Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities

Nafees Ahmed; Keyur G Brahmbhatt; Shabana Khan; Melissa Jacob; Babu Lal Tekwani; Sudeep Sabde; Debashis Mitra; Inder Pal Singh; Ikhlas Khan; Kamlesh Kumar Bhutani

doi:10.1111/cbdd.1427

Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities

Nafees Ahmed, Keyur G Brahmbhatt, Shabana Khan, Melissa Jacob, Babu Lal Tekwani, Sudeep Sabde, Debashis Mitra, Inder Pal Singh, Ikhlas Khan, Kamlesh Kumar Bhutani

Malaysia Jeffrey Cheah Sch of Med & HS

Research output: Contribution to journal › Article › Research › peer-review

18 Citations (Scopus)

Abstract

Fifty analogues of batzelladine K were synthesized and evaluated for in vitro antimalarial (Plasmodium falciparum), antileishmanial (Leishmania donovani), antimicrobial (panel of bacteria and fungi), antiviral (HIV-1) activities. Analogues 14h and 20l exhibited potential antimalarial activity against chloroquine-sensitive D6 strain with IC50 1.25 and 0.88?m and chloroquine-resistant W2 strain with IC50 1.64 and 1.07?m, respectively. Analogues 12c and 14c having nonyl substitution showed the most potent antileishmanial activity with IC50 2.39 and 2.78?m and IC90 11.27 and 12.76?m, respectively. Three analogues 12c, 14c, and 14i were the most active against various pathogenic bacteria and fungi with IC50

Original language	English
Pages (from-to)	491 - 498
Number of pages	8
Journal	Chemical Biology & Drug Design
Volume	81
Issue number	4
DOIs	https://doi.org/10.1111/cbdd.1427
Publication status	Published - 2013

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Ahmed, N., Brahmbhatt, K. G., Khan, S., Jacob, M., Tekwani, B. L., Sabde, S., Mitra, D., Singh, I. P., Khan, I., & Bhutani, K. K. (2013). Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities. Chemical Biology & Drug Design, 81(4), 491 - 498. https://doi.org/10.1111/cbdd.1427

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title = "Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities",

abstract = "Fifty analogues of batzelladine K were synthesized and evaluated for in vitro antimalarial (Plasmodium falciparum), antileishmanial (Leishmania donovani), antimicrobial (panel of bacteria and fungi), antiviral (HIV-1) activities. Analogues 14h and 20l exhibited potential antimalarial activity against chloroquine-sensitive D6 strain with IC50 1.25 and 0.88?m and chloroquine-resistant W2 strain with IC50 1.64 and 1.07?m, respectively. Analogues 12c and 14c having nonyl substitution showed the most potent antileishmanial activity with IC50 2.39 and 2.78?m and IC90 11.27 and 12.76?m, respectively. Three analogues 12c, 14c, and 14i were the most active against various pathogenic bacteria and fungi with IC50",

author = "Nafees Ahmed and Brahmbhatt, {Keyur G} and Shabana Khan and Melissa Jacob and Tekwani, {Babu Lal} and Sudeep Sabde and Debashis Mitra and Singh, {Inder Pal} and Ikhlas Khan and Bhutani, {Kamlesh Kumar}",

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doi = "10.1111/cbdd.1427",

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volume = "81",

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}

Ahmed, N, Brahmbhatt, KG, Khan, S, Jacob, M, Tekwani, BL, Sabde, S, Mitra, D, Singh, IP, Khan, I & Bhutani, KK 2013, 'Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities', Chemical Biology & Drug Design, vol. 81, no. 4, pp. 491 - 498. https://doi.org/10.1111/cbdd.1427

Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities. / Ahmed, Nafees; Brahmbhatt, Keyur G; Khan, Shabana et al.
In: Chemical Biology & Drug Design, Vol. 81, No. 4, 2013, p. 491 - 498.

Research output: Contribution to journal › Article › Research › peer-review

TY - JOUR

T1 - Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities

AU - Ahmed, Nafees

AU - Brahmbhatt, Keyur G

AU - Khan, Shabana

AU - Jacob, Melissa

AU - Tekwani, Babu Lal

AU - Sabde, Sudeep

AU - Mitra, Debashis

AU - Singh, Inder Pal

AU - Khan, Ikhlas

AU - Bhutani, Kamlesh Kumar

PY - 2013

Y1 - 2013

N2 - Fifty analogues of batzelladine K were synthesized and evaluated for in vitro antimalarial (Plasmodium falciparum), antileishmanial (Leishmania donovani), antimicrobial (panel of bacteria and fungi), antiviral (HIV-1) activities. Analogues 14h and 20l exhibited potential antimalarial activity against chloroquine-sensitive D6 strain with IC50 1.25 and 0.88?m and chloroquine-resistant W2 strain with IC50 1.64 and 1.07?m, respectively. Analogues 12c and 14c having nonyl substitution showed the most potent antileishmanial activity with IC50 2.39 and 2.78?m and IC90 11.27 and 12.76?m, respectively. Three analogues 12c, 14c, and 14i were the most active against various pathogenic bacteria and fungi with IC50

AB - Fifty analogues of batzelladine K were synthesized and evaluated for in vitro antimalarial (Plasmodium falciparum), antileishmanial (Leishmania donovani), antimicrobial (panel of bacteria and fungi), antiviral (HIV-1) activities. Analogues 14h and 20l exhibited potential antimalarial activity against chloroquine-sensitive D6 strain with IC50 1.25 and 0.88?m and chloroquine-resistant W2 strain with IC50 1.64 and 1.07?m, respectively. Analogues 12c and 14c having nonyl substitution showed the most potent antileishmanial activity with IC50 2.39 and 2.78?m and IC90 11.27 and 12.76?m, respectively. Three analogues 12c, 14c, and 14i were the most active against various pathogenic bacteria and fungi with IC50

UR - http://onlinelibrary.wiley.com/doi/10.1111/cbdd.1427/pdf

U2 - 10.1111/cbdd.1427

DO - 10.1111/cbdd.1427

M3 - Article

SN - 1747-0277

VL - 81

SP - 491

EP - 498

JO - Chemical Biology & Drug Design

JF - Chemical Biology & Drug Design

IS - 4

ER -

Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal, and anti-HIV activities

Abstract

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