Rupesh Dudhe
@ghru.edu.in
Professor, School of Pharmacy
G H Raisoni University
EDUCATION
M.Pharm Ph.D.
RESEARCH INTERESTS
pharmacy, validation
Scopus Publications
Scopus Publications
Esra Tariq Anwer, O. Porwal and R. Dudhe
To develop a novel, accurate, precise and linear reverse phase high performance liquid chromatographic (RP-HPLC) methods for quantitative determination of cefotaxime sodium (CFT) in bulk drug and CFT loaded nanoparticles. Different analytical performance parameters such as linearity, precision, accuracy, specificity, limit of detection (LOD) and limit of quantification (LOQ) were determined according to International Conference on Harmonization ICH Q2B guidelines. The RP-HPLC method was developed by the isocratic technique on a reversed-phase Zorbax C18 (250 × 4.6 mm, 5µm) column with mobile phase consisting of phosphate buffer (pH7.4): acetonitrile (80:20v/v) at flow rate of 1.2 ml/min. Detection was carried out using a UV detector at 254nm. The retention time for CFT was 6.580+0.5min. The standard curve was linear over the concentration range of 10-50μg/ml with r2 close to one (0.999). The limit of detection (LOD) and limit of quantitation (LOQ) obtained for CET were 0.100μg/ml and 0.314μg/ml respectively. The developed and validated method was successfully applied for the quantitative analysis of nanoparticle. The high recovery and low relative standard deviation confirm the suitability of the proposed method for determining the assay and in vitro dissolution of a marketed formulation.
Rupesh Dudhe, Anshu C. Dudhe, and Shravan D. Raut
Bentham Science Publishers Ltd.
Background & Objectives: Nitric Oxide (NO) is frequently produced by the enzyme nitric oxide synthase (NOS) and is crucial for the control and effectiveness of the cardiovascular system. However, there is a substantial reduction in NOS activity with aging that can lead to the development of hypertension and other cardiovascular obstacles. Fortunately, NO can also be produced by sequential reduction of inorganic nitrates supplementation. This proves that NO from inorganic nitrate supplements can compensate for inadequate NOS activity, thus providing cardio protective benefits. Discussion: This review focuses on the general information about nitrous oxide, its types and mechanism of action and the fact that overview of inadequate NOS activity for cardio protective benefits was often studied for cardiovascular treatments. Conclusion: We concluded that the natural plant NO is essential for cardiovascular activity to target site with desired concentration. Moreover, the researchers focused on evidence that suggested that nitrate supplementation could help regulate blood pressure, limit progression of atherosclerosis, and improve myocardial contractility in both healthy individuals and those with cardiovascular diseases.
Anshu Chaudhary Dudhe, Rupesh Dudhe, Omji Porwal, and Gayatri katole
Bentham Science Publishers Ltd.
Abstract: Dihydropyrimidine derivatives are the most important scaffolds due to structural similarities with natural products; it is a heterocyclic compound. The chemistry of Dihydropyrimidine is a growing field. Various reaction schemes for the preparation of Dihydropyrimidines produce different biological effects and offer vast scope in the field of medicinal chemistry. This article's goal is to analyze the work that reported the recent chemistry and pharmacological activities of dihydropyrimidine derivatives.
Lata Potey, Anshu Chaudhary Dudhe, Dhanashri Tumme, Rupesh Dudhea, and Prafulla Sable
Bentham Science Publishers Ltd.
Abstract: The strategy of drug repurposing has been proved successful in response to the current coronavirus pandemic, with remdesivir becoming the first drug of choice, an antiviral drug approved for the treatment of COVID-19. In parallel to this, several drugs, such as antimalarial, corticosteroids, and antibiotics, like azithromycin, are used to treat the severe condition of hospitalized COVID-19 patients, while clinical testing of additional therapeutic drugs, including vaccines, is going on. It is reasonably expected that this review article will deliver optimized and specific curative tools that will increase the attentiveness of health systems to the probable outlook of epidemics in the future. This review focuses on the application of repurposed drugs by studying their structure, pharmacokinetic study, different mechanisms of action, and Covid-19 guidelines, which can potentially influence SARS-CoV-2. For most of the drugs, direct clinical evidence regarding their effectiveness in the treatment of COVID-19 is missing. Future clinical trial studies may conclude that one of these can be more potential to inhibit the progression of COVID-19.
