
Umangkumar Harishchandra Shah- M.Pharm, PGDPL, Ph.D
- Professor (Associate) at Charotar University of Science and Technology
Umangkumar Harishchandra Shah
- M.Pharm, PGDPL, Ph.D
- Professor (Associate) at Charotar University of Science and Technology
About
125
Publications
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Introduction
My research area is
Design and Synthesis of Anticancer Agent
Molecular Modelling
Stability Study of APIs
Impurity Profile of API's
Method Development and Validation
Current institution
Education
July 2007 - May 2009
Publications
Publications (125)
Objective: Simple, reliable, sensitive and accurate spectrophotometric and RP-HPLC methods for the estimation of INH, RIFA and PIPE in pure and pharmaceutical dosage form.
Methods: In the first Absorption correction method, methanol and distilled water were used as diluent. The wavelengths selected for the analysis were 262 nm, 338 nm and 477 nm f...
This review aims to evaluate the mechanisms of action of current and emerging anti-TB drugs and molecules, emphasizing hydrazone functionality. Hydrazone compounds, featuring an azomethine group (R 1-HN-N=CR 2 R 3), exhibit potent anti-TB and broad-spectrum anti-infective properties. It includes the synthesis and biological testing of hydrazide-hyd...
The current features of manufacturing of Large Volume Parenteral from receiving the API and excipient to the final dispatch of product addressed many features including, sampling errors, manufacturing errors other controls, and individuals involved in various phases. The pharmaceutical industry nowadays places a greater focus on production-related...
Lipid-based formulations are essential for enhancing drug solubility and bioavailability, yet selecting optimal lipid excipients for specific drugs remains challenging. This study introduces Sol_ME, a machine learning-based model designed to predict drug solubility in lipidic environments, thereby streamlining the formulation process. The Sol_ME mo...
The objective of the present study was to prepare a solid self-nano emulsifying drug delivery system (S-SNEDDS) of Fimasartan Potassium Trihydrate (FPT), a poorly water-soluble antihypertensive agent.
Equilibrium Solubility study and ternary phase diagram study were conducted for screening of excipients. D-optimal Mixture design was employed to opt...
A series of novel hybrid bipyrimidine derivatives were designed, synthesized and evaluated for their anticancer activity against the breast cancer cell line MCF-7 and the lung cancer cell line A549. The structures of all the synthesized molecules were confirmed using various spectroscopic techniques. Molecular docking studies were conducted using M...
The purpose of this study was to develop and optimize a Self-Micro Emulsifying Drug Delivery System (SMEDDS) for the poorly water-soluble drug Ticagrelor, enhancing its solubility and bioavailability. The study aimed to systematically evaluate the formulation using a mixture L-optimal design to achieve maximum transparency and minimal self-emulsifi...
Clinical trials have shown that combining a modest dose of Rivaroxaban (RIV) with Aspirin (ASP) is more effective than ASP alone in reducing cardiovascular mortality, myocardial infarction, and stroke. A high‐performance liquid chromatography method developed using Quality by Design (QbD) effectively estimates ASP and RIV for routine pharmaceutical...
Objectives: This study aimed to develop a robust Reverse Phase-High-Performance Liquid Chromatography
(RP-HPLC) method for simultaneous determination of Aspirin (ASP) and Apixaban (API) in bulk and in-house capsule formulations. Methods: The separation was conducted on a Phenomenex Luna C18 column using a Shimadzu
LC20AT High-performance liquid chr...
Cancer remains a foremost cause of mortality globally, with approximately 20 million new cases and nearly 10 million deaths reported in 2022. Lung and breast cancers are particularly prevalent and deadly, underscoring the critical need for novel therapeutic strategies. This study utilized a one-pot, multicomponent reaction (MCR) approach to synthes...
Background
Conventional chromatographic techniques and direct analysis pose challenges in detecting certain potential genotoxic impurities, primarily due to factors such as the absence of a chromophore, low molecular weight, and insufficient chromatographic retention caused by high polarity. One such compound, N, O-Dimethyl Hydroxylamine, is of par...
