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      A review on bis-hydrazonoyl halides: Recent advances in their synthesis and their diverse synthetic applications leading to bis-heterocycles of biological interest

      review-article
      Journal of Advanced Research
      Elsevier
      Bis-hydrazonoyl halides, Bis-nitrilimines, 1,3-Dipolar cycloaddition, Biological activities

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          Abstract

          This review covers a summary of the literature data published on the chemistry of bis-hydrazonoyl halides over the last four decades. The biological activities of some of the bis-heterocyclic compounds obtained from these bis-hydrazonoyl halides are also reviewed and discussed.

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          1,3,4-thiadiazole and its derivatives: a review on recent progress in biological activities.

          The 1,3,4-thiadiazole nucleus is one of the most important and well-known heterocyclic nuclei, which is a common and integral feature of a variety of natural products and medicinal agents. Thiadiazole nucleus is present as a core structural component in an array of drug categories such as antimicrobial, anti-inflammatory, analgesic, antiepileptic, antiviral, antineoplastic, and antitubercular agents. The broad and potent activity of thiadiazole and their derivatives has established them as pharmacologically significant scaffolds. In this study, an attempt has been made with recent research findings on this nucleus, to review the structural modifications on different thiadiazole derivatives for various pharmacological activities.
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            Antibacterial and antifungal activities of new pyrazolo[3,4-d]pyridazin derivatives.

            Several new pyrazolo[3,4-d]pyridazin derivatives were prepared by the reaction of two [corrected] 1H-pyrazole-3-carboxylic acids and various hydrazines. The compounds were tested for antimicrobial activities against Gram-negative, Gram-positive bacteria and fungi. The compounds named as 7e, f had the highest antimicrobial activities against Gram-negative, Gram-positive bacteria and fungi with minimum inhibitory concentrations in the range of 0.31 to<0.0024 mg ml(-1) .
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              Synthesis, reactions and biological activity of some new bis-heterocyclic ring compounds containing sulphur atom

              Background The derivatives of thieno[2,3-b]thiophene belong to a significant category of heterocyclic compounds, which have shown a wide spectrum of medical and industrial application. Results A new building block with two electrophilic center of thieno[2,3-b]thiophene derivatives 2 has been reported by one-pot reaction of diketone derivative 1 with Br2/AcOH in excellent yield. A variety of heteroaromatics having bis(1H-imidazo[1,2a] benzimidazole), bis(1H-imidazo[1,2-b][1,2,4]triazole)-3-methyl-4-phenylthieno[2,3-b]thiophene derivatives, dioxazolo-, dithiazolo-, and 1H-imidazolo-3-methyl-4-phenylthieno[2,3-b]thiophene derivatives as well pyrrolo, thiazolo -3-methyl-4-phenylthieno[2,3-b]thiophene derivatives have been designed, synthesized, characterized, and evaluated for their biological activity. Compounds 3–9 showed good bioassay result. These new derivatives were evaluated for anti-cancer activity against PC-3 cell lines, in vitro antioxidant potential and β-glucuronidase and α-glucosidase inhibitory activities. Compound 3 (IC50 = 56.26 ± 3.18 μM) showed a potent DPPH radical scavenging antioxidant activity and found to be more active than standard N-acetylcystein (IC50 = 105.9 ± 1.1 μM). Compounds 8a (IC50 = 13.2 ± 0.34 μM) and 8b (IC50 = 14.1 ± 0.28 μM) found as potent inhibitor of α-glucusidase several fold more active than the standard acarbose (IC50 = 841 ± 1.73 μM). Most promising results were obtained in β-glucuronidase enzyme inhibition assay. Compounds 5 (IC50 = 0.13 ± 0.019 μM), 6 (IC50 = 19.9 ± 0.285 μM), 8a (IC50 = 1.2 ± 0.0785 μM) and 9 (IC50 = 0.003 ± 0.09 μM) showed a potent inhibition of β-glucuronidase. Compound 9 was found to be several hundred fold more active than standard D-Saccharic acid 1,4-lactone (IC50 = 45.75 ± 2.16 μM). Conclusions Synthesis, characterization, and in vitro biological activity of a series of thieno[2,3-b]thiophene have been investigated.
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                Author and article information

                Contributors
                Journal
                J Adv Res
                J Adv Res
                Journal of Advanced Research
                Elsevier
                2090-1232
                2090-1224
                13 September 2016
                November 2016
                13 September 2016
                : 7
                : 6
                : 873-907
                Affiliations
                Department of Chemistry, Faculty of Science, University of Cairo, Giza 12613, Egypt
                Article
                S2090-1232(16)30069-8
                10.1016/j.jare.2016.09.001
                5030341
                0b6eeb2d-3784-4439-9581-e9140d136061
                © 2016 Production and hosting by Elsevier B.V. on behalf of Cairo University.

                This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

                History
                : 22 June 2016
                : 31 August 2016
                : 1 September 2016
                Categories
                Review

                bis-hydrazonoyl halides,bis-nitrilimines,1,3-dipolar cycloaddition,biological activities

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