應(yīng)用藥物化學(xué)

1、會(huì)計(jì)學(xué)1應(yīng)用藥物化學(xué)應(yīng)用藥物化學(xué)第一節(jié)第一節(jié) 引言引言一、天然生物活性物質(zhì)一、天然生物活性物質(zhì)OOCH3CH3OCH3OOOOCH3OOCH3CH3OH還原青蒿素OOCH3OOCH3CH3OCH3蒿甲醚OOCH3OOCH3CH3OCOCH2 CH2 CO2Na青蒿 琥酯CO2CH3OCOHNCH3可卡因NHCOCH2N(C2H5)2CH3CH3利多卡因H2NCOOCH2CH2N(C25)2普魯卡因(C2H5)2H2NCOOCH2CH2N(C25)2C4H9丁卡因(C2H5)2CH3-N-CH2CH2-OCOCH3 CH3CH3乙酰膽堿 CH3-N CH-O-COCHCH2 CH CH2 CH2

2、 OHCH2 CH CH3阿托品CH-COOCH2CH2N(R)2RCH-COOCH2CH2NC2H5C2H5阿地芬寧山莨菪堿HCH2OHCHOOCNCH3HO樟柳堿CH3NOCOOCHCH2OHHOH1920乙酸(活化型)多步OCOOHHOCH3SCoAHMG-CoAHMG-CoA還原酶NADPHCOOHHOCH3OH甲羥戊酸膽固醇多步21美伐他汀OOHOA-XA為CH=CH或CH2-CH2X為芳環(huán)2223琥珀酰L脯氨酸NOOHOCO2H巰甲丙脯氨酸CO2HOONCH3HS 琥珀酰L脯氨酸能抑制血管緊張素轉(zhuǎn)化酶活性的物質(zhì)，具有降壓作用。24NHNCH3NH22-甲基組胺NHNNH2H3C4-

3、甲基組胺丁咪硫脲NHNSNHCH3NHOSNNH2（C H3)2NSO2NH2雷尼替丁25262728NCONHNH2異煙肼異丙煙肼NCONHNHCH(CH3)229第三節(jié)第三節(jié)3132NNNNHOOCCHOHSOHOHClClNNONHC(CH3)3OHNHNH2NH2CCHHOHCH3NHOCH3C2H5O NHCONH2C2H5NHCONH2NHNNH2CHOCH2CH2N(CH3)2OH CH2OH NHCNF Cl CN COOH SO3H CONHCNOSNCNNNO2NHHOHOCH CH NH2OH H去甲腎上腺素 類似物HOHOCH CH NH2H H多巴胺多巴胺HOHOCH

4、 CH NH2多巴胺原藥類似物潛伏化藥特點(diǎn)前藥生物前體組成原藥基團(tuán)、片斷或載體原藥結(jié)構(gòu)改變，無載體親脂性變化較大變化較小活性反應(yīng)水解氧化或還原催化反應(yīng)化學(xué)作用或酶解只有酶催化C HC O NHNH2SC O O HO氨芐青霉素RCOC H2OCC (C H3)3OO匹氨西林RCOC H2OOH+OCC (C H3)3OHHCHO + R-C O O HC HC O NHNH2SC H3C H3OR=NCNHRONC H2R=HR=羧酸和酚類 酯 原藥水解CC H2C H2C O O HO芬布芬CC H2C H2C O O HO HHC H C HC H2C O O HC H2C HC H2C O O HO HC H2C C H2C O O HO氧化C H2C O O H聯(lián)苯乙酸7980HOHOCH CH NH2OH H去甲腎上腺素 類似物HOHOCH CH NH2H H多巴胺多巴胺HOHOCH CH NH2多巴胺C H C