Book Contents –
Preface Syllabus for GPAT About the Examination -
Unit 1: Pharmaceutics
1. Physical Pharmaceutics 2. Pharmaceutical Engineering (Unit Operation) 3. Pharmaceutical Technology and Modern Pharmaceutics 4. Dispensing Pharmacy 5. Biopharmaceutics 6. Jurisprudence 7. Cosmetics Preparation 8. Microbiology
Unit 2: Pharmacology
1. Basic...
Imidazopyridine holds significance as a crucial fused bicyclic heterocycle within the realm of medicinal chemistry, being acknowledged as a "privileged scaffold" owing to its extensive utility. Numerous methodologies for the synthesis of imidazo[1,2-a]pyridines have been documented, with a considerable focus on strategies aimed at functionalizing t...
Chalcone derivatives have been proven and documented as non-steroidal anticancer agents. A study of chalcone can be performed as an aromatase inhibitor. One crucial strategy for managing estrogen-positive breast cancer is aromatase inhibition. A total of 13 derivatives of chalcone were synthesized by the aldol condensation reaction and characterize...
Hydrazide–hydrazone derivatives are prevalent in numerous bioactive compounds, showcasing a diverse array of biological effects including antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antiviral, and antiprotozoal properties. Consequently, numerous medicinal chemists have undertaken the synthesis of variou...
Synthetic routes of chromene are an area of thrust research due to its wide application as pigments, agrochemicals, cosmetics, and an important nucleus scaffold for various pharmaco-logically active drugs. The chromene nucleus is an important moiety for the discovery of new drug candidates owing to its broad range of pharmacological actions like an...
This article presents a comprehensive and comparative analysis of the regulatory frameworks governing the approval of pharmaceuticals in the Dominican Republic, Ecuador, and Nicaragua. It delves into the intricate scientific terminology and complex procedures inher-ent in these regulatory systems, shedding light on the demanding requirements that p...
Background
Interaction of PD-1 protein (present on immune T-cell) with its ligand PD-L1 (over-expressed on cancerous cell) makes the cancerous cell survive and thrive. The association of PD-1/PD-L1 represents a classical protein-protein interaction (PPI), where receptor and ligand binding through a large flat surface. Blocking the PD-1/PDL-1 comple...
Breast cancer is a global health concern, demanding innovative treatments. Targeting the Transforming Growth Factor‐beta (TGF‐β) signaling pathway, pivotal in breast cancer, is a promising approach. TGF‐β inhibits proliferation via G1 phase cell cycle arrest, acting as a suppressor initially, but in later stages, it promotes progression by enhancin...
Context:
Peripheral neuropathy (PN) is a multifaceted complication characterized by nerve damage due to oxidative stress, inflammatory mediators, and dysregulated metabolic processes. Early PN manifests as sensory changes that develop progressively in a "stocking and glove" pattern.
Methods and mechanisms:
A thorough review of literature has bee...
Background:
Numerous naturally occurring and artificially synthesized flavonoids have garnered attention for their impressive ability to combat oxidative stress and scavenge free radicals when evaluated in laboratory settings. The core aim of our investigation revolved around assessing the antioxidant potential of a diverse range of synthesized fla...
This research has developed an improved lyophilized formulation for Pemetrexed to enhance its stabilityusing various techniques such as amino acids, boric acid, and sugars. The preliminary screening identified sorbitol as themost suitable sugar and L-Arginine as most suitable amino acid due to low degradation rate and minimal change inreconstitutio...
This review article provides an overview of the green synthesis of thiazole derivatives, emphasizing sustainable and environmentally friendly methodologies. Thiazole derivatives possess significant value and find diverse applications across various fields. However, conventional synthesis methods often involve hazardous reagents and generate substan...
Background and Purpose
The blood-brain barrier (BBB), a critical interface of specialized endothelial cells, plays a pivotal role in regulating molecular and ion transport between the central nervous system (CNS) and systemic circulation.
Experimental Approach
This review aims to delve into the intricate architecture and functions of the BBB while...
Asciminib, also known as ACP-196, is the FDA-approved low-molecular ABL kinase inhibitor. The ABL kinase is a non-receptor tyrosine kinase that helps in cell growth and survival and is a key player in the development of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ALL). The BCR-ABL fusion prot...
