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1.
Pak J Pharm Sci ; 33(1(Supplementary)): 299-306, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32122862

RESUMO

The present study was designed to develop novel lipid microparticles in order to improve solubility, dissolution and bioavailability of a lipophilic drug of BCS class II, lamotrigine. For that purpose, increase in solubility of the model drug was investigated using different lipids and the promising lipids were further used for the fabrication of microparticles. Solid lipid (GMS) and liquid lipid (olive oil) were used along with an emulsifier (Tween 80) and a stabilizer (Poloxamer 188) to prepare mircoparticles by melt emulsification method. Prepared formulations were characterized for physicochemical properties such as solubility, particle size, zeta potential, polydispersity index and entrapment efficiency. In vitro dissolution studies were carried out in 0.01 N HCl for 24 h. The findings provided that the solubility of lamotrigine was reasonably increased in GMS, olive oil, Tween 80 and poloxamer 180. The lamotrigine solubility was increased 4.92 fold with G4 microparticles formulation. Size analysis revealed that the microparticles were in range of 11.1 to 178.8 µm and the zeta potential values were from -13 to -20 mV. Microparticles prepared with solid and liquid lipids exhibited satisfactory entrapment efficiency ranging from 59 to 87%. Conclusively, the outcomes of the studies suggest the appropriateness of selected ingredients for improving solubility as well as loading of lamotrigine in microparticles for its sustained and effective delivery.

2.
Biofactors ; 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-32039535

RESUMO

Reprogrammed metabolism is key biochemical characteristic of malignant cells, which represents one of the emerging hallmarks of cancer. Currently, there is rising contemplation on oxidative pentose phosphate pathway (PPP) enzymes as potential therapeutic hits due to their affiliation with tumor metabolism. 6-Phosphogluconate dehydrogenase (6PGD), third oxidative decarboxylase of PPP, has received a great deal of attention during recent years due to its critical role in tumorigenesis and redox homeostasis. 6PGD has been reported to overexpress in number of cancer types and its hyperactivation is mediated through post-transcriptional and post-translational modifications by YTH domain family 2 (YTHDF2), Nrf2 (nuclear factor erythroid 2-related factor 2), EGFR (epidermal growth factor receptor) and via direct structural interactions with ME1 (malic enzyme 1). Upregulated expression of 6PGD provides metabolic as well as defensive advantage to cancer cells, thus, promoting their proliferative and metastatic potential. Moreover, enhanced 6PGD expression also performs key role in development of chemoresistance as well as radiation resistance in cancer. This review aims to discuss the historical timeline and cancer-specific role of 6PGD, pharmacological and genetic inhibitors of 6PGD and 6PGD as prognostic biomarker in order to explore its potential for therapeutic interventions. We anticipate that targeting this imperative supplier of NADPH might serve as tempting avenue to combat the deadly disease like cancer.

3.
Bioorg Chem ; 92: 103216, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31491567

RESUMO

In our current research, a diverse effect of acetylcholinesterase inhibitors was studied on BALB-C mice by using pentylenetetrazole (PTZ) seizure model. A series of carboxamide analogs (4a-4i) have been synthesized via Suzuki coupling reaction in moderate to good yields (35-84%). To study the efficacy of the synthesized compounds against AD, in-vitro inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) was performed. A number of compounds showed inhibition in low micromolar range. Subsequently, these compounds were evaluated for anticonvulsive effects in BALB-C mice by using pentylenetetrazole (PTZ) seizure model. The compound 4e displayed potential anticonvulsive effect and displayed 50% and 80% protection from mortality at the dose of 10 mg/kg, and 30 mg/kg respectively. The compound 4h showed some protection (33%) from mortality at 10 mg/kg and was not further explored based on non-significant delay in onset of myoclonic seizures. While, other compounds from the series did not show any anticonvulsive activity. To rationalize the observed biological activity, we performed docking studies against AChE and BChE targets. To explore the rationale of the mechanism of in-vivo anticonvulsant activity, docking studies were performed on GABAergic receptors. Moreover, in order to establish a relationship between physiochemical data of the synthesized compounds and their in-vivo performance, we employed in-silico pharmacokinetic predictions. Our in-silico predictions suggest that the plasma protein binding, low to moderate blood brain barrier penetration and low solubility are the main attributes of low in-vivo performance.

