Sandip B. Bharate

Bio: Sandip B. Bharate is an academic researcher from Council of Scientific and Industrial Research. The author has contributed to research in topics: Chemistry & Apoptosis. The author has an hindex of 34, co-authored 204 publications receiving 4566 citations. Previous affiliations of Sandip B. Bharate include University of Montana & Academy of Scientific and Innovative Research.

Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review

Abstract: Studies of active drug/excipient compatibility represent an important phase in the preformulation stage of the development of all dosage forms. The potential physical and chemical interactions between drugs and excipients can affect the chemical nature, the stability and bioavailability of drugs and, consequently, their therapeutic efficacy and safety. The present review covers the literature reports of interaction and incompatibilities of commonly used pharmaceutical excipients with different active pharmaceutical ingredients in solid dosage forms. Examples of active drug/excipient interactions, such as transacylation, the Maillard browning reaction, acid base reactions and physical changes are discussed for different active pharmaceutical ingredients belonging to different therapeutic categories viz antiviral, anti-inflammatory, antidiabetic, antihypertensive, anti-convulsant, antibiotic, bronchodialator, antimalarial, antiemetic, antiamoebic, antipsychotic, antidepressant, anticancer, anticoagulant and sedative/hypnotic drugs and vitamins. Once the solid-state reactions of a pharmaceutical system are understood, the necessary steps can be taken to avoid reactivity and improve the stability of drug substances and products.

Anti-HIV natural products

Abstract: Acquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus (HIV), is an immuno- suppressive disease that results in life -threatening oppor- tunistic infections and malignancies. Despite continuous advances made in antiretrovira l therapy, AIDS has become the leading cause of death in Africa and fourth worldwide; the number of people with HIV is increasing at an alarming rate in India and Southeast Asia. Biodiversity of the plant kingdom has always provided a source of new drug candidates for almost all disease areas. The number of compounds exhibiting anti-HIV activity and isolated from natural sources is increasing steadily. Calanolide A, a coumarin isolated from Callophyllum lanigerum and two other natural product-derived molecules, DSB and 3-hydroxymethyl- 4-methyl DCK are phase II clinical candidates, with potential to come up as drugs for treatment of HIV i nfec- tion. Here, the natural products possessing anti-HIV activity have been discussed, with main focus on recent outcomes from natural sources as anti-HIV agents. ACQUIRED immunodeficiency syndrome (AIDS) is a clinical syndrome that is the result of infection with human i mmuno- deficiency virus (HIV), which causes profound i mmuno- suppression. It has been a serious, life -threatening health problem since the first case was identified in 1981 and is the most quickly spreading disease of the century. Since the epidemic began, more than 60 million people have been infected with the virus. HIV/AIDS is now the leading cause of death in Sub-Saharan Africa. Worldwide, it is the fourth biggest killer. According to recent reports of WHO and UNAIDS, at the end of 2004, an estimated 40 million people (37.2 million adults and 2.2 million children) globally were living with HIV, out of which about 22 million had died. The most affected is Sub-Saharan Africa, where 3.1 million adults and children became infected with HIV during the year 2004 and 2.3 million died in 2004. By the end of 2004, the total number of people living with HIV/ AIDS in the region has reached 25.4 million 1 . Around 1.2 million people in Asia acquired HIV in 2004, bringing the number of people living with HIV to an estimated 8.2 million. A further 540,000 people are estimated to have died of AIDS in 2004. The spread of HIV in India has been di- verse, with much of India having a low rate of infection and the epidemic being most extreme in the southern states. As of December 2004, 92% of all nationally reported AIDS cases has been found in 10 of the 28 states and 7 union territories. The greatest numbers were in Maharashtra and Gujarat in the west; Tamil Nadu and Andhra Pradesh in the south; and Manipur in the Northeast. In the southern states, the infections are mostly due to heterosexual contact, while infections are mainly found amongst injecting drug- users in Manipur and Nagaland. The maximum number of AIDS cases has been reported in Tamil Nadu (44,492) followed by Maharashtra (12,783) out of 96,978 AIDS cases in year 2004. A very high proportion of men and women infected with HIV virus are in their active reproductive ages and around half of the people who acquire HIV become infected before they turn 25. Of greater concern is the possibility of infected mothers transferring the disease to their babies

