Letters in Drug Design & Discovery - Volume 15, Issue 8, 2018

Background: 2-Indolinone is a bicycle, heterocyclic compound analogous of indole skeleton containing a carbonyl group at 2-position of the 5-membered ring. Recently, different biological evaluations of oxindole derivatives have been reported. A variety of compounds with oxindoles moiety exhibit useful pharmaceutical properties like anti-inflammatory, anti-bacterial, anticancer, anti-proliferative, anti-hypertensive, anti-HIV Read More

Background: Novel, more lipophilic analogs of pralidoxime - 2-PAM (K347, K087) and 4-PAM (K349, K120) have been tested in this study due to the recently discovered fact that monoquaternary AChE reactivators penetrate BBB in higher amount. In vitro tests were run against the several organophosphorus agents including tabun, sarin, cyclosarin, soman, VX-agent, Russian VX-agent, diisopropylfluorophosphate and chlorp Read More

Background: The cationic surfactants are a huge group of compounds with thousands of applications. Quaternary Ammonium Salts (QAS) make up the majority of this group. Their countless applications in chemistry, the food industry and textile industry are indubitable. The antibacterial and antifungal effect of the various novel QAS is usually referred to in comparison with commercially used benzalkonium and pyridinium salt Read More

Background: Bacterial biofilms are a cause of a number of infections and are associated with specific drug resistance. In particular, dental biofilm can consist of up to 100 bacterial species and may result in the diseases in the teeth and the surrounding tissues, including dental caries and periodontal diseases. Moreover, pathogens from the dental biofilm can migrate to other organs and lead to systemic diseases. Thus, it is Read More

Background: Plectrantus barbatus Andr. (Lamiaceae) has been used in Hindu and Ayurvedic Indian traditional as well as Brazilian folk medicine for the treatment of several diseases. Chemical investigation of different parts of this plant has led to isolation of essential oil, diterpenes (abietane and labdane), flavonoids, phenolic compounds with interesting biological properties. The objective of study was to isolate pure new chemical Read More

Background: Chromene, benzochromene and their derivatives have been considered as an important class of oxygen-containing heterocycles. There has been increasing interest in the study of chromenes and benzochromenes due to their biological and pharmacological activities. Methods: 3-Amino-1-(4-chlorophenyl)-9-hydroxy-1H-benzo[f]chromene-2-carbonitrile (3) was used as precursor for the synthesis of novel 1H-benz Read More

Background: Novel 4-(3-(4-ethylpiperazin-1-yl)propoxy)-N-phenylbenzamide derivatives (C-1 to C-10) and (4-(3-(4-ethylpiperazin-1-yl)propoxy)phenyl)(4-(2-methoxyphenyl)piperazin-1- yl)ethanone derivatives (C-11 to C-16) were designed and synthesized by pharmacophore approach. Methods: All compounds were evaluated for their in-vitro cytotoxicity against a panel of three cancer cell lines (A-549 human Read More

Background: Nowadays inflammation recognized as the underlying basis of number of diseases but still NSAIDS are the first drugs of choice having several side effects. In addition to that, oxidative stress also triggers the inflammation. This creates an initiation to introduce new molecules which act as efficient COX-2 inhibitors with diminished side effects. Objective: As a part of our search for newer agents, we designed a series of Read More

Background: One of the successful approaches for rational design of bioactive compounds is the bioisosterism strategy. Thus, the bioisosteric relation of thieno[2,3-d]pyrimidin-4- ones with quinazolines, cytosine and uracil resulted in the generation of compounds with variety of biological properties including antiparasitic activity. In contrast to mammals, all parasites are unable to synthesize purines de novo and rely instea Read More

Introduction: Bacterial infections account for maximum deaths worldwide than for any other single cause. Methods: Here in, we report a convenient synthesis of new fluoroquinolone molecules substituted with endo- nortropine and its derivatives at C-7position. All the synthesized molecules, when screened for their antibacterial activity by agar diffusion method against Vibrio cholerae, Bacillus subtilis, Staphylococcus aureus and Es Read More

Background: Natural products have been an exemplary source of new drugs as they have served as direct or indirect precursors for many currently available medicines. The natural product β -elemene has been used clinically in the treatment of various cancers; however, its efficacy is hampered by its poor solubility and bioavailability. Methods: An aldehyde metabolite of β-elemene, 13-β-elemenal, was further identified Read More