4.
Mol Divers ; 2019 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-31463833

RESUMO

Organic reactions under green conditions have become popular day by day because of increased use of harmful chemicals leading to environmental hazards. This review focuses the implementation of green chemistry in Suzuki-Miyaura, Heck, Stille and Chan-Lam cross-coupling reactions incorporating a variety of strategies in which ionic liquids, water and microwave irradiations are extensively used.

5.
Mol Divers ; 23(1): 215-259, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30159807

RESUMO

Chan-Lam coupling is one of the most popular and easy methods to perform arylation of amines (N-arylations). This cross-coupling is generally performed by reacting aryl boronate derivatives with a variety of substrates involving nitrogen containing functional groups such as amines, amides, ureas, hydrazine, carbamates. This article summarizes the synthetic applications of this reaction and the efforts of scientists to develop novel and efficient methodologies for this reaction.


Assuntos
Técnicas de Química Sintética , Aminas/química , Nitrogênio/química
6.
Chem Biol Drug Des ; 93(2): 154-162, 2019 02.
Artigo em Inglês | MEDLINE | ID: mdl-30216686

RESUMO

The development of functional imaging is a promising strategy for diagnosis and treatment of infectious and cancerous diseases. In this study, epirubicin was developed as a [99m Tc]-labeled radiopharmaceutical for the imaging of multi-drug-resistant Staphylococcus aureus infections. The labeling was carried out using sodium pertechnetate (Na99m TcO4 ; ~370 MBq). The other parameters such as amount of ligand, reducing agent (SnCl2 .2H2 O), and pH were optimized. The highest labeling yield ≥96.98% was achieved when 0.3 mg epirubicin, 13 µg SnCl2 .2H2 O, and ~370 MBq Na99m TcO4 were incubated at pH 7 for 15 min in the presence of ascorbic acid at room temperature. Radiochemical purity, stability, charge, and glomerular filtration rate were studied to evaluate the biological compatibility for in vivo administration. Biodistribution investigations showed radiotracer uptake (13.89 ± 1.56% ID/gm organ) by liver and 7.79 ± 0.38% ID/gm organ by kidneys at 30 min post-injection which promisingly wash out at 24 hr post-injection. Scintigraphy study showed selective uptake in S. aureus-infected tissues in contrast to turpentine oil-induced inflamed tissues. Target-to-non-target ratio (6.7 ± 0.05) was calculated at 1 hr post-injection using SPECT gamma camera. The results of this study reveal that the [99m Tc]-epirubicin can be a choice of imaging and monitoring the treatment process of multi-drug resistant S. aureus bacterial infections.


Assuntos
Epirubicina/química , Staphylococcus aureus Resistente à Meticilina/fisiologia , Compostos Radiofarmacêuticos/química , Infecções Estafilocócicas/diagnóstico , Tecnécio/química , Tomografia Computadorizada de Emissão de Fóton Único , Animais , Estabilidade de Medicamentos , Epirubicina/sangue , Epirubicina/metabolismo , Taxa de Filtração Glomerular , Concentração de Íons de Hidrogênio , Marcação por Isótopo , Coelhos , Compostos Radiofarmacêuticos/sangue , Compostos Radiofarmacêuticos/metabolismo , Distribuição Tecidual
7.
Pak J Pharm Sci ; 32(6(Supplementary)): 2795-2800, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32024616

RESUMO

Four series of pyrazolobenzothiazine derivatives were evaluated for their anticancer activity against six different cancer cell lines i.e., KB (human oral carcinoma cells), MCF-7(human breast carcinoma cells), A549 (human alveolar adenocarcinoma cells), Hep-G2 (liver carcinoma cells), SGC-7901(human gastric carcinoma cells) and S1 (human colon carcinoma cells) using MTT assay. Among eighteen compounds tested, six compounds i.e., 1a, 1b, 1d, 4a, 4d and 4e were more active than 5-florouracil against human oral carcinoma cells (KB). Moreover, compounds 2b and 2c showed activity comparable to 5-FU against KB cell line. In addition, eight compounds were non-toxic to human PBM cells and thus exhibit selective anticancer activity.

