Aravinda Pai

Manipal Academy of Higher Education | MAHE · Manipal College of Pharmaceutical Sciences (MCOPS)

Calixarenes have always captured the attention of several researchers. They have the ability to entrap multiple molecules and form inclusion complexes with drugs due to their unique structure. Due to this property, they are being widely used in the development of several classes of drugs, most notably anticancer drugs. This review attempted to summ...

Oxadiazoles, a class of five membered heterocyclic azoles, are considered to be a versatile scaffold and is found to be a core moiety of various pharmaceutically active agents.Oxadiazoles are known to inhibit alpha-amylase and alpha-glucosidase enzyme which is rational approach for selecting oxadiazole as antidiabetic agents in controlling postpran...

As compared to standard medicinal compounds, hybrid molecules that contain multiple biologically active functional groups have greater affinity and efficiency. Hence based on this concept, we predicted that a combination of thiazolidinediones and 1,3,4-oxadiazoles may enhance α-amylase and α-glucosidase inhibition activity. A series of novel 3-((5-...

It is well known that microorganisms are omnipresent. It would be fascinating for scientists to encounter organisms that not only grow in normal conditions but are able to thrive in extreme conditions. Such organisms are suitably termed extremophiles including thermophiles, psychrophiles, alkaliphiles, piezophiles, and marine extremophiles, to name...

The classical anticancer agents do not have their efficacy on inhibiting the G2 phase of the cell cycle. There are a very few reports available on drugs that work at G2 phase. Flavopiridol is one such drug candidate. In the current study, we sought to make analogues of flavopiridol. Still, the conditions used during their synthesis were unfavourabl...

Alzheimer's is the typical type of dementia that affects Senior people and is an irrevocable, progressive neurodegenerative disorder. The characteristic symptoms are loss of memory, behavioral disturbances, mood and personality swing, followed by diminished cognitive performance. There is no permanent remedy for AD and the existing drugs in the tre...

In this present study, a new co-crystal of azithromycin with nicotinamide and naringenin has been developed with improved solubility. Azithromycin is a class II drug with poor aqueous solubility; hence an attempt has been made to improve its solubility through co-crystallization technology. In this study, the coformers selected were nicotinamide an...

Microbial enzymes are known for their versatile catalytic property. With the advent of enzyme engineering, stringent environmental rules restraining the use of toxic chemicals, and need for the sustainable resource, there is a mounting demand for the utilization of these enzymes. Classified under Gram-positive filamentous bacteria, actinomycetes ar...

An RP-HPLC technique was used to produce a cost-effective simultaneous quantification of Etoricoxib and Paracetamol in combined pharmaceutical tablet dosage forms. The approach was validated for Etoricoxib and Paracetamol using ICH recommendations over a range of 20-120ppm and 20-200ppm, respectively. At a temperature of 250C±0.50C, an analytical c...

The United Nations General Assembly (UNGA) has designed a blueprint for achieving sustainable development which is intended to be achieved by 2030. The Sustainable Development Goals (SDGs) are interlinked with 17 goals that have been set up for a better and more sustainable future for all. To achieve these goals, the practices and principles associ...

A robust, sound, and comprehensive waste management system is a fundamental aspect to achieve environmental sustainability and development. Though as individuals, people are aware and conscious of this particular aspect of waste management, there have not been any concrete steps taken to tackle the issue. As per a statistical report from World Bank...

In an effort towards the discovery of new chemical entities to combat antimicrobial resistance, a series of novel 2,4,5- triphenyl imidazole derivatives were designed to target lanosterol 14α demethylase to screen the molecules for their antimicrobial potential. The designed molecules were synthesized and characterized by MS, FTIR, and NMR. The com...

Synthesis and screening of a series of new coumarin derivatives coupled with thiazole are performed for their antimicrobial properties. A series of new thiazolyl coumarin derivatives were synthesized upon refluxing 3-bromoaceytl coumarin, substituted benzaldehyde and thiosemicarbazide in the presence of glacial acetic acid. Substituted 3-acetyl cou...