Diabetes mellitus (DM) is a chronic metabolic condition linked to high blood sugar levels. Diabetes causes complications like neuropathy, nephropathy, and retinopathy. Diabetes foot ulcer (DFU) is a significant and serious wound healing issue resulting from uncontrolled DM. The main causes of the development of the DFU are oxidative stress brought...
Adverse drug reactions (ADRs) are a significant drug-related cause of disease and death. Pharmacovigilance (PV) plays a key role in the management of ADRs. To assess the pharmacist’s knowledge, attitudes and behavior of ADRs among community and hospital pharmacists in Gujarat, a validated questionnaire was developed and used to assess the understan...
Indole is known as a versatile heterocyclic building block for its multiple pharmacological activities and has a high probability of success in the race for drug candidates. Many natural products, alkaloids, and bioactive heterocycles contain indole as the active principle pharmacophore. These encourage the researchers to explore it as a lead in th...
Berberine (BRB) is a natural alkaloid of the isoquinoline class, mostly isolated from the Berberis genus, which exhibits antibiotic, immunostimulant, antitumor, cardiovascular protection, endocrine regulator, antidepressant, neuroprotective, antioxidant, anti-inflammatory, and other pharmacological properties. The poor aqueous solubility of BRB is...
Objective
Recent scientific advances have expanded insight into the immune system and its response to malignant cells. In the past few years, immunotherapy has attained a hallmark for cancer treatment, especially for patients suffering from the advanced-stage disease. Modulating the immune system by blocking various immune checkpoint receptor prote...
Simple, rapid, sensitive, robust, and validated reverse phase- high-performance liquid chromatography RP_(HPLC) was developed for the quantification of anti-diabetic drugs Teneligliptin hydrobromide (TH) and Metformin hydrochloride (MH) in bulk and in formulation. The RP-HPLC method was developed using an HPLC system with a PDA detector. A simple,...
Background
Quinoline derivatives have evinced their biological importance in targeting bacteria by inhibiting Dihydrofolate reductase. H2SO4 was successfully applied as an acid catalyst for a green, efficient, and one-pot solvent-free synthesis of quinoline derivatives using sonochemistry approach from various aromatic amines and glycerol with affo...
Across the past 20 years, advances in the field of pathogenesis have inspired researchers to look into novel pharmacological therapeutics that are more focused on the pathophysiological events of the disease (AD). This review article discussed the prior use of statins for prevention of Alzheimer's disease, which can help prevent the disease. Other...
Peptic ulcer is a disorder that commonly has an effect on the digestive system. It is a chronic illness which has impact on
approximately, 10% of the mankind. The majority of current therapy regimens are based on western medicine. Proton pump
inhibitors (PPIs) and histamine-2 (H2) receptor antagonists, which are commonly used to treat peptic ulcers...
Flavonoids are a sort of natural substance which are basically plant secondary metabolites having a polyphenolic structure
present in a wide range of food products. Flavonoids have become a vital constituent in nutraceutical, pharmacological,
therapeutic, and cosmetic fields. This is owing to their capability to regulate essential cellular enzyme a...
Diabetes is one of the main disease having many repercussions due to which there is a huge economic burden
globally. Therefore, there is a need of good therapeutic intervention by using some nutraceuticals to combat this
dreadful disease especially complications such as diabetic neuropathy where patients suffer from severe pain and
disability. T...
Curcumin is a lipophilic polyphenolic yellow compound extracted from Curcuma longa Linn. (turmeric) rhizome with a broad spectrum of pharmacological and medicinal properties as propounded by several in vivo, in vitro and clinical studies. Considerable research over the past century has been extensively studied on chemical, biological, and analytica...
A Reverse Phase High Performance Liquid Chromatographic method was developed and validated for the simultaneous estimation of lornoxicam and tolperisone hydrochloride in bulk drug and its combined dosage form. Chromatographic separation was carried out isocratically by reverse phase water enable C18 column (250 mm × 4.6 mm, 5.0 μ) using methanol: a...
Ageing comes with degeneration in many biological activities like impairment of cognition, intelligence, attention, and memory. The decline in all those mental capabilities would be due to the abnormal changes in neuronal architecture with increasing age, chronic oxidative stress and inflammatory state of the tissue, nutritional deficiency. Nootrop...