8.
Pak J Pharm Sci ; 32(5(Supplementary)): 2215-2222, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31894047

RESUMO

Synthesis and characterization of novel structural hybrids of ciprofloxacin linked with a variety of anilides have been described in this paper. Antitumor activity of these derivatives was assessed against liver cell line (Huh-7) using MTT assay. Among the synthesized derivatives, compound 6a inhibited the growth of tumor cells by displaying 68.36% cell viability at 100 µg/mL concentration which was then in-silico modelled to delineate the potential mechanistic insights for its antiproliferative activity. The PASS prediction indicated the TopII as potential anticancer target of compound 6a. The induced fit docking revealed that compound 6a inhibits the TopII with superior binding affinity and forms stronger contacts with active site's key residues responsible for DNA-TopII intercalation and catalytic inhibition consistent with its cytotoxic potential. Therefore, compound 6a can be considered as a potential lead for further optimization in the development of ciprofloxacin-derived anticancer drugs.

9.
Mol Biol Rep ; 45(5): 1457-1468, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29974398

RESUMO

Diagnosis of deep-seated bacterial infection remains a serious medical challenge. The situation is becoming more severe with the increasing prevalence of bacteria that are resistant to multiple antibiotic classes. Early efforts to develop imaging agents for infection, such as technetium-99m (99mTc) labeled leukocytes, were encouraging, but they failed to differentiate between bacterial infection and sterile inflammation. Other diagnostic techniques, such as ultrasonography, magnetic resonance imaging, and computed tomography, also fail to distinguish between bacterial infection and sterile inflammation. In an attempt to bypass these problems, the potent, broad-spectrum antibiotic ciprofloxacin was labeled with 99mTc to image bacterial infection. Initial results were encouraging, but excitement declined when controversial results were reported. Subsequent radiolabeling of ciprofloxacin with 99mTc using tricarbonyl and nitrido core, fluorine and rhenium couldn't produce robust infection imaging agent and remained in discussion. The issue of developing a robust probe can be approached by reviewing the broad-spectrum activity of ciprofloxacin, labeling strategies, potential for imaging infection, and structure-activity (specificity) relationships. In this review we discuss ways to accelerate efforts to improve the specificity of ciprofloxacin-based imaging.


Assuntos
Infecções Bacterianas/diagnóstico por imagem , Infecções Bacterianas/tratamento farmacológico , Ciprofloxacino/química , Ciprofloxacino/uso terapêutico , Imagem Molecular/métodos , Animais , Infecções Bacterianas/metabolismo , Ciprofloxacino/farmacocinética , Radioisótopos de Flúor/química , Humanos , Marcação por Isótopo/métodos , Compostos Radiofarmacêuticos/síntese química , Tecnécio/química
10.
Mol Divers ; 22(2): 447-501, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29728870

RESUMO

Aziridine ring opening reactions have gained tremendous importance in the synthesis of nitrogen containing biologically active molecules. During recent years, a great effort has been put forward by scientists toward unique bond construction methodologies via ring opening of aziridines. In this regard, a wide range of chiral metal- and organo-catalyzed desymmetrization reactions of aziridines have been reported with carbon, sulfur, oxygen, nitrogen, halogen, and other nucleophiles. In this review, an outline of methodologies adopted by a number of scientists during 2013-2017 for aziridine ring opening reactions as well as their synthetic applications is described.


