Girish Kumar Gupta

• M.Pharm. (Pharm. Chemistry), Ph.D, FICCE, CITI-HIPS
• Professor (Full) at Sri Sai College of Pharmacy, Sri Sai Group of Institutes, Badhani-Pathankot

Background The global interest in edible medicinal herbs for healthcare has significantly increased during the last few years.Ganoderma lucidum is a medicinal mushroom which is known to be a potential source of many therapeutic and pharmaceutical products with significant health importance. Methodology The available literature using PubMed, Scopus...

Pyrazoles are an important class of heterocycles for new drug development that attracted much attention in the field of medicinal chemistry. In literature several pyrazole derivatives have been reported as target structures and evaluated for their biological activities. This review focuses on the development of various pyrazole derivatives up to 20...

Synthesis of some new 3,5-diamino-4-(4'-fluorophenylazo)-1-aryl/heteroarylpyrazoles (5a–5i) was achieved by the treatment of aryl/heteroarylhydrazines 4a–4i with 2-[(4-fluorophenyl)hydrazono]malononitrile 3 in refluxing ethanol. The structure of the compounds was established on the basis of IR, NMR (1H and 13C) and mass spectral studies. All the ni...

Background: Advanced glycation end products (AGEs) are basically the end result of glycation of proteins and/or lipids in the presence of sugars. Specific cases of hyperglycemia have been reported with increased propensity of generation of AGEs. Many chronic and deadly diseases such as diabetes, cancer and neurodegenerative disorders have been kno...

Background: Cancer has gradually become one of the leading causes of death worldwide. The incidence of cancer among the population has increased alarmingly over the last two decades, primarily due to an increasing population of immune-compromised patients and the continuing rise in anti-cancer drug resistance. Azole found privileged structure in m...

Nitrogen-containing acyclic, cyclic, and heterocyclic compounds and their derivatives have received increasing attention as a source of therapeutic agents. Oximes are an interesting class of Nitrogen-containing compounds possessing a wide variety of applications. Over the last decade, the interest in oximes and their derivatives has intensified. Ma...

To combat resistance against current antimalarials, modifying key pharmacophores and exploring novel parasite-specific drug targets remained one of the key drug design strategies. The resistance to quinoline-based antimalarials arises often due to the efflux of the drug. Hence, the development of newer agents containing bulkier pharmacophores will...

Indian Patent

Coronavirus disease 2019 (COVID-19)-associated mucormycosis (CAM) is responsible for a high mortality rate due to its unique and severe host-pathogen interactions. Critically ill or immunocompromised COVID-19 patients are more prone to suffer from aggressive mycoses. Probable victims include those with uncontrolled diabetes mellitus (DM), metabolic...

Background The development of digital technologies and the evolution of open innovation approaches have enabled the creation of diverse virtual organizations and enterprises coordinating their activities primarily online. The open innovation platform titled “International Natural Product Sciences Taskforce” (INPST) was established in 2018, to bring...

In the present work, RP-HPLC method was developed for the analysis of Moxifloxacin in the marketed ophthalmic formulation. This eye solution is used to treat infections of the eye including bacterial conjunctivitis. The chromatographic separation was achieved with UV detection at 292 nm. The stationary phase used is Sunfire C18 column (250 mm × 4.6...

In Silico Chemistry and Biology Current and Future Prospects

In the processes of molecular docking and simulation studies; the computational techniques have a vast and significant role in drug discovery process. The rigid view in the binding of both target and ligand is the basis of modeling strategy process. More evolution to such processes with the time has lead in revealing the path of understanding the d...

Method development is a broad term. In both quantitative and qualitative analysis developing a new method either for estimation of quantity of substance or to check the presence of the required component is a necessitate step. Validation means to establish the characteristics parameters of the method. It also helps by revealing the limitations and...

Medical Microbiology

Medical Microbiology is an excellent and easy-to-use textbook which explains the roles of microorganisms in human health and illness. Written in a clear and engaging manner, the book provides an overview of pathogenic organisms, their diagnosis and treatment tools as well as the molecular mechanisms of hostpathogen interactions and antimicrobial dr...

