Author
Suleman R. Maujan
Bio: Suleman R. Maujan is an academic researcher from National Chemical Laboratory. The author has contributed to research in topics: Moiety & Catalysis. The author has an hindex of 5, co-authored 9 publications receiving 935 citations.
Topics: Moiety, Catalysis, Indole test, Aryl, Pharmacophore
Papers
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TL;DR: The present review will focus mainly on the recent literature for applications of this reaction in the field of medicinal chemistry, in particular on use of the 1,2,3-triazole moiety as pharmacophore.
Abstract: The copper(I)-catalyzed 1,2,3-triazole-forming reaction between azides and terminal alkynes has become the gold standard of 'click chemistry' due to its reliability, specificity, and biocompatibility. Applications of click chemistry are increasingly found in all aspects of drug discovery; they range from lead finding through combinatorial chemistry and target-templated in vitro chemistry, to proteomics and DNA research by using bioconjugation reactions. The triazole products are more than just passive linkers; they readily associate with biological targets, through hydrogen-bonding and dipole interactions. The present review will focus mainly on the recent literature for applications of this reaction in the field of medicinal chemistry, in particular on use of the 1,2,3-triazole moiety as pharmacophore.
983 citations
TL;DR: The new chemical entities synthesized were screened against various fungi and it was observed that the compounds 4a and 4i are potent inhibitors of Candida strains.
48 citations
TL;DR: The 1,2,3-triazole-forming reaction between azides and terminal alkynes has become the gold standard of click chemistry due to its reliability, specificity, and biocompatibility as mentioned in this paper.
Abstract: The copper(I)-catalyzed 1,2,3-triazole-forming reaction between azides and terminal alkynes has become the gold standard of 'click chemistry' due to its reliability, specificity, and biocompatibility. Applications of click chemistry are increasingly found in all aspects of drug discovery; they range from lead finding through combinatorial chemistry and target-templated in vitro chemistry, to proteomics and DNA research by using bioconjugation reactions. The triazole products are more than just passive linkers; they readily associate with biological targets, through hydrogen-bonding and dipole interactions. The present review will focus mainly on the recent literature for applications of this reaction in the field of medicinal chemistry, in particular on use of the 1,2,3-triazole moiety as pharmacophore.
30 citations
TL;DR: In this paper, a short synthetic strategy for 3,6-disubstituted N -2-thienyl/aryl-indoles, involving reaction of substituted 2,4-difluoro/dichloro-styrene epoxide with substituted 2-formylaminothiophenes or substituted N -formylanilines in the presence of a base followed by treatment with an acid, has been developed.
12 citations
TL;DR: In this paper, a simple and efficient methodology has been described for the selective oxidation of secondary benzylic alcohols to the corresponding ketones, and the method has been applied to a wide range of applications.
Abstract: A simple and efficient methodology has been described for the selective oxidation of secondary benzylic alcohols to the corresponding ketones. In contrast, primary benzylic alcohols afforded dimethyl acetals.
7 citations
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TL;DR: The present work aims to summarize the current approaches adopted for the synthesis of the 1,2,3-triazole and medicinal significance of these architectures as a lead structure for the discovery of drug molecules such as COX-1/COX-2 inhibitors, HIV protease inhibitors, CB1 cannabinoid receptor antagonist and much more which are in the pipeline of clinical trials.
563 citations
TL;DR: This review addresses the areas such as the underlying mechanisms, eight different targets such as ergosterol synthesis, chitin synthesis, ergosterols disruptors, glucan synthesis, squalene epoxidase, nucleic acid synthesis, protein synthesis, microtubules synthesis, and the current research work going on worldwide on different heterocycles.
522 citations
TL;DR: The recent results described in the literature since 2010 are reviewed, classified according to the nature of the catalyst precursor: copper(I) or copper(II) salts or complexes, metallic or nano-particulated copper and several solid-supported copper systems.
Abstract: The reactions of organic azides and alkynes catalysed by copper species represent the prototypical examples of click chemistry. The so-called CuAAC reaction (copper-catalysed azide-alkyne cycloaddition), discovered in 2002, has been expanded since then to become an excellent tool in organic synthesis. In this contribution the recent results described in the literature since 2010 are reviewed, classified according to the nature of the catalyst precursor: copper(I) or copper(II) salts or complexes, metallic or nano-particulated copper and several solid-supported copper systems.
399 citations
TL;DR: A comparison of the drug potency of the hybrid molecules with their individual counterparts is discussed for quantifying the significance of the concept of molecular hybridisation.
313 citations
TL;DR: The present study furnishes an overview of the hydroxy or/and methoxy-substituted 9,10-dihydro/phenanthrene, methylated, prenylated and other monomeric derivatives, dimeric and trimeric phenanthrenes and their biological activities.
282 citations