Alex Joseph

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

M-Pharm, Ph.D

About

86
Publications
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894
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Publications

Publications (86)
Article
A new series of 2‐aminobenzothiazole derivatives was designed, synthesized and evaluated for their anticancer activity against the MCF7, MDAMB‐231, and HepG2 cancer cell lines. All synthesized derivatives (8a–8n) demonstrated moderate to high anticancer activity against the tested cell lines. As the most potent compound in the series, compound 8i d...
Article
Background: Non-small cell lung cancer (NSCLC) is a deadly disease that affects millions globally and its treatment includes surgery, chemotherapy, and radiotherapy. Chemotherapy and radiotherapy have many disadvantages, which include potential harmful side effects. Due to the widespread use of drugs in lung cancer, drug treatment becomes challengi...
Article
Addressing the increasing incidences of cancer worldwide along with the multifaceted problem of drug resistance via development of new anticancer agents has become an essential goal. Due to the known cytotoxic effects and reported Akt inhibitory potential of azaindoles we designed a new framework incorporating the structural features of rosuvastati...
Article
Cancer is one of the top causes of death worldwide, with over a million fatalities reported each year. Anti-cancer drugs are crucial for cancer treatment, but the growth of drug resistance, side effects, and multidrug-resistant due to mutations have created substantial demands for new, effective, and safe compounds with diverse mechanisms of action...
Article
Background: Despite recent advances in the treatment of squamous cell skin cancer (SCSC), the disease persists, and treatment resistance develops. Thus, identifying new targets and developing new therapeutic approaches showing low vulnerability to drug resistance is highly needed. Purpose: This study aimed to reveal novel targeted phytotherapeutic...
Article
Cancer is one of the leading causes of death. Globally a huge number of deaths and new incidences are reported annually. Heterocyclic compounds have been proved to be very effective in the treatment of different types of cancer. Among different heterocyclic scaffolds, quinazoline and quinazolinone core were found versatile and interesting with many...
Article
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Inflammatory bowel disease is a chronic disorder of the large intestine with the prevalence of approximately 400 cases in 100000, and it is rising day by day. However, several drugs like sulfasalazine (com-posed of sulfapyridine and 5-aminosalicylic acid or 5-ASA), corticosteroids, and immunosuppressants manage the disease. But there are no absolut...
Poster
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Drug repurposing approach for Inflammatory Bowels Disease by USFDA approved drugs by in silico method using Maestro, Schrodinger.
Article
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Due to complicated anatomical and physical properties, targeted drug delivery to ocular tissues continues to be a key challenge for formulation scientists. Various attempts are currently being made to improve the in vivo performance of therapeutic molecules by encapsulating them in various nanocarrier systems or devices and administering them via i...
Article
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Magic spot synthetases are emerging targets to overcome persistence caused by stringent response. The 'stringent response' is a bacterial stress survival mechanism, which results in the accumulation of alarmones (also called Magic spots) leading to the formation of dormant persister cells. These 'sleeper cells' evade antibiotic treatment and could...
Article
Pyrimidine is an aromatic and heterocyclic organic compound containing a 6-membered ring consisting of four carbon and two nitrogen atoms on alternative positions. Pyrimidine scaffolds described theirexistence inthe medicinal chemist's cause for their synthesizing practicability and nonpoisonous nature. However, the reason behind neurological disor...
Article
Gold nanoparticles have found a wide range of application in biomedical sciences. Unique properties of these metal nanoparticles include surface plasmon resonance and size dependent colour change. Various molecules have been functionalized on the gold nanoparticles surface but carbohydrates have garnered attention due to their properties and their...
Article
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COVID-19, a respiratory pandemic associated with morbidity and mortality due to the lack of FDA approved drugs for the appropriate preventive or treatment strategies. Repurposed drugs such as antiviral and antimalarials are in clinical trials for the development of novel therapeutic agents for the treatment of SARS-CoV-2 infection. The main proteas...
Article
In the present work, lactoferrin (Lf) based nanoparticle incorporated self-supporting gel encapsulating a flavonoid, quercetin (Q), was developed. The complex formation between Lf and Q was assessed using molecular docking and dynamics simulation that lactoferrin and quercetin showed strong interaction and binding supporting hydrophobic interaction...
