Characterisation of novel anti-HIV/tuberculosis natural product analogues.

نویسندگان

  • Z W Chen
  • G Liu
  • X F Lu
  • L Liu
  • X Zhang
  • T C K Lau
  • S K W Tsui
  • Y X Kang
  • P R Zheng
  • B J Zheng
چکیده

Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are one of the key components of antiretroviral drug regimens against human immunodeficiency virus type 1 (HIV-1) replication. (+)-calanolide A, which is purified from the rainforest plant Calophyllum, is an anti-HIV-1/ tuberculosis drug. In our previous study, a library of (+)-calanolide A was constructed and one novel compound 10-chloromethyl-11demethly-12-oxocalanolide A (F18) with improved antiviral activity was identified. This study investigated antiviral breadth, drug-resistance profile, and underlying mechanism of action of F18.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Sansanmycin natural product analogues as potent and selective anti-mycobacterials that inhibit lipid I biosynthesis

Tuberculosis (TB) is responsible for enormous global morbidity and mortality, and current treatment regimens rely on the use of drugs that have been in use for more than 40 years. Owing to widespread resistance to these therapies, new drugs are desperately needed to control the TB disease burden. Herein, we describe the rapid synthesis of analogues of the sansanmycin uridylpeptide natural produ...

متن کامل

Design, Synthesis and Anti-Tubercular Activity of Novel 1, 4-Dihydropyrine-3, 5-Dicarboxamide Containing 4(5)-Chloro-2-Ethyl-5(4)-Imidazolyl Moiety

Current researches have showed that N3, N5-diaryl-2, 6-dimethyl -1, 4-dihydropyrine-3, 5- dicarboxamide analogues demonstrate notable anti-tubercular activity. In this study, Hantzsch condensation was used to design and synthesize new analogues of dihydropyridine (DHP). Different diary carboxamides were inserted at positions 3 and 5 of the DHP ring. 4(5)-chloro-2-ethyl-5(4)-imidazolyl moiety wa...

متن کامل

Design, Synthesis and Anti-Tubercular Activity of Novel 1, 4-Dihydropyrine-3, 5-Dicarboxamide Containing 4(5)-Chloro-2-Ethyl-5(4)-Imidazolyl Moiety

Current researches have showed that N3, N5-diaryl-2, 6-dimethyl -1, 4-dihydropyrine-3, 5- dicarboxamide analogues demonstrate notable anti-tubercular activity. In this study, Hantzsch condensation was used to design and synthesize new analogues of dihydropyridine (DHP). Different diary carboxamides were inserted at positions 3 and 5 of the DHP ring. 4(5)-chloro-2-ethyl-5(4)-imidazolyl moiety wa...

متن کامل

Venom Components of Iranian Scorpion Hemiscorpius lepturus Inhibit the Growth and Replication of Human Immunodeficiency Virus 1 (HIV-1)

Background: During the recent years, significant progress has been achieved on development of novel anti-viral drugs. Natural products are assumed as the potential sources of novel anti-viral drugs; therefore, there are some previous studies reporting the anti-viral compounds from venomous animals. Based on the significant value for tracing of non-toxic anti-viral agents from natural resources,...

متن کامل

Application of Genetic Algorithms for Pixel Selection in MIA-QSAR Studies on Anti-HIV HEPT Analogues for New Design Derivatives

Quantitative structure-activity relationship (QSAR) analysis has been carried out with a series of 107 anti-HIV HEPT compounds with antiviral activity, which was performed by chemometrics methods. Bi-dimensional images were used to calculate some pixels and multivariate image analysis was applied to QSAR modelling of the anti-HIV potential of HEPT analogues by means of multivariate calibration,...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Hong Kong medical journal = Xianggang yi xue za zhi

دوره 21 Suppl 7  شماره 

صفحات  -

تاریخ انتشار 2015