• Title/Summary/Keyword: Synthetic drugs

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SYNTHETIC DEVELOPMENT OF NEW 1$\beta$-SUBSTITUTED CARBAPENEMS

  • Nagao, Yoshimitsu
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.34-35
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    • 1993
  • The Development of new asymmetric induction methods useful for syntheses of biologically active natural products and drugs, using C4-chiral 1,3-th-iazolidine-2-thiones, has been a recent focus of interest. 1-8) The present account describes the significance of particular heterocycles in the synthetic development of new 1${\beta}$-substituted carbapenems. A fungal metabolite, (+)-thienamycin (1) has attracted one's attention as a hopeful candidate for new-generation antibiotic drugs because of its strong antimicrobial activities and wide antimicrobial spectra due to the extensive inhibition against various ${\beta}$-lactamases. However, it has been serious problems toward a practically useful drug that (+)-thienamycin is fairly labile in the solution and can be metabolized by renal dehydropept- idase-I (DHP-I). Recently, a Merck Sharp & Dohme research group exploited a non-natural ${\beta}$-lactam, imipenem (2) which has been appeared in the drug market as the first carbapenem-type antibiotic drug. 9) However 2 must be used with a DHP-I inhibitor, cilastatin sodium (3).9) Thus, a 1,${\beta}$-methyl- carbapenem derivative 4 has been disclosed by the same group. 10) It seems to be more hopeful candidate as a new-generation antibiotic because it can directly resist against metabolism by the renal DHP-1 without an enzyme inhibitor 3. 10)

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A Study on the Tyrosinase Inhibitory and Antioxidant Effect of Microalgae Extracts

  • Ji, Keunho;Kim, Yeeun;Kim, Young Tae
    • Microbiology and Biotechnology Letters
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    • v.49 no.2
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    • pp.167-173
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    • 2021
  • Reactive oxygen species (ROS) disrupt the cellular redox balance, exert cytotoxic effects, and consequently promote the development of various diseases in humans. Previous studies have reported that antioxidants counteract the adverse effects of ROS. Several studies examine the whitening effects of various agents based on their ability to inhibit tyrosinase activity. Tyrosinase is a critical enzyme involved in the synthesis of melanin, which protects the skin against radiation. Various agents exhibiting antioxidant and tyrosinase inhibitory activities have been synthesized. However, these synthetic drugs are associated with toxicity, decreased safety, and poor skin penetration in vivo, which has limited the clinical application of synthetic drugs. This study examined the antioxidant and tyrosinase inhibitory activities of some microalgae. The methanol, dichloromethane, and ethyl acetate extracts of four microalgal species (Tetraselmis tetrathele, Dunaliella tertiolecta, Platymonas sp., and Chaetoceros simplex) were prepared. The physiological and whitening effects of microalgal extracts were investigated by measuring the antioxidant and tyrosinase inhibitory activities. The ethyl acetate extract of D. tertiolecta exhibited the highest antioxidant and tyrosinase inhibitory activities. Future studies must focus on examining the whitening effects of microalgae on cell lines to facilitate the development of microalga-based therapeutics for skin diseases, functional health foods, and whitening agents. Thus, microalgae have potential applications in the pharmaceutical, food, and cosmetic industries.

Structure elucidation and determination of illegal compounds (Anti-impotance drug analogues) in foods (식품 중 부정유해물질 (발기부전치료제 유사물질) 구조규명 및 분석)

  • Choi, Dongmi
    • Analytical Science and Technology
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    • v.21 no.2
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    • pp.65-83
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    • 2008
  • It is noted that illegal hazardous foods containing unauthorized drugs or synthetic drung analogues are increasing. Especially, reported are unknown compounds that have the modified chemical structures of the anti-impotence drugs such as sildenafil, vardenafil, and tatalafil. In addition, it is very reserved, since illegal synthetic compounds having similar chemical structures modified from anti-impotence drug to avoid the government inspection are not proved their safety at all. This review in ulation to food safety, lists the illegal compounds added to foods and describes about the analytical methods to chanacterize 16 anti-impotence drug analogues such as homosildenafil, hongdenafil, pseudovardenafil, aminotadalafil, hydroxyhomosildenafil, hydroxyhongdenafil, dimethylsildenafil, xanthoanthrafil, hydroxyvardenafil, norneosildenafil, demethylhongdenafil, piperidinohongdenafil, carbodenafil, thiosildenafil, dimethylthiosildenafil, and acetylvardenafil.

