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    1-Pendahuluan Kimia Medisinal

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    amalia shalda
    This document discusses sources of active compounds for medicinal chemistry, including plants, microbes, and marine organisms. It describes some examples of traditionally used plants and their active compounds. It also discusses approaches to drug discovery such as isolation of active substances, structure elucidation, structure-activity relationships, and synthesis of lead compounds. The target of penicillin is mentioned as the bacterial cell wall.

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    1-Pendahuluan Kimia Medisinal

    Uploaded by

    amalia shalda
    93 views39 pages
    This document discusses sources of active compounds for medicinal chemistry, including plants, microbes, and marine organisms. It describes some examples of traditionally used plants and their active compounds. It also discusses approaches to drug discovery such as isolation of active substances, structure elucidation, structure-activity relationships, and synthesis of lead compounds. The target of penicillin is mentioned as the bacterial cell wall.

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    This document discusses sources of active compounds for medicinal chemistry, including plants, microbes, and marine organisms. It describes some examples of traditionally used plants and their active compounds. It also discusses approaches to drug discovery such as isolation of active substances, structure elucidation, structure-activity relationships, and synthesis of lead compounds. The target of penicillin is mentioned as the bacterial cell wall.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    93 views39 pages

    1-Pendahuluan Kimia Medisinal

    Uploaded by

    amalia shalda
    This document discusses sources of active compounds for medicinal chemistry, including plants, microbes, and marine organisms. It describes some examples of traditionally used plants and their active compounds. It also discusses approaches to drug discovery such as isolation of active substances, structure elucidation, structure-activity relationships, and synthesis of lead compounds. The target of penicillin is mentioned as the bacterial cell wall.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 39

    Pendahuluan kimia medisinal

    Suryawati, M.Sc., Apt.


    Sumber zat aktif
    • Plant-derived

    • A different set of metabolites is sometimes produced in the


    different anatomical parts of the plant (e.g. root, leaves and
    flower),
    Tanaman Tradisional
    • Echinacea purpurea, Echinacea
    angustifolia, dan Echinacea
    pallida  meningkatkan daya
    tahan tubuh

    • Mek : meningkatkan sirkulasi sel


    darah putih serta meningkatkan
    produksi sitokin.

    • Efek samping yang muncul


    biasanya adalah alergi.

    • Pada penggunaan jangka waktu


    lama echinaceae dapat
    menyebabkan hepatotoksisitas
    atau kerusakan pada hati
    Tanaman Tradisional
    • Khasiat
    - Berdasarkan data klinis
    (hiperlipidemia, pencegahan
    aterosklerosis dan hipertensi ringan)

    - Berdasarkan penggunaan tradisional


    (dispepsia, infeksi pernafasan dan
    saluran kemih serta rematik)

     Senyawa yg
    paling penting
    untuk
    khasiatnya
    adalah senyawa
    sulfur allicin
    Brokoli (Brassica oleracea Var
    italica)
    Khasiat
    • mempercepat
    penyembuhan penyakit
    • menghambat
    perkembangan sel-sel
    kanker di dalam tubuh.
    • mencegah serangan stroke.
    • Menurunkan gula darah
    (chromium dan serat)
    • mencegah penyakit
    pengeroposan tulang
    (osteoporosis)
    ARAH PENELITIAN

    Uji
    Isolasi Obat
    aktivitas,
    toksisitas zat aktif baru
    Penghambatan beberapa enzim tertentu yang terlibat dalam
    regulasi glukosa dapat mengatasi hiperglikemia
    • Total polyphenol
    • Tannin
    • Flavonoid
    • Flavanol
    Microbial metabolites

    • Microbes compete for living space and nutrients. To survive in


    these conditions, many microbes have developed abilities to
    prevent competing species from proliferating. Microbes are
    the main source of antimicrobial drugs.

    • Streptomyces isolates have been such a valuable source of


    antibiotics, that they have been called medicinal molds. The
    classic example of an antibiotic discovered as a defense
    mechanism against another microbe is penicillin in bacterial
    cultures contaminated by Penicillium fungi in 1928
    Marine invertebrates

    • Arabinose nucleosides discovered from marine invertebrates


    in 1950s, demonstrated for the first time that sugar moieties
    other than ribose and deoxyribose can yield bioactive
    nucleoside structures.

    • For example, the cone snail toxin ziconotide, also known as


    Prialt treats severe neuropathic pain.

    • Several other marine-derived agents are now in clinical trials


    for indications such as cancer, anti-inflammatory use and pain.
    One class of these agents are bryostatin-like compounds,
    under investigation as anti-cancer therapy
    Chemical diversity
    • enabling the efficient generation of large screening libraries for
    the needs of high-throughput screening.
    • exhibit much greater chemical diversity, distributing more
    evenly to the chemical space.

    • differences between natural products and compounds in


    combinatorial chemistry libraries are :
    • the number of chiral centers (much higher in natural
    compounds),
    • structure rigidity (higher in natural compounds) and
    • number of aromatic moieties (higher in combinatorial
    chemistry libraries).
    • Other chemical differences between these two groups include
    the nature of heteroatoms (O and N enriched in natural
    products, and S and halogen atoms more often present in
    synthetic compounds), as well as level of non-aromatic
    unsaturation (higher in natural products).

    • As both structure rigidity and chirality are well-established


    factors in medicinal chemistry known to enhance compounds
    specificity and efficacy as a drug, it has been suggested that
    natural products compare favourably to today's combinatorial
    chemistry libraries as potential lead molecules.
    Synthesis
    • medicinal chemists will attempt to use structure-activity
    relationships (SAR) to improve certain features of the lead
    compound:
    • increase activity against the chosen target
    • reduce activity against unrelated targets
    • improve the druglikeness or ADME properties of the molecule.
    Structural elucidation
    • Chemical compounds exist in nature as mixtures, so the
    combination of liquid chromatography and mass
    spectrometry (LC-MS) is often used to separate the individual
    chemicals. Databases of mass spectras for known compounds
    are available, and can be used to assign a structure to an
    unknown mass spectrum.

    • Nuclear magnetic resonance spectroscopy is the primary


    technique for determining chemical structures of natural
    products. NMR yields information about individual hydrogen
    and carbon atoms in the structure, allowing detailed
    reconstruction of the molecule’s architecture.
    TRIGONELLA FOENUM dan aktivitas antihiperglikemik
    Langkah menuju penemuan zat aktif
    Cara kerja
    HUBUNGAN STRUKTUR AKTIVITAS
    Target obat
    • In general, "new targets" are all those targets that are not
    "established targets" but which have been or are the subject
    of drug discovery campaigns. These typically include newly
    discovered proteins, or proteins whose function has now
    become clear as a result of basic scientific research

    • The majority of targets currently selected for drug discovery


    efforts are proteins. Two classes predominate: G-protein-
    coupled receptors (or GPCRs) and protein kinases.
    Target penisilin : dinding sel bakteri

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