In the processes of molecular docking and simulation studies; the computational techniques have a vast and significant role in drug discovery process. The rigid view in the binding of both target and ligand is the basis of modeling strategy process. More evolution to such processes with the time has lead in revealing the path of understanding the d...

Australian Innovation Patent

HIV/AIDS pandemic is a massive serious threat to health and development of mankind and has influenced about 37.9 million people worldwide. The increasing negative health, economic and social impact of the disease has led to the search of new therapeutic candidates for mitigation of AIDS/HIV. Till now there is no treatment that can cure this disease...

Lung cancer is a leading cause of cancer deaths worldwide. The management of lung cancer treatment is often ineffective as a result of the development of drug resistance, reactions to treatment, drug-drug interactions or non-specific targeting of the anti-cancer drugs. Natural compounds show promise and potential activity in lung cancer with very f...

The World Health Organisation (WHO) announced on the 11th March 2020, a pandemic caused by a novel beta-coronavirus SARS-CoV-2, designated COVID-19. The virus emerged in December 2019 in Wuhan, China has spread across the world to be classed as a global pandemic. The traditional use of medicines from plants can be traced back to 60,000 years. Globa...

Background Tamoxifen citrate is a very prevalent drug marketed under several trade names like Apo-Tamox, Nolvadex, Tamec, Tamizam and Tamoplex. This molecule is approved by the FDA for breast cancer treatment. Some studies have shown that tamoxifen has anti-tuberculosis and anti-parasitic activities. Like any drug tamoxifen possesses side effects,...

Acquired Immunodeficiency Syndrome (AIDS), which chiefly originatesfroma retrovirus named Human Immunodeficiency Virus (HIV), has impacted about 70 million people worldwide. Even though several advances have been made in the field of antiretroviral combination therapy, HIV is still responsible for a considerable number of deaths in Africa. The curr...

Tuberculosis is a serious infectious bacterial disease. The disease is highly contagious and mostly transmitted from person to person, usually by bacteria and it is mostly transmitted by inhaling bacteria-carrying air droplets. Tuberculosis most generally attacks the lungs, but it can also infect other organs. It has resulted in progressive increas...

A lab-scale study of Scenedesmus obliquus: Acinetobacter pittii (S. obliquus: A. pitti) partnership cultured in synthetic domestic wastewater was conducted to evaluate the partnership performance for growth and removal of nutrients from wastewater. To draw out the functional dependencies of this partnership measured the ammonia-nitrogen (NH4+-N), o...

The synthesis of a novel series of 1,3,5-trisubstitiuted pyrazoline was achieved by refluxing chalcone derivative with different heteroaryl hydrazines. The newly synthesized compounds were characterized by 1H NMR, 13CNMR, mass spectral and elemental analysis data. The synthetic series of novel pyrazoline hybrids was screened for in vitro schizont m...

Tuberculosis is a serious infectious bacterial disease. The disease is highly contagious and mostly transmitted from person to person, usually by bacteria and it is mostly transmitted by inhaling bacteria-carrying air droplets. Tuberculosis most generally attacks the lungs, but it can also infect other organs. It has resulted in progressive increas...

New complexes of 1-(2,4-dinitrophenylamino)-4,4,6- trimethyl - 3, 4 - dihydropyrimidine - 2 - (1H) - thione (Hnmpt), [M(nmpt)2(H2O)n] (M(II) = Cu, Mn, Co; n = 2 and M(II) = Ni, Cd, Pd; n = 0) have been synthesized using environment friend protocol. They were characterized on the basis of elemental analyses, IR, 1H NMR, UV-visible and ESI-mass spect...

In an effort to discover an effective and selective antitumour agent, synthesis and anti-cancer potential of 4-(pyridin-4-yl)-6-(thiophen-2-yl)pyrimidin-2(1H)-one (SK-25), which has been reported earlier by us with significant cytotoxicity towards MiaPaCa-2 malignant cells, with an IC50 value of 1.95 μM and was found to instigate apoptosis. In the...