The outstanding research outcomes and registrations of myriads of probiotic strains have flooded the health market with various innovative probiotic-based products and their patents. The study of patented formulations of probiotics can give an overall insight into its existing application. A landscaping review of patents for probiotic-based prepara...
This review work discusses the applications of xenobots in drug discovery. These are the world's first tiny robots that are living. Robots are built of metals and other things that benefit humans to solve various issues; however, in this case, small xenobots were built utilizing Xenopus laevis, frog embryonic stem cells in the blastocyte stage. Xen...
Quinolines are a prominent heterocyclic motif and crucial building blocks in creating physiologically active compounds. Due to the fast development of novel medicines with a quinoline nucleus, numerous research papers have been published in a short amount of time. Therefore, to comprehend the present state of the quinoline nucleus in medicinal chem...
With the advent of a myriad of treatment possibilities for breast cancer, enzyme inhibition turns out to be the prevailing strategy for inhibiting estrogen biosynthesis. Aromatization of ring A of androstenedione, testosterone and 16-hydroxytestosterone results in increased estrogen level, which embraces the risk for breast cancer. In this present...
Background
Reading every clinical trial of any disease is tedious, and concluding the current progress in it, especially when the number of clinical trials recorded is so large. The Text Mining Platform of Artificial Intelligence (AI) can help to simplify the task.
Methods
A large pool of tuberculosis clinical trials has been searched through the...
The SARS-CoV-2 virus, accountable for the COVID-19 pandemic, is now sweeping the globe. As a result, as this disease resists testing and adoption of new treatments, repositioning existing medications may provide a quick and appealing method with established safety, features, and dose used. They are not, however, specific or focused. However, numero...
As we enter into the era of modern medicine, breast cancer remains a significant public health concern that has a noteworthy global impact in developed and developing countries. The modern era has seen an increase in the knowledge of the molecular mechanisms underlying cancer progression, leading to many anticancer drugs. The practice of curing cer...
Quinoxaline is a versatile heterocyclic moiety that possesses a wide range of biological activities. Therefore, many researchers have been performing the synthesis of quinoxaline derivatives on a daily basis. In addition, high demands for their synthesis often result in an increased generation of different waste chemicals. However, to minimize the...
World Health Organization categorized breast cancer as one of the leading cancer types in females worldwide, and its treatment remains challenging. Accumulated evidence suggested the role of estrogen and its metabolites in pre- and post-menopausal women. Upregulation of estrogen-dependent aromatase is significantly involved in the pathogenesis of b...
Background
Many natural and synthetic flavonoids have been studied and documented by inhibiting aromatase enzymes for their anti-cancer activity against breast carcinoma. The aromatase enzyme is a possible target for the estrogen's positive breast cancer receptor.
Objective
Hence, a series of flavonoids have been synthesized and assessed for their...
Objectives
Chronic renal failure (CRF) is a public health concern in both developed and developing countries. Therefore, there is still a need to look for secure and successful agents that can either minimise or prevent CRF from advancing to end-stage renal disorder. This study aimed to assess the effect of lycopene on adenine-induced CRF in the ra...
Background
Lung cancer is the leading cause of mortality in India. Adenosine receptor (AR) has emerged as a novel cancer-specific target. A3AR levels are upregulated in various tumor cells, which may mean that the specific AR may act as a biological marker and target specific ligands leading to cell growth inhibition.
Aim
Our aim was to study the...
Cancer is a frightful disease that still poses a 'nightmare' worldwide, causing millions of casualties annually due to one of the human race's most significant healthcare challenges that requires a pragmatic treatment strategy. However, plants and plant-derived products revolutionize the field as they are quick, cleaner, eco-friendly, low-cost, eff...
Simple, rapid, sensitive, robust, and validated high-performance thin-layer chromatography was developed for the simultaneous estimation of anti-diabetic drugs Teneligliptin hydrobromide (TH) and Metformin hydrochloride (MH) in bulk and pharmaceutical formulation. HPTLC system equipped Camag Linomat V, TLC Scanner IV, Twin Trough chamber, Dual-wave...