Coconut water widely consumed as a health drink by people around the world. This led to an urge to study various properties of Cocus nucifera. We evaluated anti oxidant and phyto chemical constituents of two variety of coconut the yellow and green variety. Phytochemical assays showed the presence of terpinoids, alkaloids, resin, sugars, steroids, g...

Five-feature pharmacophores consisting of a dual hydrogen bond acceptor site and three aromatic rings as characteristic pharmacophoric features were developed for a novel series of hydroxamic acid derivatives for the inhibition of HDAC 8. The hypothesis AARRR1 resulted in a statistically significant atom based 3D QSAR model with 0.7119 as R2 (regre...

Pharmacological treatment for BPH includes 5-α reductase inhibitors as Finasteride and Dutasteride as a monotherapy or in combination with antimuscarinic drugs, alpha-blockers, 5-phosphodiesterase inhibitor drugs. Androgen receptor inhibitors revealed several adverse events as decreased libido, erectile dysfunction, ejaculatory dysfunction, and gyn...

In the present review, an attempt has been made to summarize the development of various Tankyrase inhibitors, focussing on Wnt/beta-Catenin pathways along with other cancer targets. The last decade witnessed a plethora of research related to the role of various genetic and epigenetic events that are responsible for the progression of multistage can...

In the present study, a series of novel substituted pyrazole chalcones and pyrazole oximes (CF 1-15) were synthesized and characterized. Logp values were determined to assess their hydrophobicity. MTT (methyl tetrazolium) assay was performed on A-549 (lung cancer) cell lines. The MTT assay results showed the effect of various substituents on the py...

Androgen signaling is essential for the development of prostate cancer (PCa) initiated from prostatic basal cells with collocation of androgen receptor gene mutations. Phytoestrogens, the naturally occurring compounds are AR antagonist. These compounds downregulate prostate-specific antigen (PSA) expression and cell proliferation. Thus, this gives...

In the current research work, a new co-crystal of ceritinib with nicotinamide and quercetin hydrate was prepared with increased solubility. Ceritinib belongs to BCS class IV drug which having poor permeability and low aqueous solubility that leads to poor oral bioavailability. Thus, an endeavor has been made by the co-crystal technique to increase...

Caffeine is an alkaloid and well-known CNS stimulant usually added in most foods and beverages. Caffeine had drawn more attention in many nutritional products due to its stimulant effect on CNS, so that the product to which caffeine is added becomes more popular in the market. The present work was carried out to extract and estimate the amount of c...

Background With the rapid evolution in advanced computer systems and various statistical algorithms, it is now a day possible to analyze complex biological data. Bioinformatics is an interface between computational and biological assemblies. It is applied in various fields of biological as well as medical sciences. Aim The manuscript aims to summa...

Background Since last decades, breast cancer has emerged as one of the most aggressive form of cancer causing highest mortality rates. The synthetic drugs available for the treatment of breast cancer either have high toxicity or becoming resistant. In view of this, researchers are constantly in search of natural drugs that can control aggressive br...

Asparaginase, derived from microbial origin hydrolyses L-asparagine to L-aspartic acid. The enzyme finds principal use in the treatment of Acute Lymphoblastic Leukemia during childhood that primarily occurs between two to ten years of age. L-Asparaginase finds its use in management of haemopoietic disorders especially in pediatrics that is caused d...

Diabetes, a metabolic disorder responsible for worldwide pandemic wherein, epidemiological studies suggests around 425 million people around the globe have been diagnosed for diabetes. Type 1 diabetes mellitus (T1DM) indicates a complete insulin deficiency which threatens lifestyle whereas, Type2 diabetes accounts to the obesity and lack of exercis...

Introduction: In the present study cocrystal of Cytarabine with L-Tartaric acid and nicotinamide and cocrystal of Doxorubicin HCl with Maraviroc has been prepared. The Cytarabine and Doxorubicin HCl are potential anticancer drugs used in the treatment of various types of cancer. Though they have certain advantages, they also have issues like low or...

In this present study a new co-crystals of zoledronic acid with DL-tartaric acid and nicotinamide has been developed with improved solubility. Zoledronic acid is a class III drug with poor oral bioavailability due to its poor permeability and low aqueous solubility; hence an attempt has been made to improve its solubility by co-crystallization tech...