The present work describes synthesis of a series of 5-((1-(4-(4-chlorophenyl)thiazol-2-yl)-3- aryl-1H-pyrazol-4-yl)methylene)-2-(arylimino)thiazolidin-4-one derivatives and their molecular docking and biological evaluation as possible antimalarial, anthelmintic and antimicrobial agents. The synthesis of compounds has been accomplished by adopting s...

Background: Malaria, one of the most vital infectious diseases caused by protozoan parasites of the Plasmodium genus. As P. falciparum, the cause of most of the severe cases of malaria, is increasingly resistant to available drugs such as amodioquine, chloroquine, artemisinin, and antifolates, there is an urgent need of identify new targets for ch...

The human body is a home to more than 1 trillion microbes with a diverse variety of commensal microbes that play a crucial role towards the health of the individual. These microbes occupy different habitats such as gut, skin, vagina, oral etc. Not only the types and abundance of microbes are different in different organs, but also these may differ...

In an effort to discover an effective and selective antitumour agent, synthesis and anti-cancer potential of 4-(pyridin-4-yl)-6-(thiophen-2-yl)pyrimidin-2(1H)-one (SK-25), which has been reported earlier by us with significant cytotoxicity towards MiaPaCa-2 malignant cells, with an IC50 value of 1.95 μM and was found to instigate apoptosis. In the...

Aims: The current study is focused on the design and synthesis of 4-aryl/heteroaryl-4H-fused pyrans as anti-proliferative agents. All the synthesized molecules were screened against a panel of human carcinoma cell lines. Description: Significant inhibition was exhibited by the compounds against HCT-116 (Colon) and PC-3 (Prostate) cell lines while A...

Depression is a serious disorder that affects hundreds of millions of people around the world and causes poor quality of life, problem behaviors, and limitations in activities of daily living. Therefore, the search for new therapeutic options is of high interest and growth. Research on the relationship between depression and oxidative stress has sh...

1,5-Diaryl-3-trifluoromethypyrazole derivatives have acquired much attention in the past few years due to their good biological potential. In the present communication, some 1,5-diaryl-3-trifluoromethylpyrazoles were synthesized by one-pot solid phase reaction. The DNA photocleavage study of the synthesized compounds was performed using agarose gel...

Aims: The current study is focused on the design and synthesis of 4-aryl/heteroaryl-4H-fused pyrans as anti-proliferative agents. All the synthesized molecules were screened against a panel of human carcinoma cell lines. Description: Significant inhibition was exhibited by the compounds against HCT-116 (Colon) and PC-3 (Prostate) cell lines whil...

In the present study a series of metal complex of [bis (2-amino-5-aryl-1,3,4-thiadiazole]2Cl (S 1 -S 9 ) was synthesized by using ultrasound irradiation technique. The metal complex was synthesized by the reaction between ligand and appropriate metal salts (CuCl 2 . 2H 2 O, CoCl 2 . 6H 2 O, ZnCl 2 , MgCl 2 . 4H 2 O, NiCl 2 . 6H 2 O). The products w...

Pyran is a therapeutically vital oxygen containing heterocyclic moiety which exhibits an array of credible pharmacological properties. Pyran is also one of the important structural units found widely in natural products, such as coumarins, benzopyrans, sugars, flavonoids, xanthones and other natural products. The diverse anticancer capabilities of...

Pyran is an oxygen-containing heterocyclic moiety, which exhibits an array of pharmacological properties. Pyran is also one of the important structural subunits found widely in natural products, e.g. coumarins, benzopyrans, sugars, flavonoids, xanthones, etc. The diverse anticancer capabilities of pyrans have been additionally evidenced by the fact...

In order to explore the biological potential, some synthesized triazolylnucleosides were evaluated for their antibacterial, tyrosinase and DNA photocleavage activities. Triazolylnucleosides (5–12) were screened against Staphylococcus aureus (ATCC 6538), gram-positive and Escherichia coli (ATCC 10536), gram-negative bacterial strains. Among the seri...