Article
Pyrimidine is an aromatic and heterocyclic organic compound containing a 6-membered ring consisting of four carbon and two nitrogen atoms on an alternative position. Pyrimidine scaffolds described its existence between the medicinal chemist’s cause of its synthesizing practicability and nonpoisonous nature. However, the reason behind the neurologic...
Article
As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivatives are still interesting and essential. Pyrazole, a five-member heteroaromatic ring with two nitrogen atoms, has a major impact on chemical industries as well as pharmaceutical industries. Due to its wide range of biological activities against various d...
Article
Full-text available
TSPO-associated protein 1 (TSPOAP1) is a cytoplasmic protein and is closely associated with its mitochondrial transmembrane protein partner translocator protein (TSPO). To decipher the canonical signalling pathways of TSPOAP1, its role in human diseases and disorders, and relationship with TSPO; expression analyses of TSPOAP1- and TSPO-associated h...
Article
The Sonochemical synthesis of a library of 3-methyleneisoindolin-1-one based novel small molecules derived from rosuvastatin designed as potential anticancer agents was undertaken. A Cu-mediated coupling-cyclization strategy was employed to prepare this new class of compounds in a single pot with notable regioselectivity. The use of a terminal alky...
Article
Full-text available
Recently, the pandemic outbreak of a novel coronavirus, officially termed as severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), indicated by a pulmonary infection in humans, has become one of the most significant challenges for public health. In the current fight against coronavirus disease-2019, the medical and health authorities across...
Article
COVID-19 is a global pandemic, primarily affecting the pulmonary system and its effects on other systems are not certain. Coronavirus, the causative organism, binds with angiotensin-converting enzyme 2 (ACE2) receptors in the lungs and produces pneumonia-like symptoms. ACE2 is highly expressed in the lungs produces pneumonia-like symptoms. Other th...
Article
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Black Phosphorus is one of the emerging members of two dimensional (2D) materials which has recently entered the biomedical field. Its anisotropic properties and infrared bandgap have enabled the researchers to discover its applicability in several fields including, optoelectronics, 3D printing, bioimaging, and others. Characterization techniques l...
Article
NLRP3 inflammasome activation and subsequent release of IL-1β are being explored as a causal pathology for inflammatory and autoimmune disorders. Modulation of this pathway by the compounds from natural sources may provide a better targeted approach with improved therapeutic outcome. The study was carried out to test the ability of phenylpropanoic...
Article
The current review focuses towards the advancements made in the past decade in the field of nanotechnology for the early Alzheimer’s disease (AD) diagnosis. This review includes the application of nanomaterials and nanosensors for the early detection of the main AD biomarkers (amyloid beta, phosphorylated tau, apolipoprotein E4 allele or APOE4, mic...
Article
Diabetes is a chronic progressive metabolic disease caused by insulin deficiency or insulin resistance. In spite of the availability of several antihyperglycaemics, there is a need for the development of safer antidiabetic drugs due to their undesirable effects. Sodium-glucose cotransporter-2 inhibitors are a class of antidiabetics, which hinder th...
Article
Background: Presence of residual solvents in pharmaceuticals can be a potential risk factor to human health because of its toxicity. Gas chromatography used for its excellent separation abilities and lower limit of detection. Racecadotril, an antidiarrheal drug, reported having four residual solvents, namely n-Hexane, isopropyl alcohol, toluene and...
Article
Alzheimer’s disease (AD) is a complex neurodegenerative disease which leads to insidious deterioration of brain function and is considered the sixth leading cause of death in the world. Alzheimer’s patients suffer from memory loss, cognitive deficit and behavioral changes; thus, they eventually follow a low-quality life. AD, considered as a multifa...
Article
Pandemic coronavirus disease-2019, commonly known as COVID-19 caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is a highly contagious disease with a high mortality rate. Various comorbidities and their associated symptoms accompany SARS-CoV2 infection. Among the various comorbidities like hypertension, cardiovascular disease a...
Article
Influenza viruses are known to cause acute respiratory illness, sometimes leading to high mortality rates. Though there are approved influenza antivirals available, their efficacy has reduced over time, due to the drug resistance crisis. There is a perpetual need for newer and better drugs. Drug screening based on the interaction dynamics with diff...
Article
Background Over the last few decades, there has been a growing interest in Two-Dimensional Liquid Chromatography (2D-LC). This advanced technology has become a relevant solution for solving all the analytical challenges encountered in the pharmaceutical industry. The primary purpose of this review is to give a brief account of the developing techni...