Extensive exploration of soil microorganisms in search of novel metabolites have edified researchers on the available natural products for drug discovery. Actinomycetes are filamentous Gram positive bacteria capable of producing wide array of bioactive metabolites. High GC content in the DNA, makes the organism unique and peculiar from other microo...

Methylcobalamin is a highly photolabile and unstable molecule and hence, studies regarding photodegradation of methylcobalamin were carried out.. In order to investigate the stability studies, the drug was subjected to photodegradation by exposing it to different light conditions in the validated photostability chamber as per ICH Q1B guideline. The...

In the present study, we have applied seven available similarity based binary fingerprints as implemented in the new cheminformatics package Canvas, on a validated dataset for the test compounds selectively inhibiting CDK2/Cyclin A. The fingerprint methods used were: Linear, Dendritic, Radial, MOLPRINT2D, Pairwise, Triplet, and Torsion. Out of the...

Aim/Background: The anomalous production of dihydrotestosterone (DHT) observed in benign prostatic hyperplasia and prostate cancer particularly in tissues of the prostate gland. The primary male sex hormone, testosterone (T) is improved to a metabolite in cells by 5a-reductase (5aR) type II enzyme through NADPH. A metabolite is DHT which is more po...

A robust and reliable 3D QSAR model which is pharmacophore based has been developed in the present study, based on reported sequence of purine analogues for the inhibition of serine threonine class of cancer drug target. The present model showed statistical significance with regression coefficient value of r 2 = 0.98 and cross validation coefficien...

Co-crystal synthesis has become a field of high interest in the last decade. This category of solid forms has a variety of applications in industries such as textile, paper and electronics. For many purposes co-crystals will have superior properties in comparison to traditional salt crystals. This review article will focus on the application of co-...

In the present study, five important binary fingerprinting techniques were used to model novel flavones for the selective inhibition of Tankyrase I. From the fingerprints used: the fingerprint atom pairs resulted in a statistically significant 2D QSAR model using a kernel-based partial least square regression method. This model indicates that the p...

In the present review, the application of finger-print based molecular similarity applications and their role in drug design is discussed briefly. Finger-print based molecular similarity methods are gaining importance in the modern drug discovery owing to their statistical accuracy and reliable predictivity. Some of the important similarity coeffic...

In the present review, the application of fingerprint based molecular similarity applications and their role in drug design is discussed briefly. Fingerprint based molecular similarity methods are gaining importance in the modern drug discovery owing to their statistical accuracy and reliable predictivity. Some of the important similarity coefficie...

In recent years, drugs from natural sources are becoming important owing to their potency and less toxicity. Natural products from marine microorganisms and marine algae are one of the highly explored areas in natural product research. Plenty of marine natural product being isolated and is showing a wide array of biological activity. The present re...

The present study envisages a fast and reliable 3D QSAR approach utilising pharmacophore mapping for the identification of specific inhibitors for the CDK2 inhibitors belonging to the kinase class. The model generated resulted in a statistically significant 3D QSAR equation with regression coefficient value of ( r² = 0.8131) and cross validation co...

The following study was done to establish that etravirine, which is an anti-human immuno deficiency virus drug, when produced as co-crystals helps in improving its solubility. The produced cocrystals were also characterized. According to the Biopharmaceutical Classification System, etravirine is categorised in class IV category; that is; a drug hav...

A series of novel flavone-4-oximes were synthesized by the oximation of substituted flavones. The synthesized compounds were characterized by various spectrochemical methods including IR, MS and NMR spectroscopy. Out of the 14 test compounds screened for their antioxidant activity, compounds such as JGS-VI (a N,N dimethyl benzaldehyde derivative) a...

Etravirine is a drug used alongside other medication in the treatment of HIV and is a non-nucleoside reverse transcriptase inhibitor. It is a BCS class IV drug, having low solubility and high permeability (Drugbank, https://www.drugbank.ca/drugs/DB06414) [1]. As a result, large doses of the drug are required for treatment. Two pills have to be take...

Alzheimer’s disease (AD) is one among the common type of dementia in elder people above the age group of 65 years. This was once considered a rare disorder but in recently was considered as a great threat and risk factor to the elderly community above 60 years. AD is also considered a highly prevalent neurodegenerative disease. AD is characterized...