In order to explore the biological potential, some synthesized triazolylnucleosides were evaluated for their antibacterial, tyrosi-nase and DNA photocleavage activities. Triazolylnucleosides (5-12) were screened against Staphylococcus aureus (ATCC 6538), gram-positive and Escherichia coli (ATCC 10536), gram-negative bacterial strains. Among the ser...

Pyran is an oxygen-containing heterocyclic moiety, which exhibits an array of pharmacological properties. Pyran is also one of the important structural subunits found widely in natural products, e.g. coumarins, benzopyrans, sugars, flavonoids, xanthones, etc. The diverse anticancer capabilities of pyrans have been additionally evidenced by the fact...

Background: A set of novel sulfanyl aminonaphthoquinone derivatives (5a-j) were synthesized starting from 2,3-dichloro-1,4-naphthoquinone (1). The amine substituents were introduced via a nucleophilic substitution at reflux temperature. Subsequent reactions of 2-chloro- 3-arylamino-1,4-naphthoquinones (3a-d) with different thiols (4a-c) led to the...

Antibacterial and antifungal organic compounds are becoming increasingly important for biomedical applications. This study deals with the synthesis, characterization of structures, in silico PASS prediction, and the discovery of antibacterial and antifungal properties based on new sulfanyl-1,4-naphthoquinone derivatives containing an arylamine with...

Background & objective: The inhibitory effects of four series of aryl butene derivatives, active against breast cancer, on the monophenolase activity of tyrosinase, in melanin-free ink from Sepia officinalis, have been studied. Hydroxytamoxifen 1, ferrociphenol 17 and several aryl butene analogs have shown strong antiproliferative activity on horm...

Background: A number of benzimidazole derivatives such as benomyl and carbendazim have been known for their potential role as agricultural fungicides. Simultaneously carbendazim has also been found to inhibit proliferation of mammalian tumor cells specifically drug and multidrug resistant cell lines. Objective: To understand the dual role of Car...

Background: Regucalcin (RGN), a calcium regulating protein having anti-prolific, antiapoptotic functions, plays important part in the biosynthesis of ascorbic acid. It is a highly conserved protein that has been reported from many tissue types of various vertebrate species. Employing its effect of regulating enzyme activities through reaction with...

A number of 2-(aryl/alkyl)thio-3-chloro-l,4-naphthoquinones (3a-g) and 2,3-(aryl/alkyl)thio-l,4-naphthoquinones (4a-d, 4f-g) were obtained by the reactions of 2,3-dichloro-1,4-naphthoquinone (1) with some various thiols and subsequently used as building blocks for thesynthesis of 2-(arylthio)-3-amino-1,4-naphthoquinone (5a-c, 5f) derivatives. The s...

Background: The most recurrent and considered second most frequent cause of cancer-related deaths worldwide in women is the breast cancer. The key to diagnosis is early prediction and a curable stage but still treatment remains a great clinical challenge. Origin of the Problem: A number of studies have been carried out for the treatment of breast...

The severity of diseases gives rise to the need to develop new ideas for the discovery of drugs. Traditional drug development methods have been very costly and time consuming that is why computer-assisted methods have taken a center stage: they help in accelerating the whole process of drug development. Novel drugs are designed according to the spe...

Chemical Drug Design provides a compact overview on recent advances in this rapidly developing field. With contributions on in silico drug design, natural product based compounds, as well as on ligand- and structure-based approaches, the authors present innovative methods and techniques for identifying and synthetically designing novel drugs.

Mistletoe is a group of obligate plant semi-parasites. Since ancient times, it is regarded as a medicinal plant, but current empirical studies have validated its therapeutic relevance. The biological roles have been attributed to the phytochemicals, namely, alkaloids, viscotoxins, triterpenoids, lectins and polysaccharides. Its anticancer effect ha...