Shaping of Hormone drug Knowledge and drug market: Athletes use and consumption of synthetic hormones (호르몬 약물 지식과 시장의 형성: 운동선수들의 합성 호르몬 사용과 소비)

  • Han, Gwnag Hee;Kim, Byung Soo
    • Journal of Science and Technology Studies
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    • v.14 no.1
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    • pp.87-116
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    • 2014
  • This article focuses on synthetic hormone consumption that illegal act of heterogeneous forms of pharmaceuticalization. Athletes are not unfamiliar with the use of synthetic hormones that contain anabolic steroids. Synthetic hormones are used to increase muscle mass and strength. This drug use practice cannot simply be viewed as illegal. Athletes accumulate knowledge on these hormones that conflicts with the knowledge proffered by physicians and they consume drugs responsibly. Physicians' knowledge of these hormones is limited to their use in the treatment of abnormalities. Athletes, however, are expanding the role of these hormones to include their potential for enhancement. Thereby, a new value is assigned to synthetic hormones, and an informal market is formed. Previous studies in the fields of biopolitics and biomedicalization have mainly focused on the formal connection between biomedical science and the institutional network. This article, therefore, analyzes the informal and the various aspects of biomedicalization.

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Anticonvulsant potential of some traditional medicinal plants

  • Asif, Mohammad
    • CELLMED
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    • v.4 no.1
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    • pp.1.1-1.13
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    • 2014
  • Epilepsy has now become the most serious brain disorder. A number of synthetic antiepileptic drugs are available in practice, however their effectiveness does not grip true with the entire population suffering from epilepsy. Traditional systems of medicine are popular in developing countries and most of the population relies on traditional medicines for their primary health care need. Medicinal plants to be an important source of traditional medicines. Various plants are used for the treatment of epilepsy in traditional system of medicines and various plants are yet to be scientifically investigated. Phyto-constituents have been the basis of treatment of human diseases including epilepsy. Herbal products are extensively used for the treatment of many diseases worldwide and where allopathic fails or has severe side effects. Psycho neural drugs are also have very serious side effects like physical dependence, tolerance, deterioration of cognitive function and effect on respiratory, digestive and immune system. So the treatments through herbal medicines are widely used across the world due to their wide applicability and therapeutic efficacy with least side effects, which in turn has accelerated the research regarding natural therapy. In this review we have summarized some herbal anti-epileptics.

DELTA OPIOID ANALGESICS

  • Burks, Thomas F.
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.50-62
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    • 1994
  • Opium, morphine and rotated natural and synthetic opiates have been used since antiquity, and to the present, for the relief of moderate and severe pain. Morphine and pharmacologically related drugs, however, produced an array of undesired or dangerous side effect that limit their use as analgesics. Prominent among the limiting side effects are constipation, respiratory depression, release of prolactin, and liability for the production of drug dependence. It was our aim to develop, if possible, a drug or class of drugs with analgesic activity similar to that of morphine, but without the serious side effects associated with morphine. Our overall strategy was to take advantage of advancing knowledge concerning multiple types of opioid receptors, to develop ligands selective for the delta type receptors, to determine whether delta receptor agonists offer advantages over mu agonists, then to design compounds with pharmacokinetic properties compatible with practical therapeutic application. All but the last of these objectives have been realized.

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Anticonvulsant potential of some medicinal plants and their beneficial properties

  • Asif, Mohammad
    • CELLMED
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    • v.3 no.4
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    • pp.27.1-27.13
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    • 2013
  • Epilepsy has now become the most serious brain disorder. A number of synthetic antiepileptic drugs are available in practice, however their effectiveness does not grip true with the entire population suffering from epilepsy. Traditional systems of medicine are popular in developing countries and most of the population relies on traditional medicines for their primary health care need. Medicinal plants to be an important source of traditional medicines. Various plants are used for the treatment of epilepsy in traditional system of medicines and various plants are yet to be scientifically investigated. Phytoconstituents have been the basis of treatment of human diseases including epilepsy. Herbal products are extensively used for the treatment of many diseases worldwide and where allopathic fails or has severe side effects. Psycho neural drugs are also have very serious side effects like physical dependence, tolerance, deterioration of cognitive function and effect on respiratory, digestive and immune system. So the treatments through herbal medicines are widely used across the world due to their wide applicability and therapeutic efficacy with least side effects, which in turn has accelerated the research regarding natural therapy. In this review we have summarized some herbal antiepileptics.

