School Of Basic And Applied Sciences

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Subject: search.filters.subject.Drug discovery

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    Drug Discovery and Development: From Targets and Molecules to Medicines
    (Springer Singapore, 2021-02-18T00:00:00) Poduri, Ramarao
    This book describes the processes that are involved in the development of new drugs. The authors discuss the history, role of natural products and concept of receptor interactions with regard to the initial stages of drug discovery. In a single, highly readable volume, it outlines the basics of pharmacological screening, drug target identification, and genetics involved in early drug discovery. The final chapters introduce readers to stem therapeutics, pharmacokinetics, pharmacovigilance, and toxicological testing. Given its scope, the book will enable research scholars, professionals and young scientists to understand the key fundamentals of drug discovery, including stereochemistry, pharmacokinetics, clinical trials, statistics and toxicology. � Springer Nature Singapore Pte Ltd. 2021.
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    An Overview on Biological Evaluation of Tetrazole Derivatives
    (Springer Nature, 2022-03-07T00:00:00) Kabi, Arup K.; Sravani, Sattu; Gujjarappa, Raghuram; Garg, Aakriti; Vodnala, Nagaraju; Tyagi, Ujjawal; Kaldhi, Dhananjaya; Velayutham, Ravichandiran; Singh, Virender; Gupta, Sreya; Malakar, Chandi C.
    Tetrazoles are distinguished by a five-membered, doubly unsaturated ring which consists of four nitrogen and one carbon atom with a molecular formula CN4H2, which have a wide range of medicinal activity and potential role in biosciences. Interest in tetrazole chemistry in recent decades has been increasing rapidly because of diverse biological and pharmaceutical applications, mostly due to the diversity of this N-heterocyclic moiety in medicinal chemistry. This moiety offers a more appreciative pharmacokinetic profile and plays the role of metabolically stable substitute for carboxylic acid functional group as well as exhibits a broad range of biological effects such as analgesic, antibacterial, anticancer, anti-inflammatory, antidiabetic, antifungal, antitubercular and antihyperlipidemic activities. This chapter highlights the unique features of the potential possible role of tetrazole derivatives and summarizes biological and pharmacological activities. � 2022, The Author(s), under exclusive license to Springer Nature Singapore Pte Ltd.
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    An Overview on Biological Activities of 1,2,3-Triazole Derivatives
    (Springer Nature, 2022-03-07T00:00:00) Kabi, Arup K.; Sravani, Sattu; Gujjarappa, Raghuram; Garg, Aakriti; Vodnala, Nagaraju; Tyagi, Ujjawal; Kaldhi, Dhananjaya; Singh, Virender; Gupta, Sreya; Malakar, Chandi C.
    Among the nitrogen-embedded heterocycles, 1,2,3-triazoles derivatives are widely explored and earned considerable attraction in pharmaceutical industry and academics. 1,2,3-Triazoles have attracted significant consideration during the last few years due to widespread implementation in synthetic organic chemistry, drug discovery process, supramolecular chemistry, chemical biology, polymer chemistry, fluorescent imaging as well as materials chemistry. Even though absent in nature, these N-heterocycles have a wide spectrum of medicinal applications against several malignant cells, microorganisms, viruses and their preclusive actions are resistant to various enzymes. Moreover, 1,2,3-triazoles-based scaffolds have been extensively immersed as a linker and a functional moiety, mainly owing to the fact that their processing simplicity, orthogonality development and attractive �Click� properties. This chapter highlights the recent developments on diversified biological efficiencies of 1,2,3-triazoles and their approach in the progress of novel bioactive as well as pharmacoactive entities in future. � 2022, The Author(s), under exclusive license to Springer Nature Singapore Pte Ltd.
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    An Overview on Biological Activity of Benzimidazole Derivatives
    (Springer Nature, 2022-03-07T00:00:00) Kabi, Arup K.; Sravani, Sattu; Gujjarappa, Raghuram; Garg, Aakriti; Vodnala, Nagaraju; Tyagi, Ujjawal; Kaldhi, Dhananjaya; Singh, Virender; Gupta, Sreya; Malakar, Chandi C.
    Benzimidazole moiety plays a key role in variety of heterocyclic scaffolds which derive the biological functioning of essential molecules. Because of the skeletal resemblance with the naturally appearing nucleotides, benzimidazole and its analogues exhibited numerous medicinal and pharmacological performances. They are appraised as the auspicious class of bioactive molecules which endorse diverse actions like antiprotozoal, antimicrobial, antimalarial, anti-helminthic, anti-inflammatory, anti-mycobacterial, antiviral, and antiparasitic. Moreover, benzimidazole has recognized paramount responses in current years and is an enormously important pharmacophoric heterocyclic moieties in recent drug innovations and medicinal chemistry. This chapter will be beneficial for the researchers working in the fields of medicinal chemistry in visualizing the diverse pharmacological activities of benzimidazole derivatives in developing a SAR on benzimidazole drugs. � 2022, The Author(s), under exclusive license to Springer Nature Singapore Pte Ltd.
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    Exploration of Pd-catalysed four-component tandem reaction for one-pot assembly of pyrazolo[1,5-c]quinazolines as potential EGFR inhibitors
    (Academic Press Inc., 2019) Ansari, A.J; Joshi, G; Yadav, U.P; Maurya, A.K; Agnihotri, V.K; Kalra, S; Kumar, R; Singh, S; Sawant, D.M.
    A series of pyrazolo[1,5-c]quinazolines as EGFR inhibitors was designed and synthesized by highly efficient and novel multicomponent route involving Pd-catalyzed tandem one-pot four-component reaction. The reaction proceeds with good functional group tolerance under a simple condition with excellent regioselectivity and high efficiency. Target compounds were screened against cancer cell lines MDA-MB-231, A549 and H1299. Of these, 9b and 10b exhibited superior anticancer activity (IC50 < 2.5 ?M) to erlotinib and gefitinib. Synthetics were able to inhibit EGFR mediated kinase activity, induced ROS in cancer cells promoting mitochondrial mediated apoptosis via halting cell cycle progression at G1 phase.