This chapter enlightens the new concept of structure and ligand based drug designing. It is time saving technique and most reliable as in this method target is being modulated to obtain desired activity despite of hit and trial method which is tedious and less reliable. This chapter also comprises of different steps to be taken during the process o...

A set of novel sulfanyl aminonaphthoquinone derivatives (5a-j) were synthesized starting from 2,3-dichloro-1,4-naphthoquinone (1). The amine substituents were introduced via a nucleophilic substitution at reflux temperature. Subsequent reactions of 2-chloro-3-arylamino-1,4-naphthoquinones (3a-d) with different thiols (4a-c) led to the formation of...

Some 2,5-disubstituted-1,3,4-oxadiazole derivatives have been synthesized conveniently via oxidative cyclization of various synthesized aroylhydrazones by (diacetoxyiodo)benzene in dichloromethane under mild reaction conditions. In addition, the effect of electron-withdrawing/releasing groups on the formation of oxadiazole nucleus has also been stu...

Biomaterials and sustainable resources are two complementary terms supporting the development of new sustainable emerging processes. In this context, many interdisciplinary approaches including biomass waste valorization and proper usage of green technologies, etc., were brought forward to tackle future challenges pertaining to declining fossil res...

In the recent past trifluoromethylpyrazoles have gained much attention, particularly as anti-inflammatory and antibacterial agents, in the field of medicinal chemistry. The location of trifluoromethyl group, specially on 3- or 5-position of pyrazole nucleus, is greatly associated with variation in activity profile of the compounds. Therefore, the m...

An attempt toward designing of some butenolide derivatives against Cerebral Malaria (CM), as inhibitors of Intercellular adhesion molecule- 1(ICAM-1) was carried out using in silico approaches of molecular docking studies. ADME-T studies were also performed to further optimize the ligands. Binding conformations were compared with Artesunate, the ma...

Obesity is one of the greatest health threats of this century which involves the great risk of co-morbid diseases such as hypertension, type-2 diabetes and dyslipidaemia. In the present study, in-silico docking using pyranopyrazoles (1a-f) as an inhibitor against fat mass and obesity associated protein (FTO) via Molegro Virtual Docker software has...

A computational and docking study has been carried out on pyran-pyrimidine hybrids by using Molegro Virtual Docker software to predict their binding modes and orientation into the active site of cyclooxygenase-II enzyme. A series of 6-aryl-4-(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-2-(S-benzylthio) pyrimidines has emerged as a novel class of COX-II...

Imidazoles, natural or synthetic constitute an important class of bioactive heterocycles which have been found more effective in the treatment of various infectious and life threatening diseases. They exhibit a broad spectrum of biological activities such as anti-diabetic, antiviral, anticancer, anti-inflammatory, antibacterial and antifungal etc....

A series of new quinolin-2-yl moiety linked hydrazones of various aryl/heteroaryl aldehydes has been prepared which on treatment with iodobenzene diacetate in dichloromethane yielded novel triazolo[4,3-a]quinoline derivatives. All the synthesized compounds were characterized on the basis of their FT-IR, 1H, 13C NMR, and mass spectral data. Compound...

In the present study, synthesis of a series of some novel 3-(Quinolin-3-yl)-5,7-dimethyl-1,2,4-triazolo[4,3-a]pyrimidine derivatives (4a-e) has been achieved by oxidative cyclization of new pyrimidinyl hydrazone intermediates (3a-e) using hypervalent iodine reagent(III) under mild conditions. The structures of all synthesized compounds were establi...

The solvent free synthesis of metal complexes of two tridentate Schiff's bases, Salicylidene-N-cyanoacetohydrazone (CNL1) and 2-Hydroxy-l-benzilidene-N-cyanoacetohydrazone (CNL2) with Co(II), Ni(II), Cu(II), Zn(II) has been achieved successfully under mild reaction conditions. Among synthesized compounds tested for their DNA photocleavage potential...

