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Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.

ABSTRACT: Tetrahydropyrazolo[1,5-a]pyrimidine scaffold was identified as a hit series from a Mycobacterium tuberculosis (Mtb) whole cell high through-put screening (HTS) campaign. A series of derivatives of this class were synthesized to evaluate their structure-activity relationship (SAR) and structure-property relationship (SPR). Compound 9 had a promising in vivo DMPK profile in mouse and exhibited potent in vivo activity in a mouse efficacy model, achieving a reduction of 3.5 log CFU of Mtb after oral administration to infected mice once a day at 100 mg/kg for 28 days. Thus, compound 9 is a potential candidate for inclusion in combination therapies for both drug-sensitive and drug-resistant TB.

SUBMITTER: Yokokawa F

PROVIDER: S-EPMC4027361 | biostudies-literature | 2013 May

REPOSITORIES: biostudies-literature

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Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.

Yokokawa Fumiaki F Wang Gang G Chan Wai Ling WL Ang Shi Hua SH Wong Josephine J Ma Ida I Rao Srinivasa P S SP Manjunatha Ujjini U Lakshminarayana Suresh B SB Herve Maxime M Kounde Cyrille C Tan Bee Huat BH Thayalan Pamela P Ng Seow Hwee SH Nanjundappa Mahesh M Ravindran Sindhu S Gee Peck P Tan Maria M Wei Liu L Goh Anne A Chen Pei-Yu PY Lee Kok Sin KS Zhong Chen C Wagner Trixie T Dix Ina I Chatterjee Arnab K AK Pethe Kevin K Kuhen Kelli K Glynne Richard R Smith Paul P Bifani Pablo P Jiricek Jan J

ACS medicinal chemistry letters 20130401 5

Tetrahydropyrazolo[1,5-a]pyrimidine scaffold was identified as a hit series from a Mycobacterium tuberculosis (Mtb) whole cell high through-put screening (HTS) campaign. A series of derivatives of this class were synthesized to evaluate their structure-activity relationship (SAR) and structure-property relationship (SPR). Compound 9 had a promising in vivo DMPK profile in mouse and exhibited potent in vivo activity in a mouse efficacy model, achieving a reduction of 3.5 log CFU of Mtb after oral ...[more]

PMID: 24900693

Dataset Information

Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.

Publications

Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.

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