anticonvulsivantes/síntese química , Anticonvulsivantes/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Antivirais/síntese química , Antivirais/farmacologia , Catálise , Desenho de Fármacos , Química Verde , Humanos , Nanopartículas Metálicas/química , Metais/química , Estrutura Molecular , Relação Estrutura-Atividade
20.
Comb Chem High Throughput Screen ; 21(4): 236-253, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29611485

RESUMO

BACKGROUND: Heterocycles have extended into widespread use for generating large collection of molecules in multi-component reactions. The development of new strategies for fused pyrimidobenzothiazole system has remained a highly attractive but challenging proposition for scientists working all around. OBJECTIVE: The main objective of this work is to explore the utility of different catalysts as an ecofriendly reaction medium for green Biginellis reaction. METHOD: A detailed study of Biginellis reactions using various catalysts was done using different research tools. The methods involved reaction of equimolar mixture of benzothiazole, 1,3-diketone and aldehyde as reactants by conventional and greener pathways via Knoevenagal condensation. RESULTS: The present review has several significant advantages for the scientists regarding green synthesis viz. green conditions, short reaction times, high yields, clean reaction conditions, easy isolation of products, simple work-up procedure and mild reaction conditions. CONCLUSION: Our report gives an overview of the combinatorial libraries for fused benzothiazole entities using metal catalyst, acid catalyst, ionic liquids, phase transfer catalyst, nano catalyst, etc.


Assuntos
Benzotiazóis/síntese química , Técnicas de Química Combinatória/métodos , Aldeídos/química , Catálise , Química Verde , Cetonas/química , Pirimidinas/química
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