Search results for: Yogesh Yadav

Items from 1 to 13 out of 13 results

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Base‐Induced Annulation of Glycal‐Derived α‐iodopyranone with 2‐Aminopyrimidinones: Access to Chiral Imidazopyrimidinones

Vinay Kumar Mishra, Ghanshyam Tiwari, Ashish Khanna, Yogesh Yadav, more

European Journal of Organic Chemistry > 27 > 8 > n/a - n/a

A simple, environmentally benign and catalyst‐free method for the synthesis of chirally enriched imidazo[1,2‐a]pyrimidinone glycohybrids has been successfully developed. The protocol is based on a base‐induced annulation of α‐iodo‐pyranone with Michael addition of 2‐aminopyrimidinones followed by intramolecular nucleophilic substitution reaction. The privilege of this method includes mild reaction...

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Recent Efforts in Identification of Privileged Scaffolds as Antiviral Agents

Yogesh Yadav, Kavita Singh, Sunil Sharma, Vinay Kumar Mishra, more

Chemistry & Biodiversity > 20 > 10 > n/a - n/a

Viral infections are the most important health concern nowadays to mankind, which is unexpectedly increasing the health complications and fatality rate worldwide. The recent viral infection outbreak developed a pressing need for small molecules that can be quickly deployed for the control/treatment of re‐emerging or new emerging viral infections. Numerous viruses, including the human immunodeficiency...

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Inhibition of 11β‐Hydroxysteroid dehydrogenase‐1 with AZD4017 in patients with nonalcoholic steatohepatitis or nonalcoholic fatty liver disease: A randomized, double‐blind, placebo‐controlled, phase II study

Yogesh Yadav, Kelly Dunagan, Rachita Khot, Sudhakar K. Venkatesh, more

Diabetes, Obesity and Metabolism > 24 > 5 > 881 - 890

Aim To evaluate whether short‐term treatment with a selective 11β‐Hydroxysteroid dehydrogenase‐1 (11β‐HSD1) inhibitor, AZD4017, would block hepatic cortisol production and thereby decrease hepatic fat in patients with nonalcoholic fatty liver disease (NAFLD)/nonalcoholic steatohepatitis (NASH), with or without type 2 diabetes (T2D). Materials and Methods This was a randomized, double‐blind, placebo‐controlled,...

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Effects of heterocyclic N-alkyl chain length on cancer cell uptake of near infrared heptamethine cyanine dyes

Yogesh Yadav, Andrew Levitz, Sanam Dharma, Ritu Aneja, more

Dyes and Pigments > 2017 > 145 > C > 307-314

Cancer theranosis has materialized as a significant alternative to the separate diagnosis and treatment of cancer optimizing efficacy. Based on our previous work, it was determined that esterified heptamethine cyanine dyes were selectively cytotoxic to cancer cells. In order to determine the optimal N-alkyl chain length, a series of nine near-infrared fluorescent heptamethine cyanine dyes with monoester,...

article

Bilateral variant branching pattern of posterior cord of brachial plexus

Vishnu Pandey, Yogesh Yadav, Veena Bharihoke, Vishram Singh

Journal of the Anatomical Society of India > 2016 > 65 > S1 > S76-S78

Variant branching pattern of the cords of brachial plexus has been an area of concern for surgeons opting to explore this region. Anaesthetic blocks and surgical approaches are the highlights of these interventions, where a keen familiarization of the anatomy of this region is mandatory.The present case description reports a bilateral variant branching pattern of the posterior cord in an adult male...

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Design, synthesis and bioevaluation of novel 6-(4-Hydroxypiperidino)naphthalen-2-ol-based potential Selective Estrogen Receptor Modulators for breast cancer

Amitabh Jha, Yogesh Yadav, Ajay B. Naidu, V. Kameswara Rao, more

European Journal of Medicinal Chemistry > 2015 > 92 > C > 103-114

In a study directed towards development of novel Selective Estrogen Receptor Modulators (SERMs), 1-(4-(2-(dialkylamino)ethoxy)benzyl)-6-(4-hydroxypiperidin-1-yl)-2-naphthol and corresponding aryl methyl ethers were synthesized and bioevaluated against the estrogen-responsive human MCF-7 breast cancer cell line. The phenolic analogs displayed little or no activity, but aryl methyl ether analogs showed...

