Oxidation studies on Andrographolide

Jones oxidation of Andrographolide (1), gave mixture of three products (3-dehydroandrographolide (5), 3,19-bis dehydroandrographolide (6) and 19-dehydroandrographolide (7). Tritylation of andrographolide at C19-OH resulted to products 8 and diene 9, which can be converted to its acetate 10 and oxidation product 11.     

Geometry of Coadjoint Orbits and Multiplicity-one Branching Laws for Symmetric Pairs

Consider the restriction of an irreducible unitary representation π of a Lie group G to its subgroup H. Kirillov’s revolutionary idea on the orbit method suggests that the multiplicity of an irreducible H-module ν occurring in the restriction π|_H could be read from the coadjoint action of H on \(\mathcal {O}^{G} \cap \text {pr}^{-1}({\mathcal {O}}^{H})\), provided π and ν are ‘geometric quantizations’ of a G-coadjoint orbit \(\mathcal {O}^{G}\) and an H-coadjoint orbit \(\mathcal {O}^{H}\), respectively, where \(\text {pr} \colon \sqrt {-1}\mathfrak {g}^{\ast } \to \sqrt {-1}\mathfrak {h}^{\ast }\) is the projection dual to the inclusion \(\mathfrak {h} \subset \mathfrak {g}\) of Lie algebras. Such results were previously established by Kirillov, Corwin and Greenleaf for nilpotent Lie groups. In this article, we highlight specific elliptic orbits \(\mathcal {O}^{G}\) of a semisimple Lie group G corresponding to highest weight modules of scalar type. We prove that the Corwin–Greenleaf number \(\sharp (\mathcal {O}^{G} \cap \text {pr}^{-1}({\mathcal {O}}^{H}))/H\) is either zero or one for any H-coadjoint orbit \(\mathcal {O}^{H}\), whenever (G,H) is a symmetric pair of holomorphic type. Furthermore, we determine the coadjoint orbits \(\mathcal {O}^{H}\) with nonzero Corwin–Greenleaf number. Our results coincide with the prediction of the orbit philosophy, and can be seen as ‘classical limits’ of the multiplicity-free branching laws of holomorphic discrete series representations (Kobayashi [Progr. Math. 2007]).     

Synthesis of macrosphelides with a thiazole side chain: new antitumor candidates having apoptosis-inducing property

Hybrid compounds of macrosphelides and epothilones, both of which are natural macrolides having a 16-membered skeleton, were designed and synthesized using a ring-closing metathesis (RCM) strategy. Some of these hybrids were found to exhibit notable apoptosis-inducing activity against human lymphoma cells with higher potency than parent natural macrosphelides, and to be a promising lead compound for development of a new antitumor agent.     

Essential Spectra, Matrix Operator and Applications

This paper gives a survey on some recent results on the spectral theory of block operator matrices. We study the closeness in the product space and we give some conditions to characterize the essential spectra in the Browder resolvent set case. Furthermore, we apply the obtained results to several models such as delay equations, Sturm–Liouville problem and transport equations.     

Facile one-pot synthesis,butyrylcholinesterase and α-glucosidase inhibitory activities,structure–activity relationship,molecular docking and DNA–drug binding analysis of Meldrum’s acid derivatives

Research on Chemical Intermediates - Meldrum’s acid derivatives were facile synthesized by one-pot condensation process and characterized by NMR (1H, 13C, DEPT-90 and DEPT-135) and EI-MS. The...     

Novel class of hybrid natural products derived from lupeol as antimalarial agents

Thirty-four novel hybrid lupeol derivatives (4-18) were prepared and evaluated for antimalarial activity in vitro against Plasmodium falciparum. Three compounds (13d, 16a and 17a) have shown antimalarial activity at lower dose (10 microg mL(-1)) than lupeol.     

Synthesis of unsymmetrical substituted 1,4-dihydropyridines through thermal and microwave assisted [4+2] cycloadditions of 1-azadienes and allenic esters

Thermal and microwave assisted [4+2] cycloadditions of 1,4-diaryl-1-aza-1,3-butadienes with allenic esters lead to cycloadducts, which after a 1,3-H shift afford variedly substituted unsymmetrical 2-alkyl-1,4-diaryl-3-ethoxycarbonyl-1,4-dihydropyridines in high yields. Reactions carried out under microwave irradiation are cleaner and give higher yields with much shortened reaction times. Density functional theory (DFT) at the B3LYP/6-31G* level has been used to calculate geometric features of the reactants, barrier for s-trans to s-cis and reverse isomerization of azadienes (5a-d, 10a-e), dihedral angles between N(1), C(2), C(3), and C(4) atoms of azadienes along with various indices such as chemical hardness (eta), chemical potential (micro), global electrophilicity (omega), and the difference in global electrophilicity (Deltaomega) between the reacting pairs and Fukui functions (f (+) and f(-)). The results revealed that s-trans is the predominant conformation of azadienes at ambient temperature and the barrier for conversion of the s-trans rotamer of 1-azadienes to s-cis may be the major factor influencing the chemoselectivity, i.e., [4+2] verses [2+2] cycloaddition. The regiochemistry of the observed cycloadditions is collated with the obtained local electrophilicity indices (Fukui functions). Transition states for the formation of both [4+2] and [2+2] cycloadducts as located at the PM3 level indicate that the transition state for the formation of [4+2] cycloadducts has lower energy, again supporting the earlier conclusion that preferred formation of [4+2] cycloaaducts at higher temperature may be a consequence of barrier for s-trans to s-cis transformation of 1-azadienes.     

An eco-friendly multi-analyte high-performance thin layer chromatographic densitometric determination of amoxicillin,metronidazole, and famotidine in their ternary mixtures and simulated gastric juice: A promising protocol for eradicating Helicobacter pylori

Gastrointestinal tract disorders constitute a heavy burden to healthcare providers. To eradicate Helicobacter pylori infection, different triple therapy protocols have been proposed. Among which are combinations of proton pump inhibitors (e.g., omeprazole), histamine-2 receptor antagonists (e.g., famotidine), along with antibiotics (e.g., amoxicillin). In this work, a sensitive and accurate high-performance thin-layer chromatographic method was developed for the simultaneous determination of amoxicillin, metronidazole, and famotidine in bulk powder and laboratory-prepared combined-tablet mixtures. Complete separation of the cited compounds was achieved using pre-coated silica gel plates with a mixture of methanol:chloroform:toluene:water:glacial acetic acid (5:2:1.5:0.5:0.1 v/v/v/v/v) as the mobile phase. The method was fully validated as per the international conference of harmonization guidelines. Good linearity, a correlation coefficient of 0.9991, was obtained in the concentration ranges 0.1–1.6 μg/band (amoxicillin), 0.1–0.9 μg/band (metronidazole), and 0.1–0.9 μg/band (famotidine). Since the method allowed the determination of the three compounds in combined tablets with a high degree of selectivity, accuracy, precision, with cost-effectiveness, it could be used for regular quality control. Moreover, the applicability of the proposed method was extended to the determination of the ternary mixture in simulated gastric juice. Method greenness was assessed using different green metrics.