Nitin Kumar, Ankita Bhatnagar, and Rupesh Dudhe
Elsevier BV
Abstract A novel series of 3-(4, 5-dihydro-1-phenyl-5-substituted phenyl-1H-pyrazol-3-yl)-2H-chromen-2-one derivatives were synthesized. In the first step salicylaldehyde was reacted with ethylacetoacetate at room temperature by stirring which gives compound (I). Compound (I) when refluxed with substituted benzaldehyde and diethylamine in the presence of n-butanol for 4–5 h gives substituted derivatives (IIa–d). Compounds synthesized in step 2 when refluxed with phenyl hydrazine in the presence of pyridine for 6–7 h gives the title compounds (IIIa–d). All the synthesized compounds were sent to NCI for anticancer activity. Synthesized compounds were tested for anticancer activity against 60 different cell lines. From the data thus obtained it was observed that simple coumarin ring derivatives were more effective in inhibiting the growth of cancerous cell lines, than coumarin-pyrazoline derivatives. Among all the synthesized compounds, irrespective of compounds having simple coumarin ring and coumarin-pyrazoline combination, compounds IIa–c, IIIb and IIId were potent anticancer agents. Compounds were active for the single dose therapeutic program at the dose of 1.00E-5 molar concentration. The main anti cancer activity is assumed to be due to the presence of the lactone structure in coumarin moiety.
Manjit Jaiswal, Rupesh Dudhe, and P. K. Sharma
Springer Science and Business Media LLC
An advanced mode of drug delivery system has been developed to overcome the major drawbacks associated with conventional drug delivery systems. This review gives a detailed idea about a nanoemulsion system. Nanoemulsions are nano-sized emulsions, which are manufactured for improving the delivery of active pharmaceutical ingredients. These are the thermodynamically stable isotropic system in which two immiscible liquids are mixed to form a single phase by means of an emulsifying agent, i.e., surfactant and co-surfactant. The droplet size of nanoemulsion falls typically in the range 20–200 nm. The main difference between emulsion and nanoemulsion lies in the size and shape of particles dispersed in the continuous phase. In this review, the attention is focused to give a basic idea about its formulation, method of preparation, characterization techniques, evaluation parameters, and various applications of nanoemulsion.
Tejprakash Singh, Rupesh Dudhe, Nitin Kumar, and PramodKumar Sharma
Siree Journals
Aim: It was aimed to synthesise some novel thiazolidinone derivatives and assess them for antidiabetic activity. Material and Methods: A series of substituted 5-ethylidene-2-(phenylimino) thiazolidin-4-ones were prepared by using phenylthiourea (I) as a starting material. Phenylthiourea on reaction with ethylchloroacetate, in the presence of ethanol and fused sodium acetate, gave 2-(phenylimino) thiazolidin-4-one (II), and 2-(phenylimino) thiazolidin-4-one on further reaction with substituted benzaldehyde gave substituted 5-ethylidene-2- (phenylimino) thiazolidin-4-one (III - XVIII). The synthesized compounds were authenticated on the basis of elemental analysis, IR, 1H NMR, and Mass spectral analysis and some of the compounds were selected on the basis of a literature review, to evaluate them for their antidiabetic activity. Results and Conclusion: All The tested compounds 5-(4-fluorobenzylidene)-2-(phenylimino) thiazolidin-4-on (VII) and 5-(4-Methylbenzylidene)-2-(phenylimino)thiazolidin-4-one (X), 5-(2, 4-dinitrobenzylidene)-2-(phenylamino) thiazolidin-4-one (XVII) were found to be ineffective in lowering the blood glucose level.