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Novel third-generation water-soluble noscapine analogs as superior microtubule-interfering agents with enhanced antiproliferative activity

Maged Henary, Lakshminarayana Narayana, Shazia Ahad, Sushma R. Gundala, more

Biochemical Pharmacology > 2014 > 92 > 2 > 192-205

Noscapine, an opium-derived ‘kinder-gentler’ microtubule-modulating drug is in Phase I/II clinical trials for cancer chemotherapy. However, its limited water solubility encumbers its development into an oral anticancer drug with clinical promise. Here we report the synthesis of 9 third-generation, water-soluble noscapine analogs with negatively charged sulfonato and positively charged quaternary ammonium...

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Phosphonated Near‐Infrared Fluorophores for Biomedical Imaging of Bone

Hoon Hyun, Hideyuki Wada, Kai Bao, Julien Gravier, more

Angewandte Chemie > 126 > 40 > 10844 - 10848

The conventional method for creating targeted contrast agents is to conjugate separate targeting and fluorophore domains. A new strategy is based on the incorporation of targeting moieties into the non‐delocalized structure of pentamethine and heptamethine indocyanines. Using the known affinity of phosphonates for bone minerals in a model system, two families of bifunctional molecules that target...

article

Phosphonated Near‐Infrared Fluorophores for Biomedical Imaging of Bone

Hoon Hyun, Hideyuki Wada, Kai Bao, Julien Gravier, more

Angewandte Chemie International Edition > 53 > 40 > 10668 - 10672

article

Synthesis and evaluation of antiproliferative activity of a novel series of hydroxychavicol analogs

Yogesh Yadav, Eric A. Owens, Vibhuti Sharma, Ritu Aneja, more

European Journal of Medicinal Chemistry > 2014 > 75 > Complete > 1-10

We have recently demonstrated that hydroxychavicol is a major constituent and the most active biophenolic of Piper betel leaves with significant antiproliferative activity in the micro molar range. Herein we present the design, synthesis and evaluation of fifteen novel hydroxychavicol analogs with varying antiproliferative activities in cancer cell lines from two representative tissue types, namely,...

article

Design, synthesis and bioevaluation of novel candidate selective estrogen receptor modulators

Yogesh Yadav, Erin D. MacLean, Annyt Bhattacharyya, Virinder S. Parmar, more

European Journal of Medicinal Chemistry > 2011 > 46 > 9 > 3858-3866

In an systematic attempt to develop novel Selective Estrogen Receptor Modulators (SERMs), chiral 1-((4-(2-(dialkylamino)ethoxy)phenyl)(2-hydroxynaphthalen-1-yl)methyl)piperidin-4-ols were designed based on an accepted pharmacophore model. Simpler prototypes, viz. racemic 1-((2-hydroxynaphthalen-1-yl)arylmethyl)piperidin-4-ols, were first synthesized to develop kinetic resolution to pure enantiomers...

article

Unique disposition of suprahyoid musculature

Vandana Mehta, Vanita Gupta, Jyoti Arora, Ashwani Kumar, more

Asian Journal of Oral and Maxillofacial Surgery > 2011 > 23 > 3 > 150-152

Geniohyoid (GH) plays a vital role in maintaining upper airway patency and anomalies pertaining to this muscle should not be overlooked. In fact, a careful recognition of these variations is mandatory while planning any interventional procedure in the suprahyoid region. We report a rare muscular anomaly in the suprahyoid region of the neck. The significance of the stratification of the GH muscle could...

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Microwave-assisted synthesis of antimicrobial dihydropyridines and tetrahydropyrimidin-2-ones: Novel compounds against aspergillosis

Anil K. Chhillar, Pragya Arya, Chandrani Mukherjee, Pankaj Kumar, more

Bioorganic & Medicinal Chemistry > 2006 > 14 > 4 > 973-981

Ten 4-aryl-1,4-dihydropyridine and three 4-aryl-1,2,3,4-tetrahydropyrimidin-2-one derivatives have been synthesized and examined for their activity against pathogenic strains of Aspergillus fumigatus and Candida albicans. Although none of the three compounds belonging to pyrimidin-2-one series showed any activity against two pathogens, two of the compounds of the dihydropyridine series, that is, diethyl...

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