Boronated Porphyrins and Chlorins as Potential Anticancer Drugs

  • Ol'shevskaya, Valentina A.;Zaytsev, Andrey V.;Savchenko, Arina N.;Shtil, Alexander A.;Cheong, Chan-Seong;Kalinin, Valery N.
    • Bulletin of the Korean Chemical Society
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    • v.28 no.11
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    • pp.1910-1916
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    • 2007
  • Analyzed are recent advances in design of novel boronared conjugates of synthetic and natural porphyrins and chlorins. These compounds showed high efficacy as cytotoxic agents for tumor cells in culture and as phototoxins in photodynamic therapy of tumor xenografts. Thus, boronated porphyrins and chlorins emerge as promising class of anticancer agents with potentially multiple advantages: the chemotherapeutic drugs alone and photo- and radiosensitizers in binary treatments.

Development of novel method for evaluation of antitumor effect of anticancer drugs on hepatocellular carcinoma induced using 3'-methyl-4-diethylaminoazobenzene in Sprague-Dawley rat (3'-methyl-4-diethylaminoazobenzene으로 유발된 랫트 hepatocellula carcinoma 모델에서 항암제의 항암효과에 대한 평가기법 개발)

  • Kim, Gon-sup;Kim, Jong-shu
    • Korean Journal of Veterinary Research
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    • v.37 no.3
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    • pp.509-523
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    • 1997
  • This study was carried out for investigating antitumor effects of 5-fluorouracil(5-FU), methotrexate(MTX) and retinoic acid(RA) on hepatocellular carcinoma induced in Sprague-Dawley rat. Antitumor effects were examined a flow cytometric DNA distributions by flow cytometry and stuied ATP/Pi using nuclear magnetic resorance, and the enzymatic activity of thymidylate synthetase and dihydrofolate reductase as well as contents of total collagen and sialic acid were measured with spectrophotometer. In this study, S phase fraction, contents of sialic acid and total collagen were decreased in the induced hepatocellular carcinoma treated with 5-FU and MTX, and synergistic effects of anticancer drugs were exhibited in the hepatocellular carcinoma treated with 5-FU and MTX simultaneously, and the inhibition of thymidylate synthetic and dihydrofolate reductase activity were shown in the hepatocellular carcinoma treated with 5-FU, MTX, and 5-FU and MTX simultaneously. On the other hand, the ratio of ATP/Pi were increased in all groups except group treated with RA. The experimental results suggest that above method may be valuable for evaluating antitumor effect of anticancer drugs.

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Research Trend of Antiviral Natural Products for Companion Animal (천연물 유래의 반려동물 항바이러스활성물질 연구 동향)

  • Kang, Byeong Ku;Yang, Seo Young;Kim, Young Ho
    • Korean Journal of Pharmacognosy
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    • v.50 no.1
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    • pp.1-10
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    • 2019
  • Recently, companion animal culture has grown rapidly and mature, raising interest in preventing and treating animal diseases. In particular, viral infection was a serious threat to companion animal health because there was no proper antiviral drugs. Synthetic antiviral drugs have limitations such as low efficiency, toxicity, and occurrence of resistant viruses. Therefore, attempts to find new anti-viral drugs from natural sources have continued. This review focused on the natural products and active substances that exhibit antiviral activity against three viruses: canine distemper virus (CDV), canine parvovirus (CPV), and feline calicivirus (FCV) that cause fatal diseases in dogs and cats. Natural plant extracts, flavonoids, polysaccharides, alkaloids and saponins showed antiviral activity with various mechanisms and differences in activity depending on the structure. Especially, quercetin and epigallocatechin-3-gallate (EGCG) showed antiviral activity through a multi-mechanism that interferes with the attachment and penetration stages of the virus and inhibits the viral polymerase within the cell. Some natural plant extracts showed a virucidal activity and showed the potential effect as a preventative agent to prevent the viral infection. This review is expected to provide research trend on the development of antiviral natural products for companion animals.