The last decade witnessed several scientific experiments with the aim to correlate the structure of chemical entities to their biological activities, toxicities and other molecular properties. Chemical species are mathematically represented based on specified algorithms in molecular descriptors. They play extremely important role in the field of ch...

The present study aimed to identify the photochemical constituents and possible microbicidal potential of ethanol and aqueous extract of Acalypha indica leaf extract on various gut pathogens. Shade dried leaves of Acalypha indica were extracted with solvents of increasing polarity. In vitro anti microbial activity of the water and alcoholic extract...

The subsequent artefact entail of extremely subtle and informal Reversed phase HPLC (RP-HPLC) technique for approximation ofMethylcobalamin in large quantity. Shimadzu LC-20-AD(Kyoto, Japan), with auto sampler and (PDA/UV) detector was used for the separation of Methylcobalamin.C18 Hypersil BDS (5.0 micron,150 x 4.6mm) column was aimed at the separ...

In the present study a new co-crystal of Ticagrelor with L-Tartaric acid has been prepared with improved solubility. Ticagrelor is a class VI drug with poor solubility and permeability; hence an attempt has been made to improve its solubility by co-crystallization technology.A co-crystal is a structurally homogeneous crystalline material containing...

The subsequent artefact entail of extremely subtle and informal Reversed phase HPLC (RP-HPLC) technique for approximation ofMethylcobalamin in large quantity. Shimadzu LC-20- AD(Kyoto, Japan), with auto sampler and (PDA/UV) detector was used for the separation of Methylcobalamin.C18 Hypersil BDS (5.0 micron,150 x 4.6mm) column was aimed at the sepa...

This study establishes that etraverine, an anti human immuno deficiency virus drug, is produced as cocrystals to improve the solubility of the same by cocrystallisation methods and characterization of the cocrystals formed. Etraverine belongs to the class IV category as per the Biopharmaceutical Classification System which are basically classified...

Pharmacophore based screening was undertaken for a set of 30 flavones exhibiting Tankyrase I inhibitory activity. The two isoenzymes Tankyrase I and Tankyrase II share 80% sequence homology. This gives rise to the fine tuning required in the designing of small molecules wchich can selectively inhibit one or the other. In a recent study it was repor...

Drug discovery based on the pharmacophore searching is used in the leading modification and searching programmes. In this context, it was thought appropriate to extensively perform pharmacophoric searching in our laboratory for identifying an ideal scaffold for designing an anticancer candidate that eventually could emerge out to become a CDK inhib...

Terminalia tomentosa bark. Belongs to the family Combretaceae. Bark is astringent and useful in the treatment of ulcers, vata, fractures, hemorrhages, bronchitis and diarrhea.This study establish the antiinflammatory activity of ethanolic (TEA) and aqueous (TEW) of T. tormentors aback extracts in in-vitro methods by Inhibition protein denaturation...

The western Ghats of India present Pharmacognosists and botanist a rich source of biological diversity to explore their unearthed potential. V. indica, one among the thousands of such plant growing in the southern states of India especially in Kerala, Karnataka and Tamil Nadu, at about 750 m altitude is a slow growing plant of Dipterocarpaceae fami...

Introduction: Luteolin, a natural flavonoid is known to possess variety of pharmacological activity, particularly growth inhibition. Reports are available to substantiate the interaction of luteolin with tankyrase II, one of the key enzymes responsible for sustenance of telomeres and involved in promoting cellular function. Objective:In our study,...

The following article consist of highly sensitive and easy RP-HPLC method to estimate Ticagrelor in bulk. Ticagrelor was separated using Shimadzu LC-20-AD with auto sampler and PDA/UV detector. The separation was achieved using a C18 Vydac Monomeric 120A (5.0 micron, 250 x 4.6mm) column. Acetonitrile: Water Milli Q (60:40 v/v) at a flow rate of 1.0...

Epigenetic modulation of gene expression has drawn enormous attention among researchers globally in the present scenario. Since their discovery, Jmj-C histone demethylases were identified as useful markers in understanding the role of epigenetics in inflammatory conditions and in cancer as well. This has created arousal of interest in search of sui...