Article
A new class of 3-substituted isocoumarin/3-alkylidenephthalide based novel small molecules derived from rosuvastatin were designed and synthesized via the ultrasound assisted Cu-mediated coupling-cyclization in a single pot with remarkable regioselectivity. The phthalides were generally obtained at lower temperature whereas the use of elevated temp...
Article
Drug‐Target interaction (DTI) plays a crucial role in drug discovery, drug repositioning and understanding the drug side effects which helps to identify new therapeutic profiles for various diseases. However, the exponential growth in the genomic and drugs data makes it difficult to identify the new associations between drugs and targets. Therefore...
Article
A-ring modifications of betulinic acid isolated from Diospyros peregrina was carried out and the chemically modified derivatives were characterized by spectroscopic methods. Chemically modified betulinic acid analogues were subjected to molecular docking studies on topoisomerase-1 and were evaluated for in vitro and in vivo anticancer activity. In...
Article
An improved process for the synthesis of latanoprost having excellent optical purity (de 99.9%, [α]D²⁰ = +35.37° (c = 0.90, acetonitrile)) without use of preparative HPLC is described. This process involves effective purification of hydroxyl intermediate (5A) through solvent crystallization followed by inhibition of inversion of the chiral center a...
Article
Full-text available
Currently many people with epilepsy do not have seizure control even with the best available medications. Moreover various antiepileptics have adverse cognitive impact with other side effect. Thus, need for new antiepileptic drugs still remains challenge. However, many of the natural components have antiepileptic action and this fact remains scient...
Article
Currently many people with epilepsy do not have seizure control even with the best available medications. Moreover various antiepileptics have adverse cognitive impact with other side effect. Thus, need for new antiepileptic drugs still remains challenge. However, many of the natural components have antiepileptic action and this fact remains scient...
Article
Para-methoxycinnamic acid (PMCA) and Ethyl-p-methoxycinnamate (EPMC) are reported to possess neuroprotective effect in reversing an acute memory deficit. However, there is a dearth of evidence for their therapeutic effect in chronic memory deficit. Thus, there is a scope to study these derivatives against the chronic model of cognitive dysfunction....
Article
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The enzyme tyrosinase regulates melanogenesis and skin hyperpigmentation by converting L-3,4-dihydroxyphenylalanine (L-DOPA) into dopaquinone, a key step in the melanin biosynthesis. The present work deals with design and synthesis of various oxindole-based chalcones as monophenolase and diphenolase activity inhibitors of tyrosinase. Among the scre...
Article
Full-text available
We had previously demonstrated the anti-diabetic potential and pancreatic protection of two thiazolidin-4-one derivatives containing nicotinamide moiety (NAT-1 and NAT-2) in STZ-induced diabetic mice. However, due to the limitations of the STZ model, we decided to undertake a detailed evaluation of anti-diabetic potential of the molecules on a high...
Article
The 3-substituted oxindole derivatives were designed, synthesized, and evaluated for antidepressant activity by employing forced swimming test, tail suspension test, and MAO-A inhibition assay. Results of biological studies revealed that the majority of compounds exhibited potent to moderately potent activity and among them, 12 displayed potency co...
Article
Full-text available
Marsilea quadrifolia Linn. (MQ) has been used for insomnia and epileptic disorders in traditional Indian medicine. The present study is to isolate the active component responsible for antiepileptic property of MQ by evaluating its ability to minimize the reactive oxidative damage in brain due to chronic epilepsy in rat. 1- Triacontanol cerotate (1T...
Article
Full-text available
Context: The study was aimed to develop a polymeric nanoparticle formulation of anticancer drug carboplatin using biodegradable polymer polycaprolactone (PCL). The formulation is intended for intranasal administration to treat glioma anticipating improved brain delivery as nasal route possess direct access to brain and nanoparticles have small siz...
Article
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The flavone moiety is a potential pharmacophore known for its diverse range of pharmacological activities. Aminoflavones have recently been the subject of considerable attention as lead molecules in several cancer research projects. Imidazolidinone heterocycles represent another biologically active scaffold with known cytotoxic properties. In an at...