Piperine, a bioactive alkaloid of pepper has been considered for its medicinal properties and received significant attention from pharmaceutical scientists for its bioavailability enhancement action and the development of novel formulations. Piperine has shown numerous health effects and therapeutic properties; however, its pharmacological actions...
Complete Companion for GPAT and other Competitive Examinations in Pharmacy
The pharmaceutical industry and most particularly the biopharmaceutical industry are demanding advancements in analytical techniques. The field of proteomics and peptide mapping needs sensitive analysis and sophisticated instrumentation, which needs hyphenated analytical techniques to be explored. In addition to effective detection and characteriza...
Background
Probe sonication and High-speed homogenizer are comparatively costly equipment to fabricate the nanoparticles. Many academic and research institutions cannot afford the procurement and maintenance of such sophisticated equipment. In the present work, a newer idea is conceptualized, which can be adopted by the underprivileged research ins...
In the original publication, the title was wrongly published. The correct title should read as “Comparative study of the UV-Chemometrics, Ratio spectra derivative and HPLC-QbD methods for the simultaneous estimation of carisoprodol, paracetamol and caffeine in its triple combination formulation CARISOMA”.
Objective
Immediately after the outbreak of nCoV, many clinical trials are registered for COVID-19. The numbers of registrations are now raising inordinately. It is challenging to understand which research areas are explored in this massive pool of clinical studies. If such information can be compiled, then it is easy to explore new research studie...
Objective: Immediately after the outbreak of nCoV, many clinical trials are registered for COVID-19. The numbers of registrations are now raising inordinately. It is challenging to understand which research areas are explored in this massive pool of clinical studies. If such information can be compiled, then it is easy to explore new research studi...
For simultaneous analysis of Ciprofloxacin Hydrochloride (CIP), phenazopyridine Hydrochoride (PHE), in its drug-dose type, chemometric-assisted UV spectrophotometric methods have been established and validated. The chemometric methods used were partial least square (PLS) regression, principal component regression (PCR) and classical least square (C...
Phytotoxins are secondary metabolites that occur naturally in plants. They can be produced by the plant's metabolic system or excreted by microorganisms within the plant. Their toxicity varies from unnoticeable to fatal and they are found in both non‐food and food sources. Reacting oxygen species are one of the most common characteristics of some o...
In this chapter the history of drug discovery from microorganisms and future perspectives for research on microorganisms as a source of drugs are summarized. The chapter starts with the introduction of microbes, microbial metabolites, and antibiotics and then proceeds to the different classes of drugs obtained from the different types of microorgan...
Natural products played an important role in various drug discovery and development approaches. They are known to be the rich resources for the identification of new chemical entities (NCEs) intended to treat various diseases. Many drugs have been discovered and developed from natural sources. Indeed, collaborative efforts involving biologists as w...
Background/Objective
Benign prostate hyperplasia (BPH) is an abnormal growth of prostate observed commonly in elderly males. Artemisinin has been reported to reduce the levels of testosterone. This study is designed to evaluate the efficacy of Artemisinin on testosterone propionate (TP) induced benign prostate hyperplasia.
Materials and methods
Ma...
Protein tyrosine phosphatase 1B (PTP1B) is an important target for the treatment of diabetes. A series of thiazolidin‐4‐one derivatives 8–22 was designed, synthesized and investigated as PTP1B inhibitors. The new molecules inhibited PTP1B with IC50 values in the micromolar range. 5‐(Furan‐2‐ylmethylene)‐2‐(4‐nitrophenylimino)thiazolidin‐4‐one (17)...
Beta site amyloid precursor protein cleaving enzyme 1 (BACE1) is a rational target in Alzheimer’s disease (AD) drug development due to its role in amyloidogenic cleavage of Amyloid precursor protein (APP) in generating Amyloid β (Aβ). This β-secretase cleaves not only Amyloid precursor protein (APP) and its homologues but also small series of subst...
Chemometric is the use of mathematical and statistical methods to improve the understanding of chemical
information and to correlate quality parameters or physical properties to analytical instrument data.
In current work, two chemometric methods named as principal component regression (PCR) and PLS
partial least square (PLS) based on the use of sp...
