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Novel Anti-tubercular drug design:

Code 14121976

Nicotinic acid has no anti-tubercular action but, nicotinamide has anti-tubercular action comparable to that of para-amino salicylic acid.M.tuberculosis has the

Nicotinic Acid        Nicotinamide

Gemfibrozil
ability to split amides so once inside the organism INH is split to isonicotinic acid which is the active form of the drug. Infact INH is inactive against typical mycobacteia which lacks amidase enzyme. Within the organism nicotinamide is split into nicotinic acid which brings about the bacteriostatic action.

In humans nicotinic acid is a hypolipidemic drug. Another group of drug used in humans as a hypolipidemic drug is fibric acid derivative. Both have similar pharmacological action.

1. Both increase HDL.
2. Both decreases TG.
3. Both increase LPL activity.
4. Both increases apo-A.
5. So thought was focused on if fibric acid derivatives could be designed to act as anti tubercular drug

The hydrazide derivative was thought off, as it’s a potent anti tubercular moiety. To support this claim it can be found that almost all anti tubercular drugs have at least an -C=O-NH2 moiety in its structure. It may be proposed that the amide and hydrazide moieties favor the uptake of the drug by the organism.

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ANTI-BIOTICS :

Code: 551975

The anti-biotic activity of d-cycloserine is attributed to its resemblance to d-alanine; it’s proposed that it acts as a false substrate of alanine. So We though of designing a cyclic analogue of aspartic acid. As aspartic acid is an integral part of the protein build up of many microorganism.

In S-1 the –o- moiety incorporated in the ring is replaced by isosteric CH2 group. In S-2 the position of oxygen is interchanged with that of carbon and the carbon moiety is replaced by nitrogen. This scheme closely resembles the modification of alanine to cycloserine.

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ANTI-CONVULSANTS:

Code: 1641946 The plan is to fuse the structures of both these potent anti-convulsants so that it will provide a broad spectrum of action.

It should be noted that almost all anti epileptic drugs have an –amideketo-- group incorporated in them. The amideketo group potenciates the anti - convulsant action. The modified compound has the valpoic acid basic nucleus coupled to the open chain analogue of phenytoin

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NOOTROPICS:

Code: 28111947

WE personally feel that designing a structure isosteric with that of glutamic acid will provide a potent nootropic. The cyclization will increase the lipophilisity and hence easy access through blood-brain barrier.

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VASODIALATOR:

Code: 2651976

if the pyridine nucleus is replaced with cyclohexane moiety it will closely resemble nifeepine. We are interested in this molecule as a vasodilator. It also has the potent CH (CH3) 2 b-blocker moiety.

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HAIR GROWTH PROMOTOR:

Code : 2652002

The 3⁰ nitrogen improves lipid solubility and thus improved penetration through scalp and more effective vasodilatation. No appreciable change in basicity will occur as 10 nitrogen is modified to its 3⁰ nitrogen.

Sildenafil citrate as a hair growth promoter:

Sildenafil citrate has been popular with people as a drug for erectile dysfunction. But we pharmacology who learn the mechanism of action at the molecular level can think of innovative novel implementations. One among them is hair growth.

Already it has been used to treat pulmonary hypertension in neonates successfully in “Amirtha Institute of Technology” of late. Another possibility as we see is hair growth stimulation by improved vasodilatation.

Sildenafil causes increased levels of cGMP by inhibiting the enzyme phosphodiesterase and thus enhancing the effect of nitric oxide. Now why can’t this drug be used to improve blood circulation to scalp and thus improve hair growth?

A novel and enthusiastic idea would be to form a combination of Sildenafil + minoxidil + pilocarpin

Pilocarpine augments the synthesis of nitric acid from endothelial cells. Both nitric oxide and GMP decreases Ca2+ influx, the third constituent minoxidil improves further dilation by another channel (i.e.) k+ channel. There by causing profound vasodilatation by all possible means.

Minoxidil-Finasteride Combo:

Particulars	Minoxidil	Finasteride
Volume of distribution	526 lts	761 lts
Octanol/water coeff	1.24	1.258
Solubility in alcohol	1 in 25	freely
Plasma t1/2	4.2 hrs	4.7 hrs

With the above data it can be easily concluded that if these two drugs are combined in the topical formulation it will prove to be extremely effective.

The advantages are:

1. Due to the more or less similar Octanol/water coefficient finasteride can achieve epidermal penetration similar to that of minoxidil.
2. The topical formulation also alleviates the systemic side effects of finateride like impotence.
3. Minoxidil is formulated as a solution in alcohol. As finasteride is freely soluble in alcohol, the vehicle may not be of concern provided that there is no chemical interaction between the two drugs.

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