Metal-free domino one-pot protocols for quinoline synthesis

Abstract: Quinoline is one of the most widely investigated scaffolds by synthetic chemists because of its medicinal importance. A wide range of metal-catalyzed, metal-free, multi-step or domino one-pot protocols are reported in the literature for construction of this scaffold. Several reviews have appeared on synthetic aspects of this scaffold, however there is no focused review on metal-free domino one-pot protocols. Domino one-pot protocols offer an opportunity to access highly functionalized final products from simple starting materials. Because of this unique feature of domino protocols, in recent years their utility for generation of molecular libraries has been widely appreciated. In this review, all contributions till March 2015 are surveyed with particular emphasis on metal-free domino reactions for quinoline ring construction and are discussed herein along with mechanistic aspects.

I and i

Abstract: There is, I think, something ethereal about i —the square root of minus one. I remember first hearing about it at school. It seemed an odd beast at that time—an intruder hovering on the edge of reality. Usually familiarity dulls this sense of the bizarre, but in the case of i it was the reverse: over the years the sense of its surreal nature intensified. It seemed that it was impossible to write mathematics that described the real world in …

International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2

Abstract: There are at least two types of cannabinoid receptors (CB1 and CB2). Ligands activating these G protein-coupled receptors (GPCRs) include the phytocannabinoid Δ9-tetrahydrocannabinol, numerous synthetic compounds, and endogenous compounds known as endocannabinoids. Cannabinoid receptor antagonists have also been developed. Some of these ligands activate or block one type of cannabinoid receptor more potently than the other type. This review summarizes current data indicating the extent to which cannabinoid receptor ligands undergo orthosteric or allosteric interactions with non-CB1, non-CB2 established GPCRs, deorphanized receptors such as GPR55, ligand-gated ion channels, transient receptor potential (TRP) channels, and other ion channels or peroxisome proliferator-activated nuclear receptors. From these data, it is clear that some ligands that interact similarly with CB1 and/or CB2 receptors are likely to display significantly different pharmacological profiles. The review also lists some criteria that any novel “CB3” cannabinoid receptor or channel should fulfil and concludes that these criteria are not currently met by any non-CB1, non-CB2 pharmacological receptor or channel. However, it does identify certain pharmacological targets that should be investigated further as potential CB3 receptors or channels. These include TRP vanilloid 1, which possibly functions as an ionotropic cannabinoid receptor under physiological and/or pathological conditions, and some deorphanized GPCRs. Also discussed are 1) the ability of CB1 receptors to form heteromeric complexes with certain other GPCRs, 2) phylogenetic relationships that exist between CB1/CB2 receptors and other GPCRs, 3) evidence for the existence of several as-yet-uncharacterized non-CB1, non-CB2 cannabinoid receptors; and 4) current cannabinoid receptor nomenclature.

Natural product synthesis using multicomponent reaction strategies.

Abstract: The preparation of urea by Wöhler constituted a landmark achievement in organic chemistry, and it laid the ground for the early days of target-oriented organic synthesis.1 Since then, significant progress has been achieved in this discipline; many powerful single bond forming reactions and asymmetric variants have been developed. These discoveries have paved the way for the stereoselective assembly of complex organic molecules, a task deemed inconceivable by early practitioners. A great many strategies were invented by chemists in order to facilitate the synthesis of complex natural products.2 One avenue in emulating nature’s efficiency would * To whom correspondence should be addressed. E-mail: dennis.hall@ ualberta.ca. † Novartis Institute for Biomedical Research. ‡ Department of Chemistry, University of Alberta. Chem. Rev. 2009, 109, 4439–4486 4439

Biomedical Importance of Indoles

Abstract: The indole nucleus is an important element of many natural and synthetic molecules with significant biological activity. This review covers some of the relevant and recent achievements in the biological, chemical and pharmacological activity of important indole derivatives in the areas of drug discovery and analysis.