Assuntos
Aziridinas/química , Estereoisomerismo
11.
Appl Biochem Biotechnol ; 185(1): 127-139, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29098558

RESUMO

Bacterial infection poses life-threatening challenge to humanity and stimulates to the researchers for developing better diagnostic and therapeutic agents complying with existing theranostic techniques. Nuclear medicine technique helps to visualize hard-to-diagnose deep-seated bacterial infections using radionuclide-labeled tracer agents. Metronidazole is an antiprotozoal antibiotic that serves as a preeminent anaerobic chemotherapeutic agent. The aim of this study was to develop technetium-99m-labeled metronidazole radiotracer for the detection of deep-seated bacterial infections. Radiosynthesis of 99mTc-metronidazole was carried by reacting reduced technetium-99m and metronidazole at neutral pH for 30 min. The stannous chloride dihydrate was used as the reducing agent. At optimum radiolabeling conditions, ~ 94% radiochemical was obtained. Quality control analysis was carried out with a chromatographic paper and instant thin-layer chromatographic analysis. The biodistribution study of radiochemical was performed using Escherichia coli bacterial infection-induced rat model. The scintigraphic study was performed using E. coli bacterial infection-induced rabbit model. The results showed promising accumulation at the site of infection and its rapid clearance from the body. The tracer showed target-to-non-target ratio 5.57 ± 0.04 at 1 h post-injection. The results showed that 99mTc-MNZ has promising potential to accumulate at E. coli bacterial infection that can be used for E. coli infection imaging.


Assuntos
Infecções por Escherichia coli , Escherichia coli/metabolismo , Metronidazol/química , Compostos Radiofarmacêuticos , Tecnécio/química , Animais , Modelos Animais de Doenças , Infecções por Escherichia coli/diagnóstico por imagem , Infecções por Escherichia coli/tratamento farmacológico , Infecções por Escherichia coli/metabolismo , Coelhos , Compostos Radiofarmacêuticos/síntese química , Compostos Radiofarmacêuticos/química , Compostos Radiofarmacêuticos/farmacocinética , Compostos Radiofarmacêuticos/farmacologia , Ratos , Ratos Sprague-Dawley
12.
Mol Divers ; 22(1): 191-205, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29138964

RESUMO

Thiolysis of epoxides offers an efficient and simple synthetic approach to access [Formula: see text]-hydroxy sulfides which are valuable scaffold in the synthesis of various important molecules in medicinal chemistry. This review article presents a recent compilation of the synthetic approaches developed after 2000 for the thiolysis of epoxides.


Assuntos
Compostos de Epóxi/química , Modelos Químicos , Enxofre/química , Catálise , Líquidos Iônicos/química , Metais/química , Estrutura Molecular , Solventes/química
13.
Pak J Pharm Sci ; 30(4): 1327-1334, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29039333

RESUMO

Natural resources right from the beginning of the human civilization has paved the way to human being to combat different challenges. The big challenge was to safe the human being from diseases and shortage of food. Plants helped the man in both areas very efficiently. No doubt when plants are used as food actually we are also taking lot of compounds of medicinal values in an excellent combination which naturally reduce the risk of diseases. Extraction and purification of several medicinally important compounds also gave the way to develop pharmaceutical industry in addition to its own therapeutic effects against different lethal diseases. Pumpkin is one of the several medicinal important vegetables used in different way on the behalf of its admirable power to combat different diseases. Antioxidant and biological studies showed very important results. A good coherence was found among extraction yield (10.52 to 18.45%), total phenolics (1.13 to 6.78 mg GAE/100g), total flavonoids (0.23 to 0.72mg CE/100g) and antioxidant potential (≻70%). Antibacterial assays of peel and puree extracts advocated good potential to stop the growth and division of pathogenic bacteria. Further biological activity study was carried out using MDBK cancer cell line. The growth inhibitory effect on cancer cell line using MTT assay showed methanol extracts of peel and puree both remained efficient to inhibit growth (≻35%) and cell division of cancer cells. Our results showed that extracts of pumpkin puree and its waste, peel, may be utilize to prepare functional food against pathogenic born diseases and most active compounds may also be extracted, concentrated and converted into tablets or suspension form for therapeutic purposes.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Cucurbita/química , Extratos Vegetais/farmacologia , Antibacterianos/química , Antioxidantes/química , Divisão Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Flavonoides/análise , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/farmacologia , Humanos , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Fenóis/análise , Extratos Vegetais/química
14.
Appl Biochem Biotechnol ; 183(1): 374-384, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28285355

