Current Bioactive Compounds - Volume 14, Issue 2, 2018

Background: A significant number of heterocyclic compounds were developed as poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. Among them, 2-substituted benzimidazole-4- carboxamide derivatives have gained importance in comparison with other heterocyclic systems.A new library of benzimidazole 4-carboxamides were synthesised and screened for PARP-1 inhibitory activity. Method: A facile and convergent synthesis Read More

Background and objective: Isolate TD-015, obtained from the Thar Desert (India), was subjected to investigation for its antimicrobial activity and identification of the contributing compound(s). Method: TD-015 was isolated from the Thar Desert (India), identified by 16S rDNA sequencing and analyzed for the hyper-variable regions. Culture supernatant of TD-015 was tested for antimicrobial activity following organic solvents ex Read More

Background: Spirocyclic compounds are important because of their unique structure and diverse biological activities. The indolo-spirocyclic scaffold is regularly found as a core structure of a representative family of bioactive natural products and among pharmaceutics, like alstonisine and spirotyprostatine. In the present work, indolo-spirocyclic compounds 3a-g and 4a,b have been successfully synthesized via electrophilic c Read More

Background: Literature review for azetidinone and its derivatives suggested its wide applications in almost every stratum. However, despite the evergreen applicative profile, an increase in resistance towards specific class has been on a parallel increase. Thus, in view of the versatility in synthetic method and step into further assessing the pharmacological profile of this class of compounds, it was thought to synthesize th Read More

Background: Diarrheal disease is a leading cause of mortality and morbidity, especially among children in the developing countries resulting in a major health care problem. So, the present study was designed to investigate antidiarrheal activity and mechanism of action of probiotic using the Swiss mice model of castor oil induced diarrhea. Methods: In the current study, we selected the model of diarrhea induced by castor oil i Read More

Background: Microbes are often internalized by host cells as part of the infection process. Compounds that can modulate such uptake may have applications in prevention of infectious diseases. Capsaicinoids, capsinoids, and other Capsicum sp. components are reported to target several pathological processes including microbial infections. Capsicum phytochemicals can alter biophysical properties of animal cell membran Read More

Background: Epilepsy is a common neurological disorder characterized by recurrent unprovoked seizures. Approximately 60 million people worldwide suffer from epilepsy, making this condition the second leading neurological disorder. Epilepsy also affects about 4% of individuals over their lifetime. The most commonly used anticonvulsant drugs are associated with numerous side effects including ataxia, hepatotoxicity Read More

Background: Infectious diseases are the leaders among the challenging drug targets because of the multi-drug resist antimicrobial pathogens and continuous rise in the emerging infections from known and unknown sources. Though there is an availability of a large number of antibiotics and chemotherapeutics for medical use, the emerging resistance drives it for the search of new classes of antimicrobial agents. In the prese Read More

Background: One of the important chemical agents in designing of anti-convulsant, antiatherosclerotic and anti-cancer drugs are pyridine derivatives. Alkyl and aryl derivatives of cyanopyridones show antimicrobial, antihypertensive, anti-inflammatory, analgesic, antipyretic properties as well as 1KK-b inhibitor properties. Methods: N-acyclic nucleosides 2-5 were synthesized by the reaction of the sodium salt of (4- chlor Read More

Background: This paper aims at establishing pharmacognostic parameters and anatomical descriptors of Ficus palmata Forssk. (Bedu) for the first time by utilizing more sophisticated modalities like HPTLC fingerprinting and scanning electron microscopy (SEM) in addition to the conventional analytical techniques. Ficus palmata Forssk. is a well known, yet minimally explored plant of western Himalaya despite its tremendous tr Read More

Background: The essential oils of Mentha species are used in pharmaceutical, cosmetic and perfume industry and also for flavoring and preservation of several food. Moreover, Mint's essential oils are also searched for their biological activities such as antimicrobial, antioxidant, and cytotoxic properties. Mentha mozaffarianii is an endemic medicinal mint of Iran rich in essential oil, but not yet studied for its cytotxic ac Read More

Background: Human lactate dehydrogenase 5 (hLDH5) represents a promising anticancer target, particularly for the treatment of hypoxic tumors, where it is often hyperexpressed. In fact, by catalyzing the reduction of pyruvate to lactate, hLDH5 allows the survival of tumor cells under hypoxic conditions by means of glycolysis. Despite the efforts dedicated to the identification and development of hLDH5 inhibitors, only few com Read More

Background: Alhagi pseudoalhagi (Camel thorn) is a herbaceous perennial plant. Recently, several investigations have been conducted for its medical and pharmaceutical applications. Methods: The aerial part of the plant was air dried and extracted by different solvents with increasing polarity. The residue from each extract was in-vitro tested against C. albicans that has been previously isolated from vaginal candidiasis Read More