The biological and medicinal properties of flavonoids have prompted enormous research aimed at developing synthetic routes to these heterocyles. This review focuses on the general structures and classification, food sources, medicinal properties associated with this system. Various synthetic methods developed till now for these compounds are review...

Review: methods to synthesize spiro ketals and their pharmacological evaluation from yar 1979 to 2012

In continuation of our efforts to find new biologically active agents, regioselective synthesis of a series of 2-(3,5-dimethyl-1H-pyrazol-1-yl)-1-arylethanones 4a-k has been achieved under facile, extremely mild and greener reaction conditions with excellent yields. Moreover, one pot multicomponent reaction has also been reinvestigated under previo...

The open access has revolutionized the information approach-ability and application. It is advantageous to the researcher community by providing immediate visibility to the authors and usage of their results. It also has an application access to information everywhere without any charges. Directory of Open Access Journals (DOAJ) is the major contri...

Objective: 1-(subsituted)-4,4,6-trimethyl-3,4-dihydropyrimidine-2(1H)-thione: Green synthesis, antibacterial activity and DNA photocleavage activity. Methods: In the present study, 1-(subsituted)-4,4,6-trimethyl-3,4-dihydropyrimidine-2(1H)-thione has been achieved under mild reaction conditions by employing microwave assisted and grind stone method...

In search of a new class of potential antimicrobial agents, some 1, 4-diaryl-2- mercaptoimidazoles (5a–5h) were prepared by employing a mild and green approach in which substituted anilines 3 were treated with phenacylbromide 2 in the presence of Na 2 CO 3/K 2 CO 3 followed by the treatment of a solid catalyst, p-TSA (para toluene sulphonic acid),...

In search of novel chemical nucleases the synthesis of dehydroacetic acid based tridentate hydrazone Schiff base and its colored complexes with Co(II), Ni(II), Cu(II), Mn(II), and Zn(II) has been achieved. All synthesized compounds were screened for their DNA cleavage potential using the plasmid DNA. The hydrazone Schiff base was synthesized via a...

A series of metal complexes of Cu(II), Ni(II), Co(II), Mn(II), Zn(II) with a tetradentate N,N`-bis(1-(4-hydroxy-6- methyl-2-oxo-2H-pyran-3-yl)ethylidene)malonohydrazide Schiff ’s base has been synthesized under solvent free conditions. Structures of the compounds were confirmed on the basis of spectroscopic data. All compounds were screened for the...

A simple, efficient and rapid practical procedure for the preparation of various thiazole derivatives 3 has been developed. The present protocol offers the solid phase reaction of various α-bromoketones with a wide variety of thioamides/thioureas in the presence of sodium carbonate at room temperature (within 3-5 minutes). More specifically, it als...

A large number of structurally diverse natural compounds containing azole nucleus constitute an important class of biologically active heterocycles that are gaining more attention in the field of medicinal chemistry. Among azoles, pyrazoles are rarely found in nature probably due to difficulty in the formation of N-N bond by living organisms. Howev...

Dehydroacetic acid (DHA) and its simple derivatives find many interesting applications in the synthesis of various heterocyclic compounds of potential biological interest. A variety of DHA based chemical reactions were found to be useful in the synthesis of 3-cinnamoyl-4-hydroxy-6-methyl-2-oxo-2H-pyrans i.e. Chalcone analogues of DHA, pyranopyrazol...

Objective: 1-(subsituted)-4,4,6-trimethyl-3,4-dihydropyrimidine-2(1H)-thione: Green synthesis, antibacterial activity and DNA photocleavage activity. Methods: In the present study, 1-(subsituted)-4,4,6-trimethyl-3,4-dihydropyrimidine-2(1H)-thione has been achieved under mild reaction conditions by employing microwave assisted and grind stone meth...

In search of a new class of organic compounds as potential COX-2 inhibitors, various 4-Fluorophenylhydrazones (3a–3i) have been synthesized and molecular docking study was conducted. All the synthesized compounds were also evaluated for their in vivo anti-inflammatory potential using carrageenan-induced rat paw odema method. In the present manuscri...