RESUMO

Bacterial infection is one of the vital reasons of morbidity and mortality, especially in developing countries. It appears silently without bothering the geological borders and imposes a grave threat to humanity. Nuclear medicine technique has an important role in helping early diagnosis of deep-seated infections. The aim of this study was to develop a new radiopharmaceutical 99mTc-labeling sulfadiazine as an infection imaging agent. Radiolabeling of sulfadiazine with technetium-99m (99mTc) was carried out using stannous tartrate as a reducing agent in the presence of gentistic acid at pH = 5. The quality control tests revealed ~98% labeling efficiency. Paper chromatographic (PC) and instant thin-layer chromatographic (ITLC) techniques were used to analyze radiochemical yield. Biodistribution and infection specificity of the radiotracer were performed with Escherichia coli (E. coli) infection-induced rats. Scintigraphy and glomerular filtration rate (GFR) study was performed in E. coli-infected rabbits. Scintigraphy indicated E. coli infection targeting potential of 99mTc-SDZ, while biodistribution study showed minimal uptake of 99mTc-SDZ in non-targeted tissues. The uptake in the kidneys was found 2.56 ± 0.06, 2.09 ± 0.10, and 1.68 ± 0.09% at 30 min, 1 h, and 4 h, respectively. The infected muscle (target) to non-infected muscle (non-target) ratio (T/NT) was found 4.49 ± 0.04, 6.78 ± 0.07, and 5.59 ± 0.08 at 30 min, 1 h, and 4 h, respectively.


Assuntos
Infecções por Escherichia coli/diagnóstico por imagem , Escherichia coli , Marcação por Isótopo/métodos , Sulfadiazina , Tecnécio , Animais , Infecções por Escherichia coli/tratamento farmacológico , Camundongos , Coelhos , Cintilografia , Ratos , Ratos Sprague-Dawley , Sulfadiazina/química , Sulfadiazina/farmacocinética , Sulfadiazina/farmacologia , Tecnécio/química , Tecnécio/farmacocinética , Tecnécio/farmacologia
15.
J Labelled Comp Radiopharm ; 60(5): 242-249, 2017 05 15.
Artigo em Inglês | MEDLINE | ID: mdl-28181269

RESUMO

The radiolabeled drug 99m Tc-tazobactam (99m Tc-TZB) was developed and assessed as an infection imaging agent in Pseudomonas aeruginosa and Salmonella enterica infection-induced animal models by comparing with inflammation induced animal models. Radiosynthesis of 99m Tc-TZB was assessed while changing ligand concentration, reducing agent concentration, pH, and reaction time while keeping radioactivity constant (~370 MBq). Percent labeling of the resulting complex was measured using paper chromatography and instant thin layer chromatography. The analysis of the 99m Tc-TZB complex indicated >95% labeling yield and electrophoresis revealed complex is neutral in nature. The biodistribution study also showed predominantly renal excretion; however liver, stomach, and intestine also showed slight tracer agent uptake. The agent significantly accumulated in Pseudomonas aeruginosa and Salmonella enterica infection induced tissues 3.58 ± 0.26% and 2.43 ± 0.42% respectively at 1 hour postinjection. The inflamed tissue failed to uptake noticeable activity at 1 hour time point. The scintigraphic study results were found in accordance with biodistribution pattern. On the basis of our preliminary results, the newly developed 99m Tc-TZB can be used to diagnose bacterial infection and to discriminate between infected and inflamed tissues.


Assuntos
Ácido Penicilânico/análogos & derivados , Infecções por Pseudomonas/diagnóstico por imagem , Cintilografia/métodos , Infecções por Salmonella/diagnóstico por imagem , Tecnécio/química , Animais , Técnicas de Química Sintética , Concentração de Íons de Hidrogênio , Ligantes , Ácido Penicilânico/síntese química , Ácido Penicilânico/química , Ácido Penicilânico/farmacocinética , Pseudomonas aeruginosa/fisiologia , Controle de Qualidade , Coelhos , Radioquímica , Ratos , Substâncias Redutoras/química , Salmonella enterica/fisiologia , Tazobactam , Distribuição Tecidual
16.
Mol Divers ; 20(4): 969-987, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27376747

RESUMO

Ring opening of epoxides has been an area of interest for organic chemists, owing to their reactivity toward nucleophiles. Such reactions yield important products depending on the type of nucleophiles used. This review article covers the synthetic approaches (1991-2015) used for the ring opening of epoxides via carbon nucleophiles.


