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      Synthesis and Biological Activities on Metal Complexes of 2,5-Diamino-1,3,4-thiadiazole Derived from Semicarbazide Hydrochloride

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          Abstract

          A bioactive ligand, 2,5-diamino-1,3,4-thiadiazole ( L), derived from semicarbazide hydrochloride, and its metal complexes were prepared and characterized. The complexes were characterized using elemental, infra-red, ultraviolet/visible, magnetic moment, atomic absorption, thin layer chromatography and molar conductance measurements. The IR data revealed that the ligand ( L) behaved as a tridentate neutral ligand. It coordinated to the metal ion via sulphur and nitrogen of the amines. The molar conductance data reveal that the chelates are non-electrolytes. From the Ultraviolet/Visible spectra and magnetic moment data, the complexes were found to have octahedral geometrical structure. In vivo evaluation of the antimicrobial activities of the metal complexes and the ligands showed greater activity against some micro-organisms when compared to the parent compounds. The chelates do not show toxicity against the activities of enzymes from homogenates of liver, kidney and serum in experimental rats.

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          Aphrodisiac potentials of the aqueous extract of Fadogia agrestis (Schweinf. Ex Hiern) stem in male albino rats.

          M. Yakubu, Adenike Oladiji, M. A. Akanji (2005)
          To evaluate the phytochemical constituents and the aphrodisiac potential of the aqueous extract of Fadogia agrestis (Rubiaceae) stem in male albino rats. The aqueous stem extract of the plant was screened for phytochemical constituents. Male rats were orally dosed with 18 mg/kg, 50 mg/kg and 100 mg/kg body weight, respectively, of the extract at 24 h intervals and their sexual behavior parameters and serum testosterone concentration were evaluated at days 1, 3 and 5. Phytochemical screening revealed the presence of alkaloids and saponins while anthraquinones and flavonoids are weakly present. All the doses resulted in significant increase in mount frequency, intromission frequency and significantly prolonged the ejaculatory latency (P 0.05) and reduced mount and intromission latency (P 0.05). There was also a significant increase in serum testosterone concentrations in all the groups in a manner suggestive of dose-dependence (P 0.05). The aqueous extract of Fadogia agrestis stem increased the blood testosterone concentrations and this may be the mechanism responsible for its aphrodisiac effects and various masculine behaviors. It may be used to modify impaired sexual functions in animals, especially those arising from hypotestosteronemia.
          Article 0 comments Cited 31 times – based on 0 reviews     Review now
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            Enzymes in rat urine: alkaline phosphatase.

            Jeanine Plummer, P D Leathwood, Elaine Wright (1972)
            Article 0 comments Cited 21 times – based on 0 reviews     Review now
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              Synthesis and antimalarial activity of sulfonamide chalcone derivatives.

              Joel J. P. C. Rodrigues, Daria Zelasko-Leon, Philip Rosenthal … (2005)
              A series of sulfonamide chalcone derivatives were synthesized and investigated for their abilities to inhibit beta-hematin formation in vitro and their activity against cultured Plasmodium falciparum parasites. Inhibition of beta-hematin formation was minimal in the aromatic ring of the chalcone moiety as it appeared for compounds 4b, 4d-f, and greatest with compounds 4g (IC50 0.48 microM) and 4k (IC50 0.50 microM) with a substitution of 3,4,5-trimethoxyl and 3-pyridinyl, respectively. In this study, the most active compound resulted 1[4'-N(2'',5''-dichlorophenyl) sulfonyl-amidephenyl]-3-(4-methylphenyl)-2-propen-1-one 4i, effective as antimalarial by the inhibition of cultured P. falciparum parasites (1 microM). These studies open up the novel possibility of development of sulfonamide derivatives as antimalarials that target beta-hematin formation and the inhibition of the development of cultured P. falciparum parasites, which should help delay the rapid onset of resistance to drugs acting at only a single site. Results with these assays suggest that chalcones exert their antimalarial activity via multiple mechanisms.
              Article 0 comments Cited 20 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Molecules
                Journal ID (iso-abbrev): Molecules
                Journal ID (publisher-id): molecules
                Title: Molecules
                Publisher: MDPI
                ISSN (Electronic): 1420-3049
                Publication date (Electronic): 12 July 2011
                Publication date Collection: July 2011
                Volume: 16
                Issue: 7
                Pages: 5861-5874
                Affiliations
                [1 ] Department of Chemistry, University of Ilorin, Ilorin, Kwara State, Nigeria; Email: jobaleye@ 123456yahoo.com ; Tel.: +2348033582048
                [2 ] Department of Chemical Sciences, Ajayi Crowther University, Oyo State, Nigeria
                Author notes
                [* ] Author to whom correspondence should be addressed; Email: dijijohnson@ 123456yahoo.com ; Tel.: +2348035720485.
                Article
                Publisher ID: molecules-16-05861
                DOI: 10.3390/molecules16075861
                PMC ID: 6264360
                PubMed ID: 21750479
                SO-VID: 50b71cd6-e997-4e70-b9a2-cb5194542380
                Copyright © © 2011 by the authors;
                License:

                licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                Date received : 30 April 2010
                Date revision received : 27 June 2011
                Date accepted : 06 July 2011
                Categories
                Subject: Article

                Keywords: antimicrobial,toxicological,semicarbazide hydrochloride,ligand
                Data availability:
                Keywords: antimicrobial, toxicological, semicarbazide hydrochloride, ligand

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