Anshu Chaudhary, Pramod Kumar Sharma, Prabhakar Verma, Nitin Kumar, and Rupesh Dudhe
Springer Science and Business Media LLC
A novel series of 6-bromo-3-(2-morpholino methyl amino)-6-substituted phenyl pyrimidine-4-yl-2H-chromone-2-one (6aM–6jM) and 3-(2-((piperidine-1-yl)methyl amino)-6- substituted phenylpyrimidin-4-yl)-6-bromo-2H-chromone-2-one (6aP–6jP) have been synthesized from 3-(2-amino-6-pyrimidin-4-yl)-6-bromo-2H-chromen-2-one (5a–5j) which were synthesized from 3-acetyl-6-bromo-2H-chromen-2-one (3). The reactions were carried out by conventional and microwave method. The salient feature of microwave method are rapid reaction rate, cleaner reaction condition, and enhancement in chemical yield compared to conventional method, the structures of the synthesized compounds were characterized by I.R., 1H NMR, 13C NMR, Mass spectroscopic techniques. All the compounds screened at a dose of 20 mg/kg body weight by in vivo analgesic activity. Among all the synthesized compounds, compound 6aP, 6aM, 6cM, 6iM, and 6jM showed significant analgesic activity and compounds 6cM and 6iM showed highly significant activity against the standard drug Diclofenac sodium using acetic acid-induced writhing model. Among all the synthesized compounds which show potent analgesic activity such as 6aP, 6aM, 6cM, 6iM, and 6jM were further evaluated for acute- ulcerogenic activity. Among all compound 6cM and 6iM was found to be most promising analgesic agent devoid of ulcerogenic effects.
Jitendra Kumar Gupta, Pramod K. Sharma, Rupesh Dudhe, Anshu Chaudhary, Avnesh Singh, P. K. Verma, Sambhu C. Mondal, Rakesh Kumar Yadav, and Shivjee Kashyap
Springer Science and Business Media LLC
A novel series of 2-amino-4-(coumarin-3-yl)-6-substituted phenyl pyrimidines (5a–h) were synthesized from 3-acetylcoumarin (3). The structures of the synthesized compounds were elucidated by I.R., 1H NMR, 13C NMR, and Mass spectroscopic techniques. The synthesized compounds were screened for in vivo analgesic activities at a dose of 20 mg/kg body weight (b.w). Among them, compounds 5b and 5h exhibited significant analgesic activity comparable with control as well as standard drug diclofenac sodium using acetic acid-induced writhing model.
Shiv Jee Kashyap, Vipin Kumar Garg, Pramod Kumar Sharma, Nitin Kumar, Rupesh Dudhe, and Jitendra Kumar Gupta
Springer Science and Business Media LLC
In the last few decades, a lot of work has been done on thiazole ring to find new compounds related to this scaffold to act as antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective, and antitumor or cytotoxic drug molecules with lesser side effects. This review presents the up to date development on the design and development of different thiazole derivatives.
Rupesh Dudhe, Anshu Chaudhary, ShivJee Kashyap, PramodKumar Sharma, JitendraKumar Gupta, and Prabhakar Verma
Siree Journals
Background: Pyrimidine and fused pyrimidine derivatives play an important role in therapeutic strategies. It is known to be most prominent structures found in nucleic acid, including uracil, thymine, cytosine, adenine, and guanine, which are fundamental building blocks for deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). Materials and Methods: A series of 3-[2-amino-6-(substituted)-pyrimidin-4-yl]-6-(substituted)-2H-chromen-2-one derivatives were prepared by reacting salicylaldehyde with ethylacetoacetate in the presence of piperidine by Knoevenagel reaction as a starting material. The chemical structures were confirmed by means of FTIR (Fourier Transform InfraRed Spectrophotometer-8400S), 1H NMR, and elemental analysis. The data of these synthesized compounds were submitted to National Institute of Health, USA, under the drug discovery program of NCI (National Cancer Institute) and screened for anticancer activity at a single high dose (10−5 M) in full NCI 60 cell lines. Results: Unfortunately, the selected compounds have not shown any potent significant anticancer activity in the NCI 60 cell line screening. Conclusion: The compound (T2) found to be most efficient anticancer activity with selective influence on breast cancer cell lines, especially on MCF7 cell line with a growth percentage of 33.63.
S. Sharma, P.K. Sharma, N. Kumar, and R. Dudhe
Elsevier BV
Tuberculosis (TB), a contagious infection caused by Mycobacterium tuberculosis, still remains the leading cause of the worldwide death among the infectious disease. Different moieties like pyrazoline, benzimidazol, purines, thiazole, flouroquinolones, quinoxaline, oxadiazol, pyrazol, thiozolidinones and azetidinones have been studied, synthesized and evaluated worldwide against M. tuberculosis to show their antitubercular activity.