A series of 3 alpha-amino-5 alpha-cholestane and 3 alpha,7 alpha-diamino-5 alpha-cholestane derivatives containing imidazole and pyridine rings were synthesized by simple and effective reductive amination, and their in vitro activities against a range of Gram-positive and Gram-negative strains were evaluated. Most of the compound exhibited enhanced activity against MRSA pathogen. 3 alpha,7 alpha-Di(pyridylmethyl)amino-5 alpha-cholestane 10 showed the highest potency in these series toward the Gram-positive bacteria, Staphylococcus epidermidis 887E, with the lowest MIC value of 1 mu g/mL. (C) 2013 Elsevier Ltd. All rights reserved.
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CSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Bhandari, Kalpana
;
Srinivas, Nagarapu
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CSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Srinivas, Nagarapu
;
Marrapu, Vijay K.
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CSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Marrapu, Vijay K.
;
Verma, Aditya
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CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Verma, Aditya
;
Srivastava, Saumya
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CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Srivastava, Saumya
;
Gupta, Suman
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CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
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Eastern Virginia Med Sch, Ctr Pediat Res, Childrens Hosp Kings Daughters, Norfolk, VA 23501 USAEastern Virginia Med Sch, Ctr Pediat Res, Childrens Hosp Kings Daughters, Norfolk, VA 23501 USA
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Hosp Gen Gran Canaria, Serv Neumol, Las Palmas Gran Canaria, Canary Islands, Spain
Int Union TB & Lung Dis, Paris, FranceHosp Gen Gran Canaria, Serv Neumol, Las Palmas Gran Canaria, Canary Islands, Spain
Caminero, Jose A.
;
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Sotgiu, Giovanni
;
Zumla, Alimuddin
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UCL, Sch Med, Dept Infect, London W1N 8AA, EnglandHosp Gen Gran Canaria, Serv Neumol, Las Palmas Gran Canaria, Canary Islands, Spain
Zumla, Alimuddin
;
Migliori, Giovanni Battista
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Care & Res Inst, Fdn S Maugeri, WHO Collaborating Ctr TB & Lung Dis, Tradate, ItalyHosp Gen Gran Canaria, Serv Neumol, Las Palmas Gran Canaria, Canary Islands, Spain
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Wayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
Chin, Judy N.
;
Jones, Ronald N.
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JMI Labs, N Liberty, IA USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
Jones, Ronald N.
;
Sader, Helio S.
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JMI Labs, N Liberty, IA USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
Sader, Helio S.
;
Savage, Paul B.
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Brigham Young Univ, Dept Chem & Biochem, Provo, UT 84602 USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
Savage, Paul B.
;
Rybak, Michael J.
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Wayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
机构:
CSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Bhandari, Kalpana
;
Srinivas, Nagarapu
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CSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Srinivas, Nagarapu
;
Marrapu, Vijay K.
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CSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Marrapu, Vijay K.
;
Verma, Aditya
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CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Verma, Aditya
;
Srivastava, Saumya
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CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
Srivastava, Saumya
;
Gupta, Suman
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CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, IndiaCSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
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Eastern Virginia Med Sch, Ctr Pediat Res, Childrens Hosp Kings Daughters, Norfolk, VA 23501 USAEastern Virginia Med Sch, Ctr Pediat Res, Childrens Hosp Kings Daughters, Norfolk, VA 23501 USA
机构:
Hosp Gen Gran Canaria, Serv Neumol, Las Palmas Gran Canaria, Canary Islands, Spain
Int Union TB & Lung Dis, Paris, FranceHosp Gen Gran Canaria, Serv Neumol, Las Palmas Gran Canaria, Canary Islands, Spain
Caminero, Jose A.
;
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Sotgiu, Giovanni
;
Zumla, Alimuddin
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UCL, Sch Med, Dept Infect, London W1N 8AA, EnglandHosp Gen Gran Canaria, Serv Neumol, Las Palmas Gran Canaria, Canary Islands, Spain
Zumla, Alimuddin
;
Migliori, Giovanni Battista
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Care & Res Inst, Fdn S Maugeri, WHO Collaborating Ctr TB & Lung Dis, Tradate, ItalyHosp Gen Gran Canaria, Serv Neumol, Las Palmas Gran Canaria, Canary Islands, Spain
机构:
Wayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
Chin, Judy N.
;
Jones, Ronald N.
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机构:
JMI Labs, N Liberty, IA USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
Jones, Ronald N.
;
Sader, Helio S.
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JMI Labs, N Liberty, IA USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
Sader, Helio S.
;
Savage, Paul B.
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Brigham Young Univ, Dept Chem & Biochem, Provo, UT 84602 USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA
Savage, Paul B.
;
Rybak, Michael J.
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Wayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USAWayne State Univ, Eugene Applebaum Coll Pharm & Hlth Sci, Dept Pharm Practice, Antiinfect Res Lab, Detroit, MI 48201 USA