Assuntos
Técnicas de Química Sintética , Compostos de Epóxi/química , Amidas/química , Aminoácidos/química , Carbono/química , Compostos de Epóxi/síntese química , Ésteres/química , Cetonas/química , Compostos Organometálicos/química , Estereoisomerismo
17.
Molecules ; 20(8): 14699-745, 2015 Aug 13.
Artigo em Inglês | MEDLINE | ID: mdl-26287135

RESUMO

This review paper covers the major synthetic approaches attempted towards the synthesis of α-azido ketones, as well as the synthetic applications/consecutive reactions of α-azido ketones.


Assuntos
Azidas/química , Azidas/síntese química , Cetonas/química , Cetonas/síntese química
18.
Pak J Pharm Sci ; 27(3): 469-74, 2014 May.
Artigo em Inglês | MEDLINE | ID: mdl-24811803

RESUMO

Antioxidant and antibacterial potential of different solvent extracts of locally grown Hibiscus rosa-sinensis Linn was evaluated. The antioxidant activity was assessed by estimation of total flavonoids contents, total phenolic contents, DPPH free radical scavenging activity and percentage inhibition of linoleic acid oxidation capacity. Agar disc diffusion method was used to assess antibacterial potential of crude extract of H. rosa-sinensis. The yield of the crude extracts (23.21 ± 3.67 and 18.36 ± 2.98% in 80% methanol and ethanol solvents was calculated, respectively. Methanol and ethanol extract of H. rosa-sinensis showed total phenolics 61.45 ± 3.23 and 59.31 ± 4.31 mg/100g as gallic acid equivalent, total flavonoids 53.28 ± 1.93 and 32.25±1.21 mg/100g as catechine equivalent, DPPH free radical scavenging activity 75.46±4.67 and 64.98 ± 2.11% and inhibition of linoleic acid oxidation potential 75.8 ±3.22 and 61.6 ± 2.01% respectively, was measured. Antibacterial study against three human pathogens such as staphlococus sp. Bacillus sp. and Escherichia coli showed growth inhibitory effect in the range of 12.75 ± 1.17 to 16.75 ± 2.10 mm. These results showed H. rosa-sinensis indigenous to Kallar Kahar and its allied areas bear promising medicinal values and could be used for developing herbal medicines to target oxidative stress and infectious diseases.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Hibiscus , Extratos Vegetais/farmacologia , Flavonoides/análise , Flores , Depuradores de Radicais Livres/farmacologia , Hibiscus/química
19.
Chem Cent J ; 8: 74, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25685184

RESUMO

BACKGROUND: It is seen that the regioselective functionalizations of halogenated heterocycles play an important role in the synthesis of several types of organic compounds. In this domain, the Suzuki-Miyaura reaction has emerged as a convenient way to build carbon-carbon bonds in synthesizing organic compounds. Some of the most important applications of these reactions can be seen in the synthesis of natural products, and in designing targeted pharmaceutical compounds. Herein, we present the regioselective synthesis of the novel series of 2-(bromomethyl)-5-aryl-thiophenes 3a-i, via Suzuki cross-coupling reactions of various aryl boronic acids with 2-bromo-5-(bromomethyl)thiophene (2). RESULTS: The synthesized compounds were screened for their haemolytic and antithrombolytic activities. The novel compounds 3f, 3i showed highest 69.7, 33.6% haemolysis of blood cells, respectively. The antithrombolytic activity of the compounds was found to be within low to moderate against human blood clot. The compound 3i showed potent clot lysis (31.5%). CONCLUSIONS: Considering these results, it is concluded that the synthesized compounds can be used as a promising source of therapeutic agents.

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