Aromatase is an influential target to overcome estrogen receptor positive breast cancer, as the enzyme is responsible for conversion of androstenedione to estrone, a promising drug target for therapeutic management of breast cancer. Chalcones are prominent biosynthetic compounds and parent candidate for the synthesis of heterocycles with diversifie...
The book is useful for the students who is preparing for pharmacy entrance examination.
Stereochemistry has evinced the importance of many chiral drugs in aspects of drug designing and development. A literature review was conducted for several chiral drugs involving pharmacokinetic and pharmacodynamic parameters of their enantiomers along with their uses in certain diseased conditions. This article generally includes the pharmacologic...
Chromatographic separation was
achieved with a Shimadzu’s high performance liquid chromatograph and PhenomenexL1 analytical C18
column with a mobile phase of acetonitrile:ammonium acetate buffer (30 mM):methanol (50:45:5 %, v/v/v).
The flow rate was set at 1.5 ml/min and the detection wavelength was 232 nm. Quality by design approach
was employed f...
Background:
HER2 is a member of the human epidermal growth factor receptor (HER/EGFR-/ERBB) family. Amplification or over-expression of this oncogene has been shown to play a major role in the development and progression of certain destructive types of breast cancer. Several drugs like Trastuzumab, Pertuzumab, Capecitabine, and Letrozole are used i...
Background:
1,6-Dihydropyrimidine exerts notable pharmacological efficiency and emerged as integral backbones for treatment of type-II diabetes mellitus. To optimize the in vitro and In-silico study we carried out on substituted 1,6-Dihydropyrimidine. The objective of the present study is to evaluate the binding interaction of 1,6-Dihydropyrimidin...
Objective: The present work deals with the designing, scoring, synthesis and, characterization of 1-(4-(2-(4-Substitutedphenylamino)-2-oxoethyl)phenylsulfonyl)-3-(4-substitutedbenzoyl)urea (5A-5B),1-(4-(2-(4-substitutedphenylamino)-2-oxoethyl)phenylsulfonyl)-3-(4-substituted-benzoyl)guanidine(5C-5E) and, 1-(4-Substitutedbenzoyl)-3-(4-(2-oxo-2-(pipe...
Background:
A series of novel sulphonylureas/guanidine derivatives were designed, synthesized, and evaluated for the treatment of diabetes mellitus. In this study, the designed compounds were docked with AKR1C1 complexes by using glide docking program and docking calculations were performed to predict the binding affinity of the designed compounds...
Background:
High performance liquid chromatography is an integral analytical tool in assessing drug product stability. HPLC methods should be able to separate, detect, and quantify the various drug-related degradants that can form on storage or manufacturing, plus detect and any drug-related impurities that may be introduced during synthesis.
Obj...
The Pearson Guide to the GPAT and Other Competitive Examinations in Pharmacy in its third edition, is a sincere attempt to produce an eeective course material for the GPAT aspirants. The book contains six units, where the rst four units include major sections of GPAT syllabus, unit ve is for all important information regarding NIPER JEEexamination...
Three simple Thermometric assisted UV- Visible Spectrophotometric methods, Classical Least Square (CLS), Partial Least Square (PLS) and Principal Component Regression (PCR) were developed for simultaneous estimation of PCM and TOL in pharmaceutical dosage form without any chemical separation and any graphical treatment of the overlapping spectra of...
Questions
Questions (9)
Dear All
I am happy to share that our published review article is free to download till December 2023.
Title of article:
Role of Natural and Synthetic Flavonoids as Potential Aromatase Inhibitors in Breast Cancer: Structure-Activity Relationship Perspective
link to download article: https://www.eurekaselect.com/article/118556
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Dr. Umang Shah
Procedure:
1 eq. of 2 4 dihydroxyacetophenone + 2.5 eq. of MOM chloride + 3 eq. of K2CO3 in dry acetone keep it at 0 degree for 2 hours and then left it for 24 hours but still the 40% starting material is remaining, I worked up in cold water and then extract with ethyl acetate.
And it is reported procedure but still it can't be completed.
Can I put the flask under reflux condition?
Protection and deprotection of the 2 4 dihydroxy acetophenone