Article
Abstract A series of novel 5-alkyl/aryl thiadiazole substituted thiazolidin-4-ones were synthesized by a two-step process. In the first step, 5-alkyl/aryl substituted 2-aminothiadiazoles were synthesized, which on reaction with substituted aromatic aldehydes and thioglycolic acid in the presence of dicyclohexylcarbodiimide afforded thiazolidin- 4-o...
Article
Nuclear factor-kappaB (NF-κB) has been reported to regulate various genes involved in cancer and inflammation. Accordingly, drugs suppressing or inhibiting NF-κB may possess both anti-inflammatory and anticancer properties. A library of quinolone substituted thiazolidin-4-ones was docked into the active site of NF-κB and the top-ranked 31 compounds...
Article
Full-text available
1,5-Benzodiazepines and its derivatives constitute an important class of heterocyclic compounds which have proven its medicinal identity as anticancer, antioxidant, cardiovascular agents, viral infection, anticonvulsant, analgesic, sedative, antidepressive, and hypnotic agents. Keeping this in mind, the current research work is to synthesize 2,3-Di...
Article
Full-text available
Background:Diospyros peregrina (Ebenaceae) is a medium-sized evergreen tree having ethnomedicinal significance as an aphrodisiac, astringent, bactericide and for the treatment of diarrhoea, cholera, dysentery, fever, malaria and diabetes. Objectives: To evaluate the anti-oxidant and anti-cancer activity of different extracts and fractions of mature...
Article
The worldwide emergence of NDM-1 positive, multiresistant Enterobacteriacae have created a major global health problem. The NDM-1 can catalyze the hydrolysis of a various antibiotics including the latest generation carbapenems, which are often referred as the last line of antibiotics active against multiresistant gram-negative pathogens. Also there...
Article
Full-text available
Cisplatin is an anticancer drug extensively used against a variety of cancers. Cisplatin chemotherapy is found to manifest dose-dependent nephrotoxicity. Depletion of the renal antioxidant defence system has been suggested to be the main cause of cisplatin-induced nephrotoxicity. The purpose of this study is to investigate whether the ethanol extra...
Article
Nyctanthes arbor-tristis flowers were collected in the month of August from the Manipal region of the India. The flowers were shed dried, powdered and extracted with ethanol in soxhlet apparatus. Dried ethanolic extract was further subjected to fractionation by using petroleum ether, diethyl ether and ethyl acetate solvents in the order of increasi...
Article
Full-text available
Extracts from natural products, especially microorganisms, have served as a valuable source of diverse molecules in many drug discovery efforts and led to the discovery of several important drugs. Identification of microbial strains having promising biological activities and purifying the bio-molecules responsible for the activities, have led to th...
Article
Full-text available
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...
Article
Objective: Venlafaxine,hydrochloride is a structurally novel phenethyl bicyclic antidepressant, and is usually categorized as a serotonin–norepinephrine reuptake inhibitor (SNRI) but it has been referred to as a serotonin–norepinephrine–dopamine reuptake inhibitor. It inhibits the reuptake of dopamine. Venlafaxine HCL is widely prescribed in the fo...
Article
Claisen-Schmidt condensation reaction of aldehydes and ketones afforded intermediate chalcones, which were cyclized into final products as substituted 2- phenyl chromen-4-ones. The synthesized compounds were characterized by physicochemical and spectral studies. All the synthesized eight compounds were screened for antioxidant activity by DPPH radi...
Article
Full-text available
Different substitutions of imidazolones were synthesized and screened first for the in vitro anticancer activity at concentrations of 12.5 – 100 μg/ ml on Hela cell lines. Out of these eight synthesized compounds, the most active compound 3C-BRS was selected for in vivo anticancer activity using Ehrlich ascites carcinoma (EAC), using liquid tumor m...
Article
A new simple, rapid, reproducible, and stability-indicating high-performance thin-layer chromatographic method for analysis of racecadotril in the bulk drug and in a pharmaceutical formulation has been established and validated. Chromatographic separation was achieved on aluminum-backed silica gel 6017(254). HPTLC plates with n-hexane-ethyl acetate...
Article
We investigated the effects of Sphaeranthus indicus on mast cell stabilizing activity to provide scientific basis for the clinical use of S. indicus. The protective effect of different extracts of whole plant of S. indicus against compound 48/80 and sheep serum induced mast cell degranulation was evaluated. Ethanol extract of S. indicus at the dose...