Siva S. Panda

Design and synthesis of spiro[indole-thiazolidine]spiro[indole-pyrans] as antimicrobial agents.

A series of novel spiro[indole-thiazolidine]spiro[indole-pyran] derivatives were synthesized from N-(bromoalkyl)indol-2,3-diones via monospiro-bisindole intermediates; the two indole nuclei being connected via N-(CH(2))(n)-N linker. Synthesized compounds were evaluated for their antimicrobial activities in vitro against three Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis, and Staphylococcus epidermis), four Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi, and Klebsiella pneumonia) as well as four fungi (Aspergillus niger, Aspergillus fumigatus, Aspergillus flavus, and Candida albicans) using Cup plate method. Bis spiro-indoles exhibited stronger antibacterial and antifungal efficiency than their corresponding mono spiro-indoles. Compound 10e, the most active derivative was shown to inhibit the growth of all bacterial strains and two fungal strains (A. niger and C. albicans).

Biginelli Reaction: A Green Perspective

The Biginelli Reaction is a one-pot acid catalysed cyclocondensation of � -keto ester, urea and aromatic aldehyde which leads to the synthesis of functionalised 3,4-dihydro-2(H)-pyrimidinones (DHPMs). This three-component reaction for the synthesis of dihydro- pyrimidinone and corresponding dihydropyrimidinethiones has now been known for more than a century since first reported in 1893. Owing to the increasing use of Green technology approach, due to its various merits over Classical methodology and as a need for sus- tainable Chemistry, this reaction has received renewed interest for preparing DHPMs in an environmentally thoughtful manner with im- proved yields. The classical reaction has been modified in the recent past by using various catalysts and several structural variants in dif- ferent solvents to synthesize large number of Biginelli type compounds. Also, these DHPMs (synthetic and natural) possess a wide range of pharmacological activities. We hereby wish to compile, in this present review, the literature available methods related to large number of Biginelli type compounds synthesized using eco-friendly technologies. This protocol couples the benefits of Biginelli reaction with that of greener approach for organic transformations, thus facilitating efficient synthesis of bioactive compounds in environmentally be- nign way.

Novel antibacterial active quinolone-fluoroquinolone conjugates and 2D-QSAR studies.

Novel, quinolone-fluoroquinolone conjugates 10a-f, 11a-f, 13a-f and 14a-f with amino acid linkers were synthesized in good yields utilizing benzotriazole chemistry. Antibacterial bioassay showed the synthesized bis-conjugates exhibit anti-bacterial properties comparable with the parent drugs.

Synthesis of 2-Arylbenzimidazoles in Water

Abstract A simple and efficient procedure for the synthesis of 2-arylbenzimidazoles through a one-pot condensation of o-phenylenediamines with aryl aldehydes in water is described. Short reaction time, large-scale synthesis, easy and quick isolation of the product, and excellent yield are the main advantages of this procedure.

Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.

Amino acid conjugates of quinolone, metronidazole and sulfadiazine antibiotics were synthesized in good yields using benzotriazole methodology. All the conjugates were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Antibiotic conjugates were tested for activity in four medically relevant organisms; Staphylococcus aureus (RN4220), Escherichia coli (DH5α), Pseudomonas aeruginosa (PAO1), and Bacillus subtilis (168). Several antibiotic conjugates show promising results against several of the strains screened.

Xanthones as Potential Antioxidants

Xanthones (dibenzo-γ-pyrones) constitutes an important class of oxygenated heterocycles and occur as secondary metabolites in plants and microorganisms. They are known for various biological activities such as antioxidant, monoamine oxidase inhibitor, antihypertensive, hepatoprotective, antithrombotic, antifungal and anticancer. The tricyclic scaffold as well as the nature and/or position of the substituents present on it play an important role in displaying various biological activities. The unique structural scaffold and medicinal importance of xanthones have therefore attracted many Scientists in the past, to isolate or synthesize xanthones or their analogs as potential drug candidates. It would not be wrong to call them as close cousins to the polyphenol family that are known to possess strong antioxidant effects on the nervous system. The main two sources of xanthones are: Isolation from natural resources or synthesis. Though few reviews have been published in the past, mainly focusing on the anticancer activities of xanthone derivatives, but there is not a single review which is based on their antioxidant activities. We therefore have made efforts to briefly summarize natural and synthetic xanthones possessing antioxidant activity in this review.

Synthesis and molecular modeling of antimicrobial active fluoroquinolone-pyrazine conjugates with amino acid linkers

Novel fluoroquinolone-pyrazine conjugates 7a-h with amino acid linkers were synthesized in good yields utilizing benzotriazole chemistry. Antimicrobial bioassay showed that the synthesized bis-conjugates have antimicrobial properties comparable to the parent drugs. Compound 7h showed superior antibacterial activity against Staphylococcus aureus and Streptococcus pyogenes (MIC=74.6 μM and 149.3 μM, respectively). This matched well with the estimated values obtained from 3D-pharmacophore and 2D-QSAR studies (MIC=67 μM and 92.9 μM, respectively).

Quinine conjugates and quinine analogues as potential antimalarial agents

Malaria is a tropical disease, prevalent in Southeast Asia and Africa, resulting in over half a million deaths annually; efforts to develop new antimalarial agents are therefore particularly important. Quinine continues to play a role in the fight against malaria, but quinoline derivatives are more widely used. Drugs based on the quinoline scaffold include chloroquine and primaquine, which are able to act against the blood and liver stages of the parasites life cycle. The purpose of this review is to discuss reported biologically active compounds based on either the quinine or quinoline scaffold that may have enhanced antimalarial activity. The review emphasises hybrid molecules, and covers advances made in the last five years. The review is divided into three sections: modifications to the quinine scaffold, modifications to aminoquinolines and finally metal-containing antimalarial compounds.

Quinine bis-conjugates with quinolone antibiotics and peptides: synthesis and antimalarial bioassay

Benzotriazole-mediated syntheses led to novel bis-conjugates of quinine with quinolone antibiotics and amino acid linkers which were successfully prepared by two alternative routes with excellent yields and retention of chirality. These bis conjugates retain in vitro antimalarial activity with IC(50) values ranging from 12 to 207 nM, similar to quinine itself.

Regioselective synthesis and theoretical studies of an anti-neoplastic fluoro-substituted dispiro-oxindole

Single crystal X-ray studies of regioselectively synthesized fluoro-substituted dispiro-oxindole 9 revealed that the structure belongs to the monoclinic space group P21/n with four molecules in the unit cell. The structure was also investigated by AM1, PM3, and DFT studies. Compound 9 exhibits high potency against the HeLa cell line.