Metabolic disorder characterized by hyperglycemia and glycosuria with disturbed carbohydrate metabolism or metabolism of fats and amino acid resulting from defects in insulin secretion or insulin sensitivity leads to a condition called diabetes mellitus. In recent years, the peroxisome proliferatoractivated receptor γ (PPARγ) has become a validated...

Celastrus paniculatus, commonly known as Malkangani and Jyothishmati. Which is a traditional medicinal plant used in Ayurveda used for various purposes as a memory enhancer, analgesic, antiepileptic agent, anti-inflammatory and sedative. The seed extracts are extensively investigated for various neuropharmacological actions and other reports are av...

A series of novel flavone-4-oximes were synthesized by the oximation of substituted flavones. The synthesized compounds were characterized by various spectrochemical methods including IR, MS and NMR spectroscopy. Out of the 14 test compounds screened for their antioxidant activity, compounds such as JGS-VI (a N,N dimethyl benzaldehyde derivative) a...

Cancer is a complex disease characterized by a loss in the normal cell regulatory mechanisms that govern cell survival, proliferation, and differentiation. Current chemotherapeutics, as anticancer agents, are developing resistance to single drug and also to treatment therapies involving multiple drugs. Cross resistance associated with the specifici...

Background Anisochilus carnosus (L.f.) wall (Lamiaceae), an annual herb which grows at high altitude is used extensively in folk medicine for the treatment of ailments such as gastric ulcer and skin diseases. The aim of our study was to evaluate the anticancer activity of different extracts of the leaves of A.carnosus. An attempt was also made to e...

The chemical class of benzopyrone consists of a large number of compounds possessing the benzene ring fused with the oxygen containing pyrone ring. This class is further divided into the benzo-γ-pyrone i.e. flavonoids and the benzo-α-pyrone i.e. coumarins. Coumarins, the 2H-chromen-2-one and its related analogues exhibit a multitude of biological a...

In the present work, a series of novel Schiff's bases of 2-Quinolones were synthesized and characterized. The synthesized compounds were screened for their antibacterial activity against different bacterial strains. Out of the 15 compounds screene d for the antibacterial activity,3 compounds (JMB3, JMB11, JMB13) showed antibacterial activity agains...

When more number of bacteria are becoming resistant to antibiotics, the development of new disease-fighting agents has become essential. In this context, enzybiotics are alternative possibilities in fighting bacterial or fungal infections diseases. The applications of enzybiotics include different forms of prophylaxis and treatment of microbial inf...

A series of novel Schiff’s bases of 2-Quinolones have been synthesized using Coumarin 4 aldehydes and different substituted amines as starting materials under conventional heating method and were obtained in good yields. The synthesized compounds were screened for their anti-oxidant activity by DPPH· method and were also tested for their antiprolif...

Benzothiazole nucleus is present in various compounds and it is responsible for diverse biological activities. The present work mainly focused on the benzothiazoles with potential activities that are now in development. The objective of this research work is to synthesize various compounds containing benzothiazole moiety and their derivatives as we...

In the present work a series of novel flavone analogues have been synthesized, characterized by various spectrochemical methods. All the compounds have been evaluated for their antioxidant potency, and screened for antimicrobial activity. Out of the 10 compound synthesized the compounds JAK4 and JAK5 have shown antibacterial activity.

In the present work a series of novel flavone analogues have been synthesized, characterized by various spectrochemical methods. All the compounds have been evaluated for their antioxidant potency, and screened for antimicrobial activity. Out of the 10 compound synthesized the compounds JAK4 and JAK5 have shown antibacterial activity.

In the present research work we have undertaken synthesis of novel coumarin analogues. And the synthesized compounds were characterized by various spectrochemical methods including some of the important physicochemical parameters. Eight of the synthesized compounds have shown free radical scavenging activity by DPPH· and Nitric oxide scavenging act...

Quinazolinone is a versatile lead molecule for designing potential bioactive agents. The compounds that have quinazolin-4-ones moiety are associated with interesting biological activities such as antifungal, antibacterial, antiviral, antitubercular and anticancer. In view of this we have undertaken synthesis of various thiadiazol substituted quinaz...