Synthesis and structure-activity relationships of novel THF 1β- methylcarbapenems

Yang I. Lin; Panayota Bitha; Subas M. Sakya; Timothy W. Strohmeyer; Zhong Li; Ving J. Lee; Stanley A. Lang; Youjun Yang; Niraja Bhachech; William J. Weiss; Peter J. Petersen; Nilda V. Jacobus; Karen Bush; Raymond T. Testa; Francis P. Tally

doi:10.1016/S0960-894X(97)00282-5

Synthesis and structure-activity relationships of novel THF 1β- methylcarbapenems

Yang I. Lin, Panayota Bitha, Subas M. Sakya, Timothy W. Strohmeyer, Zhong Li, Ving J. Lee, Stanley A. Lang, Youjun Yang, Niraja Bhachech, William J. Weiss, Peter J. Petersen, Nilda V. Jacobus, Karen Bush, Raymond T. Testa, Francis P. Tally

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Abstract

A series of twelve highly active aminomethyl-THF 1β-methylcarbapenems 3a-1 were synthesized. Of these, carbapenems 3a-f demonstrated a spectrum of antimicrobial activity comparable to those of imipenem and meropenem with the exception of only moderate anti-pseudomonal activity. Most importantly, they demonstrated moderate intrinsic oral activity against an E. coli infection in mice.

Original language	English
Pages (from-to)	1671-1676
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	7
Issue number	13
DOIs	https://doi.org/10.1016/S0960-894X(97)00282-5
State	Published - 8 Jul 1997

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Lin, Y. I., Bitha, P., Sakya, S. M., Strohmeyer, T. W., Li, Z., Lee, V. J., Lang, S. A., Yang, Y., Bhachech, N., Weiss, W. J., Petersen, P. J., Jacobus, N. V., Bush, K., Testa, R. T., & Tally, F. P. (1997). Synthesis and structure-activity relationships of novel THF 1β- methylcarbapenems. Bioorganic and Medicinal Chemistry Letters, 7(13), 1671-1676. https://doi.org/10.1016/S0960-894X(97)00282-5

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title = "Synthesis and structure-activity relationships of novel THF 1β- methylcarbapenems",

abstract = "A series of twelve highly active aminomethyl-THF 1β-methylcarbapenems 3a-1 were synthesized. Of these, carbapenems 3a-f demonstrated a spectrum of antimicrobial activity comparable to those of imipenem and meropenem with the exception of only moderate anti-pseudomonal activity. Most importantly, they demonstrated moderate intrinsic oral activity against an E. coli infection in mice.",

author = "Lin, {Yang I.} and Panayota Bitha and Sakya, {Subas M.} and Strohmeyer, {Timothy W.} and Zhong Li and Lee, {Ving J.} and Lang, {Stanley A.} and Youjun Yang and Niraja Bhachech and Weiss, {William J.} and Petersen, {Peter J.} and Jacobus, {Nilda V.} and Karen Bush and Testa, {Raymond T.} and Tally, {Francis P.}",

year = "1997",

month = jul,

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doi = "10.1016/S0960-894X(97)00282-5",

language = "English",

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pages = "1671--1676",

journal = "Bioorganic and Medicinal Chemistry Letters",

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publisher = "Elsevier Ltd",

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Lin, YI, Bitha, P, Sakya, SM, Strohmeyer, TW, Li, Z, Lee, VJ, Lang, SA, Yang, Y, Bhachech, N, Weiss, WJ, Petersen, PJ, Jacobus, NV, Bush, K, Testa, RT & Tally, FP 1997, 'Synthesis and structure-activity relationships of novel THF 1β- methylcarbapenems', Bioorganic and Medicinal Chemistry Letters, vol. 7, no. 13, pp. 1671-1676. https://doi.org/10.1016/S0960-894X(97)00282-5

TY - JOUR

T1 - Synthesis and structure-activity relationships of novel THF 1β- methylcarbapenems

AU - Lin, Yang I.

AU - Bitha, Panayota

AU - Sakya, Subas M.

AU - Strohmeyer, Timothy W.

AU - Li, Zhong

AU - Lee, Ving J.

AU - Lang, Stanley A.

AU - Yang, Youjun

AU - Bhachech, Niraja

AU - Weiss, William J.

AU - Petersen, Peter J.

AU - Jacobus, Nilda V.

AU - Bush, Karen

AU - Testa, Raymond T.

AU - Tally, Francis P.

PY - 1997/7/8

Y1 - 1997/7/8

N2 - A series of twelve highly active aminomethyl-THF 1β-methylcarbapenems 3a-1 were synthesized. Of these, carbapenems 3a-f demonstrated a spectrum of antimicrobial activity comparable to those of imipenem and meropenem with the exception of only moderate anti-pseudomonal activity. Most importantly, they demonstrated moderate intrinsic oral activity against an E. coli infection in mice.

AB - A series of twelve highly active aminomethyl-THF 1β-methylcarbapenems 3a-1 were synthesized. Of these, carbapenems 3a-f demonstrated a spectrum of antimicrobial activity comparable to those of imipenem and meropenem with the exception of only moderate anti-pseudomonal activity. Most importantly, they demonstrated moderate intrinsic oral activity against an E. coli infection in mice.

UR - http://www.scopus.com/inward/record.url?scp=0030795176&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(97)00282-5

DO - 10.1016/S0960-894X(97)00282-5

M3 - Article

AN - SCOPUS:0030795176

SN - 0960-894X

VL - 7

SP - 1671

EP - 1676

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 13

ER -

Synthesis and structure-activity relationships of novel THF 1β- methylcarbapenems

Abstract

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