Letters in Drug Design & Discovery - Volume 15, Issue 1, 2018

Background: Mycothiol (MSH), a thiol compound found in Mycobacterium tuberculosis is required for the growth and survival of bacteria. This unusual compound is found only in actinomycetes. MSH biosynthesis involves many enzymes, one of them is MshC an essential enzyme for M. tuberculosis. Methods: NTF1836 were the first MSH biosynthesis inhibitors identified. QSAR studies were performed on a novel series of Read More

Background: A series of purinoxyphenoxypropionates were designed and synthesized by introducing 8-(trifluoromethyl)-9H-purine into the aryloxyphenoxypropionate backbone. Methods: The products were characterized by 1H NMR and HRMS. Results and Conclusion: Preliminary bioassays indicated that most of the compounds exhibited good herbicidal activity at 200 mg/L.

Introduction: The escalating threat due to dwindling effect of antibiotics and challenge of tackling rising drug-resistant infections has gathered high focus in current medicinal research. Methods: In an attempt to find new molecules that can defeat microbial resistance, two new series of 2-[2-substituted ethenyl]-5-(substituted methoxy)-1,3,4-oxadiazole derivatives were synthesized. Various aromatic hydrazides were allowed t Read More

Background: Chlamydiae, characterized by a unique biphasic life cycle, are a group of Gram-negative obligate intracellular bacterial pathogens responsible for diseases in a range of hosts including humans. Benzylidene acylhydrazide CF0001 could inhibit chlamydiae independent of iron starvation and T3SS inhibition. This finding promoted us to design and synthesize more benzylidene acylhydrazides to find novel anti-chl Read More

Background: Spiro[pyrrolidine-3,3'-oxindole] compounds are reported to be highly bioactive natural and synthetic products. Initially, spirooxindole alkaloids were isolated from plants of the Apocynaceae and Rubiaceae families, which were found to have a common scaffold, spiro[pyrrolidine-3,3'-oxindole], exhibiting anticancer activities., we specifically aimed at the synthesis, characterization and anticancer activity of novel s Read More

Background: The synthesis of new hybrid molecules consisting of several heterocyclic pharmacophores namely fluoroquinolone, 1,2,4-triazole, 1,3,4-oxadiazole and piperazine was carried out by conventional and successfully optimized microwave mediated techniques. Methods: The structures of new compounds were confirmed using spectroscopic techniques. These compounds were screened for their antibacterial Read More

Background: Platinum complexes as antitumor agents have received considerable attention due to the clinically approved and have been marketed worldwide such as cisplatin, carboplatin, oxaliplatin or marketed locally such as nedaplatin, lobaplatin and heptaplatin for treatment of various tumor diseases. However, those drugs still had their own defects and they exhibited side effects including nephrotoxicity, ototoxicity, ne Read More

Background: As reported EGFR is a sialoglycoprotein with tyrosine kinase activity involved in control of cellular survival, multiplication, differentiation and metastasis. Dysregulation or aberrant expression of EGFR has been implicated in cell transformation and having oncogenic roles in a number of human cancers. Therefore EGFR has become a significant target for developing targeted therapy for cancer. Methods: A novel series Read More

Background: Nerium oleander extract preparations have been used in the Arab folkmedicine for the treatment of solid tumors. Objective: In the current investigation, bioassay-guided fractionation of N. oleander stem methanolic extract was performed to identify the active compound(s) responsible for its antiproliferative activity and the mechanism of action of the active compounds was explored. Methods: The methanoli Read More

Background: Overexpression of Angiotensin Type 1 (AT1) receptor along with other deregulated oncogenic factors, for e.g. Vascular Endothelial Growth Factor (VEGF) triggers angiogenesis, which is one of the hallmarks of cancer. AT1 receptor, being a key component of the renin - angiotensin system (RAS), also helps in the regulation of blood pressure. In the present study, we report on the identification of novel An Read More

Background: The prevalence of morbidity and mortality due to infections from parasitic worms and protozoa is on rise especially in third world countries. The situation is further worsened by drug resistant microbial pathogens. Objectives: The antimicrobial and anthelmintic activities associated with substituted furfuraldehyde and 1,8-naphthyridine nucleus of nalidixic acid prompted us to synthesize some new quinolon Read More