Pharmaceutical Sciences and Natural Products - Research Publications

Permanent URI for this collectionhttps://kr.cup.edu.in/handle/32116/56

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    Amino Acid Derived Prodrugs: An Approach to Improve the Bioavailability of Clinically Approved Drugs
    (Bentham Science Publishers, 2021-06-04T00:00:00) Singh, Yogesh; Saklani, Samriti; Tantra, Tanmoy; Thareja, Suresh
    Amino acids derived prodrugs emerged as an attractive approach to improve oral delivery of drugs with low solubility and permeability. Conjugation of amino acids with parent drug molecules resulted in several-fold increases in water solubility. Acceptability of the amino acids derived prodrug approach increases day by day to fulfill the different characteristics needed to get the desired pharmacological or therapeutic activity. Due to the significant structural diversity of amino acids, various amino acids can be employed as a carrier to provide desirable Pharmacokinetic-Phar-macodynamic (PK-PD) characteristics. The present review focused on using amino acids as a carrier moiety to improve approved drugs' bioavailability. Attempts have been made to cover amino acid conjugated clinically available drugs. � 2021 Bentham Science Publishers.
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    Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies
    (Elsevier, 2020) Dhiman, N; Kaur, K; Jaitak, Vikas
    Cancer is a leading cause of death worldwide. Even after the availability of numerous drugs and treatments in the market, scientists and researchers are focusing on new therapies because of their resistance and toxicity issues. The newly synthesized drug candidates are able to demonstrate in vitro activity but are unable to reach clinical trials due to their rapid metabolism and low bioavailability. Therefore there is an imperative requisite to expand novel anticancer negotiators with tremendous activity as well as in vivo efficacy. Tetrazole is a promising pharmacophore which is metabolically more stable and acts as a bioisosteric analogue for many functional groups. Tetrazole fragment is often castoff with other pharmacophores in the expansion of novel anticancer drugs. This is the first systematic review that emphasizes on contemporary strategies used for the inclusion of tetrazole moiety, mechanistic targets along with comprehensive structural activity relationship studies to provide perspective into the rational design of high-efficiency tetrazole-based anticancer drug candidates. - 2020 Elsevier Ltd